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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

FieldValue
HGNC IDHGNC:30012
Approved symbolPDF
Namepeptide deformylase, mitochondrial
Location16q22.1
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000258429
Ensembl biotypeprotein_coding
OMIM618720
Entrez64146

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

ExonStartEnd
ENSE000010317806932999769330588
ENSE000016010286932691369329179

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:

TissueQTLq-valueSlopeLead variant
Skin Sun Exposed Lower legsqtl7.1e-20-0.5516:69334093:C:A
Skin Sun Exposed Lower legeqtl2.8e-19-0.2916:69334093:C:A
Artery Tibialeqtl1.0e-17-0.3516:69328549:C:G
Cells Cultured fibroblastseqtl4.6e-17-0.2216:69338024:A:G
Skin Not Sun Exposed Suprapubiceqtl7.6e-17-0.2916:69322792:A:G
Skin Not Sun Exposed Suprapubicsqtl8.4e-17-0.4716:69207984:T:C
Artery Aortaeqtl2.7e-12-0.3816:69315882:T:C
Nerve Tibialeqtl3.5e-10-0.2516:69389213:A:G
Thyroideqtl3.8e-10-0.2616:69207984:T:C
Brain Cortexsqtl6.6e-10-0.6516:69338024:A:G
Adipose Subcutaneoussqtl6.9e-10-0.3416:69321060:A:G
Artery Tibialsqtl8.7e-10+0.4116:69341755:G:A
Adipose Subcutaneouseqtl1.1e-09-0.2116:69334093:C:A
Brain Frontal Cortex BA9sqtl9.0e-09-0.6216:69338024:A:G
Esophagus Musculariseqtl3.3e-08-0.2616:69341755:G:A
Lungsqtl3.9e-08-0.3616:69344542:A:G
Adipose Visceral Omentumsqtl8.8e-08-0.3216:69334093:C:A
Esophagus Mucosaeqtl1.7e-07-0.1916:69340558:G:C
Adipose Visceral Omentumeqtl6.2e-07-0.2116:69162112:T:C
Esophagus Muscularissqtl9.8e-07-0.3916:69341755:G:A

FANTOM5 promoters

3 alternative TSS:

Promoter IDTPM avgSamples expressed
1578975.83351681
1578960.8955476
1578950.5949333

