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Summary
PDF (peptide deformylase, mitochondrial, HGNC:30012) is a protein-coding gene on chromosome 16q22.1, encoding Peptide deformylase, mitochondrial (Q9HBH1). Removes the formyl group from the N-terminal Met of newly synthesized proteins.
Protein synthesis proceeds after formylation of methionine by methionyl-tRNA formyl transferase (FMT) and transfer of the charged initiator f-met tRNA to the ribosome. In eubacteria and eukaryotic organelles the product of this gene, peptide deformylase (PDF), removes the formyl group from the initiating methionine of nascent peptides. In eubacteria, deformylation of nascent peptides is required for subsequent cleavage of initiating methionines by methionine aminopeptidase. The discovery that a natural inhibitor of PDF, actinonin, acts as an antimicrobial agent in some bacteria has spurred intensive research into the design of bacterial-specific PDF inhibitors. In human cells, only mitochondrial proteins have N-formylation of initiating methionines. Protein inhibitors of PDF or siRNAs of PDF block the growth of cancer cell lines but have no effect on normal cell growth. In humans, PDF function may therefore be restricted to rapidly growing cells.
Source: NCBI Gene 64146 — RefSeq curated summary.
At a glance
- GWAS associations: 2
- Clinical variants (ClinVar): 9 total
- GTEx eGene: eQTL in 23 tissues, sQTL in 24 (q < 0.05)
- Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 1.98 (unconstrained)
- MANE Select transcript:
NM_022341
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:30012 |
| Approved symbol | |
| Name | peptide deformylase, mitochondrial |
| Location | 16q22.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000258429 |
| Ensembl biotype | protein_coding |
| OMIM | 618720 |
| Entrez | 64146 |
Gene structure
Transcript identifiers
Ensembl transcripts: 5 — 3 protein_coding, 2 nonsense_mediated_decay
MANE Select: ENST00000288022
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 1
ENST00000288022, ENST00001073636, ENST00001125246, ENST00001125247, ENST00001134389
RefSeq mRNA: 1 — MANE Select: NM_022341
NM_022341
CCDS: CCDS10875
Canonical transcript exons
ENST00000288022 — 2 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001031780 | 69329997 | 69330588 |
| ENSE00001601028 | 69326913 | 69329179 |
Expression profiles
Bgee: expression breadth ubiquitous, 131 present calls, max score 81.19.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 7.3239 / max 45.6366, expressed in 1714 samples.
Highest expression (Bgee): male germ line stem cell (sensu Vertebrata) in testis, primordial germ cell in gonad, adult mammalian kidney, lobe of liver, stromal cell of endometrium.
Genetic regulation across tissues (GTEx eQTL / sQTL)
PDF is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 23 tissues and its splicing (sQTL) in 24 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
showing 20 of 47 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Skin Sun Exposed Lower leg | sqtl | 7.1e-20 | -0.55 | 16:69334093:C:A |
| Skin Sun Exposed Lower leg | eqtl | 2.8e-19 | -0.29 | 16:69334093:C:A |
| Artery Tibial | eqtl | 1.0e-17 | -0.35 | 16:69328549:C:G |
| Cells Cultured fibroblasts | eqtl | 4.6e-17 | -0.22 | 16:69338024:A:G |
| Skin Not Sun Exposed Suprapubic | eqtl | 7.6e-17 | -0.29 | 16:69322792:A:G |
| Skin Not Sun Exposed Suprapubic | sqtl | 8.4e-17 | -0.47 | 16:69207984:T:C |
| Artery Aorta | eqtl | 2.7e-12 | -0.38 | 16:69315882:T:C |
| Nerve Tibial | eqtl | 3.5e-10 | -0.25 | 16:69389213:A:G |
| Thyroid | eqtl | 3.8e-10 | -0.26 | 16:69207984:T:C |
| Brain Cortex | sqtl | 6.6e-10 | -0.65 | 16:69338024:A:G |
| Adipose Subcutaneous | sqtl | 6.9e-10 | -0.34 | 16:69321060:A:G |
| Artery Tibial | sqtl | 8.7e-10 | +0.41 | 16:69341755:G:A |
| Adipose Subcutaneous | eqtl | 1.1e-09 | -0.21 | 16:69334093:C:A |
| Brain Frontal Cortex BA9 | sqtl | 9.0e-09 | -0.62 | 16:69338024:A:G |
| Esophagus Muscularis | eqtl | 3.3e-08 | -0.26 | 16:69341755:G:A |
| Lung | sqtl | 3.9e-08 | -0.36 | 16:69344542:A:G |
| Adipose Visceral Omentum | sqtl | 8.8e-08 | -0.32 | 16:69334093:C:A |
| Esophagus Mucosa | eqtl | 1.7e-07 | -0.19 | 16:69340558:G:C |
| Adipose Visceral Omentum | eqtl | 6.2e-07 | -0.21 | 16:69162112:T:C |
| Esophagus Muscularis | sqtl | 9.8e-07 | -0.39 | 16:69341755:G:A |
FANTOM5 promoters
3 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 157897 | 5.8335 | 1681 |
| 157896 | 0.8955 | 476 |
| 157895 | 0.5949 | 333 |
Top tissues by expression
showing 100 of 134 tissues by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 81.19 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 80.63 | gold quality |
| adult mammalian kidney | UBERON:0000082 | 75.56 | gold quality |
| right lobe of liver | UBERON:0001114 | 74.25 | gold quality |
| stromal cell of endometrium | CL:0002255 | 74.00 | gold quality |
| gastrocnemius | UBERON:0001388 | 73.19 | gold quality |
| liver | UBERON:0002107 | 73.12 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 72.99 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 72.69 | gold quality |
| muscle of leg | UBERON:0001383 | 72.40 | gold quality |
| kidney | UBERON:0002113 | 71.72 | gold quality |
| metanephros cortex | UBERON:0010533 | 71.48 | gold quality |
| cortex of kidney | UBERON:0001225 | 71.33 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 71.07 | gold quality |
| right adrenal gland | UBERON:0001233 | 70.18 | gold quality |
| left adrenal gland | UBERON:0001234 | 70.01 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 69.81 | gold quality |
| monocyte | CL:0000576 | 69.80 | gold quality |
| leukocyte | CL:0000738 | 69.76 | gold quality |
| esophagus mucosa | UBERON:0002469 | 69.23 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 69.15 | gold quality |
| muscle tissue | UBERON:0002385 | 68.97 | gold quality |
| superior frontal gyrus | UBERON:0002661 | 68.70 | gold quality |
| body of pancreas | UBERON:0001150 | 68.48 | gold quality |
| cortical plate | UBERON:0005343 | 68.20 | gold quality |
| adrenal gland | UBERON:0002369 | 67.84 | gold quality |
| primary visual cortex | UBERON:0002436 | 67.48 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 67.24 | gold quality |
| endometrium | UBERON:0001295 | 66.88 | gold quality |
| granulocyte | CL:0000094 | 66.63 | gold quality |
| heart left ventricle | UBERON:0002084 | 66.34 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 66.07 | gold quality |
| esophagus | UBERON:0001043 | 65.82 | gold quality |
| duodenum | UBERON:0002114 | 65.74 | gold quality |
| saliva-secreting gland | UBERON:0001044 | 65.71 | gold quality |
| minor salivary gland | UBERON:0001830 | 65.57 | gold quality |
| transverse colon | UBERON:0001157 | 65.24 | gold quality |
| body of stomach | UBERON:0001161 | 65.18 | gold quality |
| bone marrow cell | CL:0002092 | 65.10 | silver quality |
| skin of leg | UBERON:0001511 | 64.93 | gold quality |
| left coronary artery | UBERON:0001626 | 64.75 | gold quality |
| zone of skin | UBERON:0000014 | 64.68 | gold quality |
| skin of abdomen | UBERON:0001416 | 64.57 | gold quality |
| tonsil | UBERON:0002372 | 64.23 | gold quality |
| heart | UBERON:0000948 | 64.08 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 63.71 | gold quality |
| thoracic aorta | UBERON:0001515 | 63.52 | gold quality |
| fundus of stomach | UBERON:0001160 | 63.47 | gold quality |
| colon | UBERON:0001155 | 63.42 | gold quality |
| ascending aorta | UBERON:0001496 | 63.41 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 63.38 | gold quality |
| ectocervix | UBERON:0012249 | 63.38 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 63.35 | gold quality |
| placenta | UBERON:0001987 | 63.29 | gold quality |
| stomach | UBERON:0000945 | 63.27 | gold quality |
| myometrium | UBERON:0001296 | 63.22 | gold quality |
| bone marrow | UBERON:0002371 | 63.16 | gold quality |
| popliteal artery | UBERON:0002250 | 63.10 | gold quality |
| tibial artery | UBERON:0007610 | 63.09 | gold quality |
| apex of heart | UBERON:0002098 | 63.00 | gold quality |
| right atrium auricular region | UBERON:0006631 | 62.90 | gold quality |
| thyroid gland | UBERON:0002046 | 62.80 | gold quality |
| body of uterus | UBERON:0009853 | 62.73 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 62.68 | gold quality |
| intestine | UBERON:0000160 | 62.57 | gold quality |
| small intestine | UBERON:0002108 | 62.56 | gold quality |
| thoracic mammary gland | UBERON:0005200 | 62.53 | gold quality |
| lower esophagus | UBERON:0013473 | 62.53 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 62.52 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 62.51 | gold quality |
| pancreas | UBERON:0001264 | 62.49 | gold quality |
| adipose tissue | UBERON:0001013 | 62.48 | gold quality |
| ventricular zone | UBERON:0003053 | 62.46 | gold quality |
| left uterine tube | UBERON:0001303 | 62.45 | gold quality |
| right coronary artery | UBERON:0001625 | 62.45 | gold quality |
| omental fat pad | UBERON:0010414 | 62.44 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 62.37 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 62.27 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 62.26 | gold quality |
| right frontal lobe | UBERON:0002810 | 62.20 | gold quality |
| prostate gland | UBERON:0002367 | 62.09 | gold quality |
| multicellular organism | UBERON:0000468 | 61.99 | gold quality |
| vagina | UBERON:0000996 | 61.91 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 61.84 | gold quality |
| urinary bladder | UBERON:0001255 | 61.82 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 61.48 | gold quality |
| spleen | UBERON:0002106 | 61.46 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 61.45 | gold quality |
| lymph node | UBERON:0000029 | 61.38 | gold quality |
| right ovary | UBERON:0002118 | 60.73 | gold quality |
| uterine cervix | UBERON:0000002 | 60.71 | gold quality |
| endocervix | UBERON:0000458 | 60.47 | gold quality |
| rectum | UBERON:0001052 | 60.45 | gold quality |
| Ammon’s horn | UBERON:0001954 | 60.43 | gold quality |
| blood | UBERON:0000178 | 59.98 | gold quality |
| putamen | UBERON:0001874 | 59.50 | gold quality |
| adenohypophysis | UBERON:0002196 | 59.38 | gold quality |
| left ovary | UBERON:0002119 | 59.33 | gold quality |
| ovary | UBERON:0000992 | 59.18 | gold quality |
| lung | UBERON:0002048 | 59.07 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 1.97 |
HPA expression
RNA tissue specificity: Low tissue specificity
showing 60 of 79 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM | Protein (IHC) |
|---|---|---|---|
| Frontal cortex | tissue | 20.7 | |
| Caudate putamen | tissue | 18.2 | |
| Cerebellum | tissue | 16.8 | low |
| Basal ganglia | tissue | 15.2 | medium |
| Hippocampal formation | tissue | 14.9 | |
| Cerebral cortex | tissue | 14.5 | medium |
| Putamen | tissue | 14.5 | |
| Somatosensory cortex | tissue | 14.5 | |
| Ventral forebrain | tissue | 14.0 | |