Top tissues by expression

showing 100 of 134 tissues by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047381.19gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099180.63gold quality
adult mammalian kidneyUBERON:000008275.56gold quality
right lobe of liverUBERON:000111474.25gold quality
stromal cell of endometriumCL:000225574.00gold quality
gastrocnemiusUBERON:000138873.19gold quality
liverUBERON:000210773.12gold quality
mucosa of transverse colonUBERON:000499172.99gold quality
hindlimb stylopod muscleUBERON:000425272.69gold quality
muscle of legUBERON:000138372.40gold quality
kidneyUBERON:000211371.72gold quality
metanephros cortexUBERON:001053371.48gold quality
cortex of kidneyUBERON:000122571.33gold quality
skeletal muscle tissueUBERON:000113471.07gold quality
right adrenal glandUBERON:000123370.18gold quality
left adrenal glandUBERON:000123470.01gold quality
right adrenal gland cortexUBERON:003582769.81gold quality
monocyteCL:000057669.80gold quality
leukocyteCL:000073869.76gold quality
esophagus mucosaUBERON:000246969.23gold quality
left adrenal gland cortexUBERON:003582569.15gold quality
muscle tissueUBERON:000238568.97gold quality
superior frontal gyrusUBERON:000266168.70gold quality
body of pancreasUBERON:000115068.48gold quality
cortical plateUBERON:000534368.20gold quality
adrenal glandUBERON:000236967.84gold quality
primary visual cortexUBERON:000243667.48gold quality
olfactory segment of nasal mucosaUBERON:000538667.24gold quality
endometriumUBERON:000129566.88gold quality
granulocyteCL:000009466.63gold quality
heart left ventricleUBERON:000208466.34gold quality
lower esophagus mucosaUBERON:003583466.07gold quality
esophagusUBERON:000104365.82gold quality
duodenumUBERON:000211465.74gold quality
saliva-secreting glandUBERON:000104465.71gold quality
minor salivary glandUBERON:000183065.57gold quality
transverse colonUBERON:000115765.24gold quality
body of stomachUBERON:000116165.18gold quality
bone marrow cellCL:000209265.10silver quality
skin of legUBERON:000151164.93gold quality
left coronary arteryUBERON:000162664.75gold quality
zone of skinUBERON:000001464.68gold quality
skin of abdomenUBERON:000141664.57gold quality
tonsilUBERON:000237264.23gold quality
heartUBERON:000094864.08gold quality
Brodmann (1909) area 9UBERON:001354063.71gold quality
thoracic aortaUBERON:000151563.52gold quality
fundus of stomachUBERON:000116063.47gold quality
colonUBERON:000115563.42gold quality
ascending aortaUBERON:000149663.41gold quality
dorsolateral prefrontal cortexUBERON:000983463.38gold quality
ectocervixUBERON:001224963.38gold quality
left lobe of thyroid glandUBERON:000112063.35gold quality
placentaUBERON:000198763.29gold quality
stomachUBERON:000094563.27gold quality
myometriumUBERON:000129663.22gold quality
bone marrowUBERON:000237163.16gold quality
popliteal arteryUBERON:000225063.10gold quality
tibial arteryUBERON:000761063.09gold quality
apex of heartUBERON:000209863.00gold quality
right atrium auricular regionUBERON:000663162.90gold quality
thyroid glandUBERON:000204662.80gold quality
body of uterusUBERON:000985362.73gold quality
esophagogastric junction muscularis propriaUBERON:003584162.68gold quality
intestineUBERON:000016062.57gold quality
small intestineUBERON:000210862.56gold quality
thoracic mammary glandUBERON:000520062.53gold quality
lower esophagusUBERON:001347362.53gold quality
right lobe of thyroid glandUBERON:000111962.52gold quality
lower esophagus muscularis layerUBERON:003583362.51gold quality
pancreasUBERON:000126462.49gold quality
adipose tissueUBERON:000101362.48gold quality
ventricular zoneUBERON:000305362.46gold quality
left uterine tubeUBERON:000130362.45gold quality
right coronary arteryUBERON:000162562.45gold quality
omental fat padUBERON:001041462.44gold quality
subcutaneous adipose tissueUBERON:000219062.37gold quality
anterior cingulate cortexUBERON:000983562.27gold quality
small intestine Peyer’s patchUBERON:000345462.26gold quality
right frontal lobeUBERON:000281062.20gold quality
prostate glandUBERON:000236762.09gold quality
multicellular organismUBERON:000046861.99gold quality
vaginaUBERON:000099661.91gold quality
muscle layer of sigmoid colonUBERON:003580561.84gold quality
urinary bladderUBERON:000125561.82gold quality
upper lobe of left lungUBERON:000895261.48gold quality
spleenUBERON:000210661.46gold quality
descending thoracic aortaUBERON:000234561.45gold quality
lymph nodeUBERON:000002961.38gold quality
right ovaryUBERON:000211860.73gold quality
uterine cervixUBERON:000000260.71gold quality
endocervixUBERON:000045860.47gold quality
rectumUBERON:000105260.45gold quality
Ammon’s hornUBERON:000195460.43gold quality
bloodUBERON:000017859.98gold quality
putamenUBERON:000187459.50gold quality
adenohypophysisUBERON:000219659.38gold quality
left ovaryUBERON:000211959.33gold quality
ovaryUBERON:000099259.18gold quality
lungUBERON:000204859.07gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

ExperimentMarker?Max mean expression
E-ANND-3no1.97

HPA expression

RNA tissue specificity: Low tissue specificity

showing 60 of 79 HPA tissues / cells by nTPM:

Tissue / cellAxisnTPMProtein (IHC)
Frontal cortextissue20.7
Caudate putamentissue18.2
Cerebellumtissue16.8low
Basal gangliatissue15.2medium
Hippocampal formationtissue14.9
Cerebral cortextissue14.5medium
Putamentissue14.5
Somatosensory cortextissue14.5
Ventral forebraintissue14.0
Occipital cortextissue14.0
Temporal cortextissue13.9
Olfactory bulbtissue13.7
Retrosplenial and cingulate cortextissue13.6
Retrosplenial cortextissue13.5
Insular cortextissue13.4
Prefrontal cortextissue13.2
Entorhinal cortextissue13.1
Amygdalatissue13.0
Motor cortextissue12.7
Septumtissue12.7
Corpus callosumtissue11.8
Periaqueductal graytissue10.7
Hypothalamustissue10.5
Midbraintissue10.2
Spinal cordtissue10.0
Thalamustissue9.9
Superior colliculitissue9.9
Medulla oblongatatissue9.5
Ponstissue9.4
Substantia nigratissue9.4
Hippocampustissue9.4medium
Choroid plexustissue8.4
Postcentral gyrustissue6.9
Locus coeruleustissue6.5
Nucleus accumbenstissue6.1
Skeletal muscletissue4.2medium
Kidneytissue2.4high
Stomach 1tissue2.3medium
Salivary glandtissue2.2medium
Pancreastissue2.2medium
Livertissue2.1medium
Duodenumtissue1.9medium
Colontissue1.7medium
Adipose tissuetissue1.6not detected
Parathyroid glandtissue1.5medium
Vaginatissue1.4medium
Small intestinetissue1.4high
Thyroid glandtissue1.3medium
Pituitary glandtissue1.2
Prostatetissue1.2low
Bone marrowtissue1.2not detected
Skin 1tissue1.1high
Esophagustissue1.1medium
Spleentissue1.1low
Lymph nodetissue1.0medium
Adrenal glandtissue1.0high
Appendixtissue0.9medium
Breasttissue0.8medium
Heart muscletissue0.8high
Rectumtissue0.8medium

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:

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-426799.9666.532368
HSA-MIR-6842-5P99.8067.541587
HSA-MIR-7110-5P99.8067.841712
HSA-MIR-6752-5P99.5967.321243
HSA-MIR-6751-5P99.5664.991145
HSA-MIR-548AH-5P99.5269.732626
HSA-MIR-448099.4266.02735
HSA-MIR-427999.1966.702437
HSA-MIR-520G-3P98.9167.381914
HSA-MIR-520H98.9167.381914
HSA-MIR-887-5P98.8265.901347
HSA-MIR-219A-2-3P98.6268.78797
HSA-MIR-93498.4970.44581
HSA-MIR-4691-5P98.4166.771343
HSA-MIR-6792-3P98.4166.861359
HSA-MIR-6810-5P98.2966.21975
HSA-MIR-450A-2-3P97.9167.561459
HSA-MIR-30C-1-3P97.8066.361499
HSA-MIR-30C-2-3P97.8066.451499
HSA-MIR-6788-5P97.8066.411532
HSA-MIR-3127-5P97.5265.24786
HSA-MIR-509-3-5P97.2167.741517
HSA-MIR-509-5P97.2167.901512
HSA-MIR-441897.0467.161372
HSA-MIR-212-5P96.8367.43950
HSA-MIR-4652-5P96.4664.22553
HSA-MIR-125896.0867.74700
HSA-MIR-187-3P81.5659.38111

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

OrganismSymbolGene ID
danio_reriopdfENSDARG00000013950
mus_musculusPdfENSMUSG00000078931
rattus_norvegicusPdfENSRNOG00000022303
drosophila_melanogasterCG31278FBGN0051278
drosophila_melanogasterCG31373FBGN0051373

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.