| Occipital cortex | tissue | 14.0 | |
| Temporal cortex | tissue | 13.9 | |
| Olfactory bulb | tissue | 13.7 | |
| Retrosplenial and cingulate cortex | tissue | 13.6 | |
| Retrosplenial cortex | tissue | 13.5 | |
| Insular cortex | tissue | 13.4 | |
| Prefrontal cortex | tissue | 13.2 | |
| Entorhinal cortex | tissue | 13.1 | |
| Amygdala | tissue | 13.0 | |
| Motor cortex | tissue | 12.7 | |
| Septum | tissue | 12.7 | |
| Corpus callosum | tissue | 11.8 | |
| Periaqueductal gray | tissue | 10.7 | |
| Hypothalamus | tissue | 10.5 | |
| Midbrain | tissue | 10.2 | |
| Spinal cord | tissue | 10.0 | |
| Thalamus | tissue | 9.9 | |
| Superior colliculi | tissue | 9.9 | |
| Medulla oblongata | tissue | 9.5 | |
| Pons | tissue | 9.4 | |
| Substantia nigra | tissue | 9.4 | |
| Hippocampus | tissue | 9.4 | medium |
| Choroid plexus | tissue | 8.4 | |
| Postcentral gyrus | tissue | 6.9 | |
| Locus coeruleus | tissue | 6.5 | |
| Nucleus accumbens | tissue | 6.1 | |
| Skeletal muscle | tissue | 4.2 | medium |
| Kidney | tissue | 2.4 | high |
| Stomach 1 | tissue | 2.3 | medium |
| Salivary gland | tissue | 2.2 | medium |
| Pancreas | tissue | 2.2 | medium |
| Liver | tissue | 2.1 | medium |
| Duodenum | tissue | 1.9 | medium |
| Colon | tissue | 1.7 | medium |
| Adipose tissue | tissue | 1.6 | not detected |
| Parathyroid gland | tissue | 1.5 | medium |
| Vagina | tissue | 1.4 | medium |
| Small intestine | tissue | 1.4 | high |
| Thyroid gland | tissue | 1.3 | medium |
| Pituitary gland | tissue | 1.2 | |
| Prostate | tissue | 1.2 | low |
| Bone marrow | tissue | 1.2 | not detected |
| Skin 1 | tissue | 1.1 | high |
| Esophagus | tissue | 1.1 | medium |
| Spleen | tissue | 1.1 | low |
| Lymph node | tissue | 1.0 | medium |
| Adrenal gland | tissue | 1.0 | high |
| Appendix | tissue | 0.9 | medium |
| Breast | tissue | 0.8 | medium |
| Heart muscle | tissue | 0.8 | high |
| Rectum | tissue | 0.8 | medium |
Brain sub-regions (HPA Brain Atlas): detected in 290; highest nTPM — Blood vessel (42.1), Dorsal hippocampus (14.9), Ventral hippocampus (13.8), Subiculum (12.6), White matter (11.8).
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): TP53
miRNA regulators (miRDB)
Targeting PDF by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).
28 miRNAs:
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-4267 | 99.96 | 66.53 | 2368 |
| HSA-MIR-6842-5P | 99.80 | 67.54 | 1587 |
| HSA-MIR-7110-5P | 99.80 | 67.84 | 1712 |
| HSA-MIR-6752-5P | 99.59 | 67.32 | 1243 |
| HSA-MIR-6751-5P | 99.56 | 64.99 | 1145 |
| HSA-MIR-548AH-5P | 99.52 | 69.73 | 2626 |
| HSA-MIR-4480 | 99.42 | 66.02 | 735 |
| HSA-MIR-4279 | 99.19 | 66.70 | 2437 |
| HSA-MIR-520G-3P | 98.91 | 67.38 | 1914 |
| HSA-MIR-520H | 98.91 | 67.38 | 1914 |
| HSA-MIR-887-5P | 98.82 | 65.90 | 1347 |
| HSA-MIR-219A-2-3P | 98.62 | 68.78 | 797 |
| HSA-MIR-934 | 98.49 | 70.44 | 581 |
| HSA-MIR-4691-5P | 98.41 | 66.77 | 1343 |
| HSA-MIR-6792-3P | 98.41 | 66.86 | 1359 |
| HSA-MIR-6810-5P | 98.29 | 66.21 | 975 |
| HSA-MIR-450A-2-3P | 97.91 | 67.56 | 1459 |
| HSA-MIR-30C-1-3P | 97.80 | 66.36 | 1499 |
| HSA-MIR-30C-2-3P | 97.80 | 66.45 | 1499 |
| HSA-MIR-6788-5P | 97.80 | 66.41 | 1532 |
| HSA-MIR-3127-5P | 97.52 | 65.24 | 786 |
| HSA-MIR-509-3-5P | 97.21 | 67.74 | 1517 |
| HSA-MIR-509-5P | 97.21 | 67.90 | 1512 |
| HSA-MIR-4418 | 97.04 | 67.16 | 1372 |
| HSA-MIR-212-5P | 96.83 | 67.43 | 950 |
| HSA-MIR-4652-5P | 96.46 | 64.22 | 553 |
| HSA-MIR-1258 | 96.08 | 67.74 | 700 |
| HSA-MIR-187-3P | 81.56 | 59.38 | 111 |
Functional genomics
gnomAD constraint: pLI 9.77e-17, LOEUF 1.98, missense Z -3.86 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD RMC): no regional variation along ENST00000288022 — one region, missense o/e 1.23.
Literature-anchored findings (GeneRIF, showing 7)
- The inhibition of HsPDF may provide an explanation for the mechanism by which actinonin is cytotoxic against various human tumor cell lines. (PMID:14637138)
- Despite the lack of true S2’ and S3’ binding pockets, confirmed through peptide binding modeling, enzyme kinetics suggest a combined contribution from P2’and P3’ positions of a formylated peptide substrate to turnover. (PMID:19236878)
- the origin, evolution and preservation of the COG8/PDF same-strand overlap follow similar mechanistic steps as those documented for antisense overlaps where gain and/or loss of splice sites and polyadenylation signals seems to drive the process. (PMID:21805148)
- these data reveals that PDF has several transcription start sites, the most important of which only 18 bp from the initiation codon. (PMID:22554513)
- This is the first report showing that PDF is over-expressed in breast, colon, and lung cancers (PMID:23815882)
- c-myc regulated the expression of human PDF. (PMID:24675470)
- compound M7594_0037 exhibited potent anticancer activities against HeLa, A549 and MCF-7 cell lines with IC50s of 35.26, 29.63 and 24.63 muM, respectively. Molecular docking studies suggested that M7594_0037 and its three derivatives could interact with Human peptide deformylase by several conserved hydrogen bonds. (PMID:27023495)
Cross-species orthologs
5 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | ENSDARG00000013950 | |
| mus_musculus | ENSMUSG00000078931 | |
| rattus_norvegicus | ENSRNOG00000022303 | |
| drosophila_melanogaster | CG31278 | FBGN0051278 |
| drosophila_melanogaster | CG31373 | FBGN0051373 |
Additional cross-species homologs
Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.
| Organism | UniProt | Identity | Method |
|---|---|---|---|
| Streptomyces coelicolor A3(2) | Q9RD27 | 85.0% | Diamond |
| Bifidobacterium adolescentis ATCC 15703 | A1A2Z1 | 83.5% | Diamond |
| Streptomyces avermitilis MA-4680 = NBRC 14893 | Q825U9 | 83.5% | Diamond |
| Bifidobacterium longum NCC2705 | Q8G534 | 83.5% | Diamond |
| Oryza sativa Japonica Group | B6RGY0 | 75.4% | Diamond |
| Solanum lycopersicum | Q9FUZ0 | 75.4% | Diamond |
| Arabidopsis thaliana | Q9FV53 | 74.2% | Diamond |
| Gloeobacter violaceus PCC 7421 | Q7NJV3 | 47.4% | Diamond |
| Rickettsia conorii str. Malish 7 | Q92JI7 | 43.0% | Diamond |
Genomic neighbors (locus context)
Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).
| Symbol | Type | Entrez |
|---|---|---|
| VPS4A | protein-coding | 27183 |
| NIP7 | protein-coding | 51388 |
| SNTB2 | protein-coding | 6645 |
| COG8 | protein-coding | 84342 |
| UTP4 | protein-coding | 84916 |
| DERPC | protein-coding | 113455421 |
| HAS3 | protein-coding | 3038 |
| CHTF8 | protein-coding | 54921 |
| TMED6 | protein-coding | 146456 |
| TERF2 | protein-coding | 7014 |
| CYB5B | protein-coding | 80777 |
Protein
Protein identifiers
Peptide deformylase, mitochondrial — Q9HBH1 (reviewed: Q9HBH1)
Alternative names: Polypeptide deformylase
All UniProt accessions (1): Q9HBH1
UniProt curated annotations — full annotation on UniProt →
Function. Removes the formyl group from the N-terminal Met of newly synthesized proteins.
Subunit / interactions. Homodimer.
Subcellular location. Mitochondrion.
Tissue specificity. Ubiquitous.
Cofactor. Binds 1 Co(2+) ion.
Similarity. Belongs to the polypeptide deformylase family.
RefSeq proteins (1): NP_071736* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR023635 | Peptide_deformylase | Family |
| IPR036821 | Peptide_deformylase_sf | Homologous_superfamily |
Pfam: PF01327
Enzyme classification (BRENDA)
- EC 3.5.1.88 — peptide deformylase (BRENDA: 55 organisms, 191 substrates, 745 inhibitors, 156 Km, 135 kcat entries)
Substrate kinetics (BRENDA)
95 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| N-FORMYL-MET-ALA-SER | 0.25–48 | 17 |
| FORMYL-MET-ALA | 0.14–28 | 15 |
| FORMYL-MET-ALA-SER | 0.2–70 | 15 |
| FORMYL-MET-ALA-LYS-TYR | 0.34–7.6 | 7 |
| N-FORMYL-MET-ALA | 2.9–480 | 7 |
| N-FORMYLMETHIONYL-LEU-P-NITROANILIDE | 0.018–0.028 | 4 |
| N-FORMYL-L-MET-L-VAL | 7.1–12.4 | 3 |
| N-FORMYL-MET-SER-ASN-GLU | 2–5.5 | 3 |
| N-FORMYL-NLE-ALA-SER | 0.6–11 | 3 |
| FORMYL-MET-LEU-P-NITROANILIDE | 0.024–0.047 | 2 |
| FORMYL-MTHQ | 1.56–2.287 | 2 |
| N-FORMYL-ASP(NH2) | 0.74–1 | 2 |
| N-FORMYL-BETA-THIAPHENYLALANYL-LYS-P-NITROANILID | 0.027–0.03 | 2 |
| N-FORMYL-GLY(NH2) | 2.9–4.3 | 2 |
| N-FORMYL-MET-LEU-GLU | 8–12 | 2 |
Catalyzed reactions (Rhea)
- N-terminal N-formyl-L-methionyl-[peptide] + H2O = N-terminal L-methionyl-[peptide] + formate (RHEA:24420)
UniProt features (26 total): helix 10, binding site 6, strand 5, transit peptide 1, chain 1, sequence variant 1, region of interest 1, active site 1
Structure
Experimental structures (PDB)
2 structures by resolution:
| PDB | Title | Method | Resolution (Å) |
|---|---|---|---|
| 3G5K | Structure and activity of human mitochondrial peptide deformylase, a novel cancer target | X-RAY DIFFRACTION | 1.7 |
| 3G5P | Structure and activity of human mitochondrial peptide deformylase, a novel cancer target | X-RAY DIFFRACTION | 1.7 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9HBH1-F1 | 86.21 | 0.75 |
Human Protein Atlas
Protein class: Enzymes, ENZYME proteins, Hydrolases, Metabolic proteins, Predicted intracellular proteins
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): mitochondria; nucleoplasm
Antibody reliability (HPA): IH approved · IF approved
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (1)
| Position | Role |
|---|---|
| 215 |
Ligand- & substrate-binding residues (6)
| Position | Role |
|---|---|
| 71 | substrate |
| 169 | substrate |
| 171 | substrate |
| 172 | Co(2+) |
| 214 | Co(2+) |
| 218 | Co(2+) |
Function
Pathways and Gene Ontology
Reactome pathways
0 curated (TAS) of 0; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
MSigDB gene sets: 85 (showing top):
BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, chr16q22, GOBP_TRANSLATION, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, ZHOU_INFLAMMATORY_RESPONSE_LIVE_DN, TIEN_INTESTINE_PROBIOTICS_24HR_UP, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_DN, NAKAMURA_TUMOR_ZONE_PERIPHERAL_VS_CENTRAL_UP, KIM_WT1_TARGETS_DN, LIU_COMMON_CANCER_GENES, GOMF_HYDROLASE_ACTIVITY_ACTING_ON_CARBON_NITROGEN_BUT_NOT_PEPTIDE_BONDS_IN_LINEAR_AMIDES, GOMF_HYDROLASE_ACTIVITY_ACTING_ON_CARBON_NITROGEN_BUT_NOT_PEPTIDE_BONDS, GRABARCZYK_BCL11B_TARGETS_DN, CHEMNITZ_RESPONSE_TO_PROSTAGLANDIN_E2_DN, GOBP_POSITIVE_REGULATION_OF_CELL_POPULATION_PROLIFERATION
GO Biological Process (4): translation (GO:0006412), positive regulation of cell population proliferation (GO:0008284), peptidyl-methionine modification (GO:0018206), post-translational protein modification (GO:0043687)
GO Molecular Function (3): peptide deformylase activity (GO:0042586), metal ion binding (GO:0046872), hydrolase activity (GO:0016787)
GO Cellular Component (1): mitochondrion (GO:0005739)
GO top-level categories
16 GO namespaces:
| Category | Terms |
|---|---|
| protein modification process | 2 |
| peptidyltransferase activity | 1 |
| translational initiation | 1 |
| translational elongation | 1 |
| translational termination | 1 |
| macromolecule biosynthetic process | 1 |
| protein metabolic process | 1 |
| protein biosynthetic process | 1 |
| cell population proliferation | 1 |
| regulation of cell population proliferation | 1 |
| positive regulation of cellular process | 1 |
| hydrolase activity, acting on carbon-nitrogen (but not peptide) bonds, in linear amides | 1 |
| cation binding | 1 |
| catalytic activity | 1 |
| cytoplasm | 1 |
| intracellular membrane-bounded organelle | 1 |
Experimentally-supported GO annotations
GO terms backed by direct experimental evidence (ECO experimental codes) — 5 of 8 annotations. The rest are phylogenetic / computational / electronic (IEA).