OrganismUniProtIdentityMethod
Streptomyces coelicolor A3(2)Q9RD2785.0%Diamond
Bifidobacterium adolescentis ATCC 15703A1A2Z183.5%Diamond
Streptomyces avermitilis MA-4680 = NBRC 14893Q825U983.5%Diamond
Bifidobacterium longum NCC2705Q8G53483.5%Diamond
Oryza sativa Japonica GroupB6RGY075.4%Diamond
Solanum lycopersicumQ9FUZ075.4%Diamond
Arabidopsis thalianaQ9FV5374.2%Diamond
Gloeobacter violaceus PCC 7421Q7NJV347.4%Diamond
Rickettsia conorii str. Malish 7Q92JI743.0%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).

SymbolTypeEntrez
VPS4Aprotein-coding27183
NIP7protein-coding51388
SNTB2protein-coding6645
COG8protein-coding84342
UTP4protein-coding84916
DERPCprotein-coding113455421
HAS3protein-coding3038
CHTF8protein-coding54921
TMED6protein-coding146456
TERF2protein-coding7014
CYB5Bprotein-coding80777

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)

IDNameType
IPR023635Peptide_deformylaseFamily
IPR036821Peptide_deformylase_sfHomologous_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.

SubstrateKm (mM)Measurements
N-FORMYL-MET-ALA-SER0.25–4817
FORMYL-MET-ALA0.14–2815
FORMYL-MET-ALA-SER0.2–7015
FORMYL-MET-ALA-LYS-TYR0.34–7.67
N-FORMYL-MET-ALA2.9–4807
N-FORMYLMETHIONYL-LEU-P-NITROANILIDE0.018–0.0284
N-FORMYL-L-MET-L-VAL7.1–12.43
N-FORMYL-MET-SER-ASN-GLU2–5.53
N-FORMYL-NLE-ALA-SER0.6–113
FORMYL-MET-LEU-P-NITROANILIDE0.024–0.0472
FORMYL-MTHQ1.56–2.2872
N-FORMYL-ASP(NH2)0.74–12
N-FORMYL-BETA-THIAPHENYLALANYL-LYS-P-NITROANILID0.027–0.032
N-FORMYL-GLY(NH2)2.9–4.32
N-FORMYL-MET-LEU-GLU8–122

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:

PDBTitleMethodResolution (Å)
3G5KStructure and activity of human mitochondrial peptide deformylase, a novel cancer targetX-RAY DIFFRACTION1.7
3G5PStructure and activity of human mitochondrial peptide deformylase, a novel cancer targetX-RAY DIFFRACTION1.7

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9HBH1-F186.210.75

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)

PositionRole
215

Ligand- & substrate-binding residues (6)

PositionRole
71substrate
169substrate
171substrate
172Co(2+)
214Co(2+)
218Co(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:

CategoryTerms
protein modification process2
peptidyltransferase activity1
translational initiation1
translational elongation1
translational termination1
macromolecule biosynthetic process1
protein metabolic process1
protein biosynthetic process1
cell population proliferation1
regulation of cell population proliferation1
positive regulation of cellular process1
hydrolase activity, acting on carbon-nitrogen (but not peptide) bonds, in linear amides1
cation binding1
catalytic activity1
cytoplasm1
intracellular membrane-bounded organelle1

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 termNSEvidence
peptidyl-methionine modificationBPdirect assay
positive regulation of cell population proliferationBPmutant phenotype
post-translational protein modificationBPdirect assay
mitochondrionCCdirect assay
peptide deformylase activityMFdirect assay

Protein interactions and networks

STRING

showing 15 of 1,118 interactions by confidence (×1000):

Protein AProtein BPartner UniProtScore
PDFMTFMTQ96DP5773
PDFMETAP1DQ6UB28605
PDFMRRFQ96E11547
PDFMETAP1P53582546
PDFTSFMP43897460
PDFMARS2Q96GW9376
PDFMARS1P56192367
PDFMETAP2P50579350
PDFHIBCHQ6NVY1334
PDFHSPE1P61604332
PDFMTRFRQ9H3J6328
PDFPCCBP05166324
PDFDERAQ9Y315322
PDFDHODHQ02127314
PDFXPNPEP3Q9NQH7313