5 experimentally-supported GO terms:
| GO term | NS | Evidence |
|---|---|---|
| peptidyl-methionine modification | BP | direct assay |
| positive regulation of cell population proliferation | BP | mutant phenotype |
| post-translational protein modification | BP | direct assay |
| mitochondrion | CC | direct assay |
| peptide deformylase activity | MF | direct assay |
Protein interactions and networks
STRING
showing 15 of 1,118 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| MTFMT | Q96DP5 | 773 | |
| METAP1D | Q6UB28 | 605 | |
| MRRF | Q96E11 | 547 | |
| METAP1 | P53582 | 546 | |
| TSFM | P43897 | 460 | |
| MARS2 | Q96GW9 | 376 | |
| MARS1 | P56192 | 367 | |
| METAP2 | P50579 | 350 | |
| HIBCH | Q6NVY1 | 334 | |
| HSPE1 | P61604 | 332 | |
| MTRFR | Q9H3J6 | 328 | |
| PCCB | P05166 | 324 | |
| DERA | Q9Y315 | 322 | |
| DHODH | Q02127 | 314 | |
| XPNPEP3 | Q9NQH7 | 313 |
IntAct
Human interaction partners of PDF in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
3 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| PRSS48 | physical association | 0.400 | 1 |
| MYO5B | physical association | 0.000 | 1 |
| RAC1 | physical association | 0.000 | 1 |
BioGRID (104 interactions; top human partners by supporting records): PTCH1 (Affinity Capture-MS; 3 records), TMEM25 (Affinity Capture-MS; 3 records), A2M (Affinity Capture-MS; 2 records), ATP5A1 (Cross-Linking-MS (XL-MS); 2 records), CETN1 (Affinity Capture-MS; 2 records), CRP (Affinity Capture-MS; 2 records), DEFA5 (Affinity Capture-MS; 2 records), ERBB3 (Affinity Capture-MS; 2 records), KIF1B (Affinity Capture-MS; 2 records), MRPS34 (Affinity Capture-MS; 2 records), OLFM4 (Affinity Capture-MS; 2 records), P4HA3 (Affinity Capture-MS; 2 records), PROC (Affinity Capture-MS; 2 records), ACTR5 (Affinity Capture-MS), ADAM21 (Affinity Capture-MS)
Disease & clinical
Genetic variants
Variant evidence for PDF: 9 ClinVar records (0 pathogenic / likely pathogenic); 2 GWAS associations.
ClinVar
9 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 7 |
| Likely benign | 0 |
| Benign | 2 |
SpliceAI
Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 23 predictions of 176):
| Position(s) | Effect | Δscore | Sites |
|---|---|---|---|
| 16:69329180–69329182 | acceptor_loss | 0.9400 | 7 |
| 16:69329817 | donor_gain | 0.9400 | |
| 16:69329888 | donor_gain | 0.9000 | |
| 16:69329798 | donor_gain | 0.8200 | |
| 16:69329995–69329996 | donor_loss | 0.8000 | 6 |
| 16:69329997 | donor_loss | 0.7900 | 3 |
| 16:69329269 | donor_gain | 0.7800 | |
| 16:69329672 | donor_gain | 0.7600 | |
| 16:69329336 | donor_gain | 0.7400 | |
| 16:69329998 | donor_loss | 0.7300 |
AlphaMissense
517 missense substitutions predicted likely pathogenic (of 1,541 scored), across 124 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:
| Residue | Likely-pathogenic substitutions | Mean am_pathogenicity | Max am_pathogenicity |
|---|---|---|---|
| M228 | 9 | 0.881 | 0.965 |
| H214 | 8 | 0.985 | 0.989 |
| H218 | 8 | 0.978 | 0.993 |
| D217 | 8 | 0.975 | 0.991 |
| D226 | 8 | 0.952 | 0.991 |
| S174 | 8 | 0.901 | 0.995 |
| N155 | 8 | 0.899 | 0.992 |
| F233 | 8 | 0.828 | 0.986 |
| F153 | 8 | 0.798 | 0.988 |
| E215 | 7 | 0.975 | 0.996 |
| C172 | 7 | 0.964 | 0.988 |
| E170 | 7 | 0.960 | 0.991 |
| F178 | 7 | 0.959 | 0.990 |
| F224 | 7 | 0.959 | 0.985 |
| W207 | 7 | 0.953 | 0.988 |
| M103 | 7 | 0.930 | 0.977 |
| S112 | 7 | 0.910 | 0.991 |
| Q213 | 7 | 0.905 | 0.992 |
| W238 | 7 | 0.898 | 0.976 |
| F64 | 7 | 0.890 | 0.955 |
HPA cancer prognostics
RNA cancer specificity: Low cancer specificity
Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.
2 prognostic cancer types:
| Cancer | Prognostic | p-value |
|---|---|---|
| Glioblastoma Multiforme (validation) | unfavorable | 0.000235 |
| Rectum Adenocarcinoma (validation) | favorable | 0.000414 |
Disease associations
OMIM: gene MIM:618720 | disease phenotypes:
GWAS associations
2 associations:
| Study | Trait | p-value |
|---|---|---|
| GCST005951_23 | Body mass index | 5e-11 |
| GCST007006_16 | Logical memory (delayed recall) in normal cognition | 7e-7 |
EFO canonical traits (from GWAS)
2 canonical traits:
| EFO ID | Trait name |
|---|---|
| EFO:0004340 | body mass index |
| EFO:0004874 | memory performance |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL4647 (SINGLE PROTEIN)
PharmGKB: 1 entry (CPIC guideline: no)
Binding affinities (BindingDB)
63 measured of 76 human assays (95 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| (R)-2-Butyl-N*1*-((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-N*4*-hydroxy-succinamide | IC50 | 1 nM |
| CHEMBL4637933 | IC50 | 2.8 nM |
| CHEMBL4638057 | IC50 | 3 nM |
| CHEMBL4632607 | IC50 | 3.6 nM |
| CHEMBL4643984 | IC50 | 4.2 nM |
| CHEMBL4639327 | IC50 | 4.9 nM |
| CHEMBL4649534 | IC50 | 4.9 nM |
| CHEMBL4641416 | IC50 | 5 nM |
| CHEMBL4636545 | IC50 | 5 nM |
| CHEMBL4643967 | IC50 | 5.5 nM |
| CHEMBL4636221 | IC50 | 5.9 nM |
| CHEMBL4634572 | IC50 | 5.9 nM |
| (S)-2-[(R)-2-Cyclohexylmethyl-3-(formyl-hydroxy-amino)-propionylamino]-3,3,N,N-tetramethyl-butyramide | IC50 | 6 nM |
| CHEMBL4637166 | IC50 | 6.1 nM |
| CHEMBL4640974 | IC50 | 6.4 nM |
| CHEMBL4645966 | IC50 | 6.5 nM |
| CHEMBL4635093 | IC50 | 7 nM |
| CHEMBL4637631 | IC50 | 7.1 nM |
| CHEMBL4642360 | IC50 | 7.2 nM |
| CHEMBL4635263 | IC50 | 7.2 nM |
| (S)-2-[(R)-2-Cyclopentylmethyl-3-(formyl-hydroxy-amino)-propionylamino]-3,3,N,N-tetramethyl-butyramide | IC50 | 8 nM |
| CHEMBL4645936 | IC50 | 8.7 nM |
| CHEMBL4646467 | IC50 | 8.8 nM |
| CHEMBL4641901 | IC50 | 8.9 nM |
| CHEMBL4640884 | IC50 | 9.3 nM |
| CHEMBL4644600 | IC50 | 9.4 nM |
| CHEMBL4638180 | IC50 | 9.5 nM |
| (R)-2-[(Formyl-hydroxy-amino)-methyl]-4-methyl-pentanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amide | IC50 | 10 nM |
| (R)-2-[(Formyl-hydroxy-amino)-methyl]-heptanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amide | IC50 | 10 nM |
| CHEMBL4636076 | IC50 | 11 nM |
| CHEMBL4645201 | IC50 | 13 nM |
| CHEMBL4643686 | IC50 | 16 nM |
| (S)-2-Mercaptomethyl-hexanoic acid [(S)-5-amino-1-(4-nitro-phenylcarbamoyl)-pentyl]-amide | KI | 19 nM |
| (R)-2-[(Formyl-hydroxy-amino)-methyl]-hex-5-enoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amide | IC50 | 20 nM |
| (S)-2-[(R)-2-Ethylsulfanylmethyl-3-(formyl-hydroxy-amino)-propionylamino]-3,3,N,N-tetramethyl-butyramide | IC50 | 20 nM |
| (S)-2-[(R)-2-Benzyl-3-(formyl-hydroxy-amino)-propionylamino]-3,3,N,N-tetramethyl-butyramide | IC50 | 20 nM |
| (R)-2-[(Formyl-hydroxy-amino)-methyl]-5-methyl-hexanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amide | IC50 | 20 nM |
| (S)-2-[(R)-2-Cyclopentyl-3-(formyl-hydroxy-amino)-propionylamino]-3,3,N,N-tetramethyl-butyramide | IC50 | 20 nM |
| CHEMBL4649755 | IC50 | 29 nM |
| (R)-2-[(Formyl-hydroxy-amino)-methyl]-pent-4-enoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amide | IC50 | 30 nM |
| (R)-2-[(Formyl-hydroxy-amino)-methyl]-octanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amide | IC50 | 30 nM |
| (R)-2-[(Formyl-hydroxy-amino)-methyl]-hex-4-ynoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amide | IC50 | 30 nM |
| CHEMBL4641571 | IC50 | 30 nM |
| CHEMBL5191348 | IC50 | 30 nM |
| (R)-2-[(Formyl-hydroxy-amino)-methyl]-nonanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amide | IC50 | 40 nM |
| (R)-2-[(Formyl-hydroxy-amino)-methyl]-decanoic acid [1-((S)-dimethyl-carbamoyl)-2,2-dimethyl-propyl]-amide | IC50 | 50 nM |
| (R)-2-[(Formyl-hydroxy-amino)-methyl]-pentanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amide | IC50 | 50 nM |
| (R)-N-((S)-1-Dimethylcarbamoyl-2,2-dimethyl-propyl)-2-[(formyl-hydroxy-amino)-methyl]-3-methyl-butyramide | IC50 | 50 nM |
| (S)-2-{(R)-2-[(Formyl-hydroxy-amino)-methyl]-butyrylamino}-3,3,N,N-tetramethyl-butyramide | IC50 | 70 nM |
| (S)-2-[(Formyl-hydroxy-amino)-methyl]-hexanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amide | IC50 | 70 nM |
ChEMBL bioactivities
77 potent at pChembl≥5 of 87 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.52 | Ki | 0.3 | nM | ACTINONIN |
| 9.00 | IC50 | 1 | nM | CHEMBL122067 |
| 8.82 | IC50 | 1.5 | nM | ACTINONIN |
| 8.56 | IC50 | 2.78 | nM | CHEMBL4637933 |
| 8.52 | IC50 | 2.99 | nM | CHEMBL4638057 |
| 8.45 | IC50 | 3.58 | nM | CHEMBL4632607 |
| 8.42 | IC50 | 3.77 | nM | CHEMBL4641062 |
| 8.39 | IC50 | 4.11 | nM | CHEMBL4635911 |
| 8.37 | IC50 | 4.24 | nM | CHEMBL4643984 |
| 8.31 | IC50 | 4.92 | nM | CHEMBL4639327 |
| 8.31 | IC50 | 4.85 | nM | CHEMBL4649534 |
| 8.30 | IC50 | 5.01 | nM | CHEMBL4641416 |
| 8.30 | IC50 | 5.01 | nM | CHEMBL4636545 |
| 8.26 | IC50 | 5.48 | nM | CHEMBL4643967 |
| 8.23 | IC50 | 5.87 | nM | CHEMBL4636221 |
| 8.23 | IC50 | 5.87 | nM | CHEMBL4634572 |
| 8.22 | IC50 | 6 | nM | CHEMBL90193 |
| 8.21 | IC50 | 6.12 | nM | CHEMBL4637166 |
| 8.19 | IC50 | 6.42 | nM | CHEMBL4640974 |
| 8.19 | IC50 | 6.47 | nM | CHEMBL4645966 |
| 8.15 | IC50 | 7.15 | nM | CHEMBL4642360 |
| 8.15 | IC50 | 7.01 | nM | CHEMBL4635093 |
| 8.15 | IC50 | 7.08 | nM | CHEMBL4637631 |
| 8.15 | IC50 | 7 | nM | CHEMBL431210 |
| 8.14 | IC50 | 7.19 | nM | CHEMBL4635263 |
| 8.10 | IC50 | 8 | nM | CHEMBL316099 |
| 8.06 | IC50 | 8.74 | nM | CHEMBL4645936 |
| 8.05 | IC50 | 8.94 | nM | CHEMBL4641901 |
| 8.05 | IC50 | 8.81 | nM | CHEMBL4646467 |
| 8.03 | IC50 | 9.42 | nM | CHEMBL4644600 |
| 8.03 | IC50 | 9.26 | nM | CHEMBL4640884 |
| 8.02 | IC50 | 9.53 | nM | CHEMBL4638180 |
| 8.00 | IC50 | 10 | nM | CHEMBL96864 |
| 8.00 | IC50 | 10 | nM | CHEMBL413726 |
| 8.00 | IC50 | 10 | nM | ACTINONIN |
| 7.96 | IC50 | 10.9 | nM | CHEMBL4636076 |
| 7.88 | IC50 | 13.1 | nM | CHEMBL4645201 |
| 7.79 | IC50 | 16.1 | nM | CHEMBL4643686 |
| 7.72 | Ki | 19 | nM | CHEMBL325246 |
| 7.70 | IC50 | 20 | nM | CHEMBL540441 |
| 7.70 | IC50 | 20 | nM | CHEMBL328502 |
| 7.70 | IC50 | 20 | nM | CHEMBL91882 |
| 7.70 | IC50 | 20 | nM | CHEMBL91835 |
| 7.70 | IC50 | 20 | nM | CHEMBL328688 |
| 7.53 | IC50 | 29.3 | nM | CHEMBL4649755 |
| 7.52 | IC50 | 30 | nM | ACTINONIN |
| 7.52 | IC50 | 30.2 | nM | CHEMBL4641571 |
| 7.52 | IC50 | 30 | nM | CHEMBL5191348 |
| 7.52 | IC50 | 30 | nM | CHEMBL91461 |
| 7.52 | IC50 | 30 | nM | CHEMBL93648 |
PubChem BioAssay actives
77 with measured affinity, of 300 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| (2R)-N’-hydroxy-N-[(2S)-1-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]-2-pentylbutanediamide | 157064: Binding affinity towards Peptide deformylase | ki | 0.0003 | uM |
| (2R)-2-butyl-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-N’-hydroxybutanediamide | 156923: Compound was evaluated for inhibition of peptide deformylase, PDF.Ni of Escherichia coli | ic50 | 0.0010 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(5-methyl-1,3-thiazol-2-yl)-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0028 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(4-methyl-1,3-thiazol-2-yl)-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0030 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(4-methylphenyl)-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0036 | uM |
| (3R)-3-(cyclopentylmethyl)-N-hydroxy-4-oxo-4-[(6S)-6-(3-phenyl-1,2,4-oxadiazol-5-yl)-5-azaspiro[2.4]heptan-5-yl]butanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0038 | uM |
| (3R)-3-(cyclopentylmethyl)-4-[(6S)-6-[3-[4-fluoro-2-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]-N-hydroxy-4-oxobutanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0041 | uM |
| (3R)-4-[(6S)-6-[3-(4-butylphenyl)-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]-3-(cyclopentylmethyl)-N-hydroxy-4-oxobutanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0042 | uM |
| (6S)-N-(5-fluoro-2-pyridinyl)-5-[(2R)-2-[2-(hydroxyamino)-2-oxoethyl]hexanoyl]-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0049 | uM |
| (3R)-3-(cyclopentylmethyl)-4-[(6S)-6-[3-[2-fluoro-4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]-N-hydroxy-4-oxobutanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0049 | uM |
| (3R)-3-(cyclopentylmethyl)-4-[(6S)-6-[3-(4-cyclopropylphenyl)-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]-N-hydroxy-4-oxobutanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0050 | uM |
| (3R)-3-(cyclopentylmethyl)-4-[(6S)-6-[3-(5-fluoro-2-pyridinyl)-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]-N-hydroxy-4-oxobutanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0050 | uM |
| (3R)-4-[(6S)-6-[3-(4-bromophenyl)-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]-3-(cyclopentylmethyl)-N-hydroxy-4-oxobutanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0055 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-pyrazin-2-yl-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0059 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(5-fluoro-2-pyridinyl)-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0059 | uM |
| (2S)-2-[[(2R)-2-(cyclohexylmethyl)-3-[formyl(hydroxy)amino]propanoyl]amino]-N,N,3,3-tetramethylbutanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0060 | uM |
| (6S)-N-(4-bromophenyl)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0061 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-phenyl-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0064 | uM |
| (3R)-4-[(6S)-6-[3-[2-chloro-4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]-3-(cyclopentylmethyl)-N-hydroxy-4-oxobutanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0065 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-[4-fluoro-2-(trifluoromethyl)phenyl]-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0070 | uM |
| (2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]hexanamide | 156922: Antibacterial activity against Escherichia coli Peptide deformylase. Ni | ic50 | 0.0070 | uM |
| (3R)-3-(cyclopentylmethyl)-N-hydroxy-4-oxo-4-[(6S)-6-[3-(2,3,5-trifluorophenyl)-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]butanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0071 | uM |
| (3R)-3-(cyclopentylmethyl)-N-hydroxy-4-oxo-4-[(6S)-6-[3-[4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]butanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0072 | uM |
| (2S)-1-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(5-fluoro-2-pyridinyl)-4-methylidenepyrrolidine-2-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0072 | uM |
| (2S)-2-[[(2R)-2-(cyclopentylmethyl)-3-[formyl(hydroxy)amino]propanoyl]amino]-N,N,3,3-tetramethylbutanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0080 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(1,3-thiazol-2-yl)-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0087 | uM |
| (3R)-3-(cyclopentylmethyl)-4-[(6S)-6-[3-(4-ethylphenyl)-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]-N-hydroxy-4-oxobutanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0088 | uM |
| (2S)-1-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(5-methyl-1,3-thiazol-2-yl)pyrrolidine-2-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0089 | uM |
| (3R)-3-(cyclopentylmethyl)-N-hydroxy-4-[(6S)-6-[3-(4-methylphenyl)-1,2,4-oxadiazol-5-yl]-5-azaspiro[2.4]heptan-5-yl]-4-oxobutanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0093 | uM |
| (6S)-5-[(2R)-2-[2-(hydroxyamino)-2-oxoethyl]hexanoyl]-N-(5-methyl-1,3-thiazol-2-yl)-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0094 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-pyrimidin-4-yl-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0095 | uM |
| (2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]heptanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0100 | uM |
| (2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]-4-methylpentanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0100 | uM |
| (2S)-1-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(5-fluoro-2-pyridinyl)pyrrolidine-2-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0109 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-pyridazin-3-yl-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0131 | uM |
| (3R)-3-(cyclopentylmethyl)-N-hydroxy-4-oxo-4-[(6S)-6-(3-pyrazin-2-yl-1,2,4-oxadiazol-5-yl)-5-azaspiro[2.4]heptan-5-yl]butanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0161 | uM |
| (2S)-N-[(2S)-6-amino-1-(4-nitroanilino)-1-oxohexan-2-yl]-2-(sulfanylmethyl)hexanamide | 156928: Compound was evaluated for inhibition of peptide deformylase, PDF.Fe of Escherichia coli | ki | 0.0190 | uM |
| (2S)-2-[[(2R)-2-benzyl-3-[formyl(hydroxy)amino]propanoyl]amino]-N,N,3,3-tetramethylbutanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0200 | uM |
| (2S)-2-[[(2R)-2-cyclopentyl-3-[formyl(hydroxy)amino]propanoyl]amino]-N,N,3,3-tetramethylbutanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0200 | uM |
| (2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]-5-methylhexanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0200 | uM |
| (2S)-2-[[(2R)-2-(ethylsulfanylmethyl)-3-[formyl(hydroxy)amino]propanoyl]amino]-N,N,3,3-tetramethylbutanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0200 | uM |
| (2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]hex-5-enamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0200 | uM |
| (3R)-3-(cyclopentylmethyl)-N-hydroxy-4-[(6S)-6-(3-methyl-1,2,4-oxadiazol-5-yl)-5-azaspiro[2.4]heptan-5-yl]-4-oxobutanamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0293 | uM |
| (2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]hex-4-ynamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0300 | uM |
| (2S)-2-[[(2R)-2-[[formyl(hydroxy)amino]methyl]pent-4-enoyl]amino]-N,N,3,3-tetramethylbutanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0300 | uM |
| (2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]octanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0300 | uM |
| (2R)-N’-hydroxy-N-[(2S)-1-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]-2-pentylbutanediamide | 1869130: Inhibition of human PDF by spectrophotometric analysis | ic50 | 0.0300 | uM |
| (6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(1-methylpyrazol-4-yl)-5-azaspiro[2.4]heptane-6-carboxamide | 1658869: Inhibition of human PDF expressed in Escherichia coli BL21 pLysS using formyl-Met-Ala-His-Ala peptide as substrate measured after 1 hr by fluorescamine-based fluorescence assay | ic50 | 0.0302 | uM |
| (2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]nonanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0400 | uM |
| (2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]decanamide | 156924: Inhibition against Escherichia coli peptide deformylase | ic50 | 0.0500 | uM |
CTD chemical–gene interactions
16 total (human), top 16 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| aristolochic acid I | decreases expression | 1 |
| lead acetate | decreases expression | 1 |
| arsenite | increases methylation | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| abrine | decreases expression | 1 |
| Oxaliplatin | increases expression, decreases response to substance | 1 |
| Sunitinib | increases expression | 1 |
| Amiodarone | increases expression | 1 |
| Arsenic | affects methylation | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Fluorouracil | increases expression, decreases response to substance | 1 |
| Oxygen | decreases expression | 1 |
| Tobacco Smoke Pollution | increases expression | 1 |
| Urethane | decreases expression | 1 |
| Cadmium Chloride | decreases expression | 1 |
| Okadaic Acid | increases expression | 1 |
ChEMBL screening assays
22 unique, capped per target: 22 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1811207 | Binding | Inhibition of human peptide deformylase at 10 uM after 1 hr by fluorescence polarization based competition assay | Identification of benzofuran-4,5-diones as novel and selective non-hydroxamic acid, non-peptidomimetic based inhibitors of human peptide deformylase. — *Bioorg Med Chem Lett* |
Clinical trials (associated diseases)
Via MONDO — disease-level, not drug-specific.
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for PDF across ~30M SureChEMBL compounds — explore on Sugi Predict.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): COG8-congenital disorder of glycosylation