IntAct

Human interaction partners of PDF in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

3 partners by confidence:

PartnerInteraction typeMIscoreRecords
PRSS48physical association0.4001
MYO5Bphysical association0.0001
RAC1physical association0.0001

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):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance7
Likely benign0
Benign2

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 23 predictions of 176):

Position(s)EffectΔscoreSites
16:69329180–69329182acceptor_loss0.94007
16:69329817donor_gain0.9400
16:69329888donor_gain0.9000
16:69329798donor_gain0.8200
16:69329995–69329996donor_loss0.80006
16:69329997donor_loss0.79003
16:69329269donor_gain0.7800
16:69329672donor_gain0.7600
16:69329336donor_gain0.7400
16:69329998donor_loss0.7300

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:

ResidueLikely-pathogenic substitutionsMean am_pathogenicityMax am_pathogenicity
M22890.8810.965
H21480.9850.989
H21880.9780.993
D21780.9750.991
D22680.9520.991
S17480.9010.995
N15580.8990.992
F23380.8280.986
F15380.7980.988
E21570.9750.996
C17270.9640.988
E17070.9600.991
F17870.9590.990
F22470.9590.985
W20770.9530.988
M10370.9300.977
S11270.9100.991
Q21370.9050.992
W23870.8980.976
F6470.8900.955

HPA cancer prognostics

RNA cancer specificity: Low cancer specificity

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

2 prognostic cancer types:

CancerPrognosticp-value
Glioblastoma Multiforme (validation)unfavorable0.000235
Rectum Adenocarcinoma (validation)favorable0.000414

Disease associations

OMIM: gene MIM:618720 | disease phenotypes:

GWAS associations

2 associations:

StudyTraitp-value
GCST005951_23Body mass index5e-11
GCST007006_16Logical memory (delayed recall) in normal cognition7e-7

EFO canonical traits (from GWAS)

2 canonical traits:

EFO IDTrait name
EFO:0004340body mass index
EFO:0004874memory 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.

LigandMeasureValue
(R)-2-Butyl-N*1*-((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-N*4*-hydroxy-succinamideIC501 nM
CHEMBL4637933IC502.8 nM
CHEMBL4638057IC503 nM
CHEMBL4632607IC503.6 nM
CHEMBL4643984IC504.2 nM
CHEMBL4639327IC504.9 nM
CHEMBL4649534IC504.9 nM
CHEMBL4641416IC505 nM
CHEMBL4636545IC505 nM
CHEMBL4643967IC505.5 nM
CHEMBL4636221IC505.9 nM
CHEMBL4634572IC505.9 nM
(S)-2-[(R)-2-Cyclohexylmethyl-3-(formyl-hydroxy-amino)-propionylamino]-3,3,N,N-tetramethyl-butyramideIC506 nM
CHEMBL4637166IC506.1 nM
CHEMBL4640974IC506.4 nM
CHEMBL4645966IC506.5 nM
CHEMBL4635093IC507 nM
CHEMBL4637631IC507.1 nM
CHEMBL4642360IC507.2 nM
CHEMBL4635263IC507.2 nM
(S)-2-[(R)-2-Cyclopentylmethyl-3-(formyl-hydroxy-amino)-propionylamino]-3,3,N,N-tetramethyl-butyramideIC508 nM
CHEMBL4645936IC508.7 nM
CHEMBL4646467IC508.8 nM
CHEMBL4641901IC508.9 nM
CHEMBL4640884IC509.3 nM
CHEMBL4644600IC509.4 nM
CHEMBL4638180IC509.5 nM
(R)-2-[(Formyl-hydroxy-amino)-methyl]-4-methyl-pentanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amideIC5010 nM
(R)-2-[(Formyl-hydroxy-amino)-methyl]-heptanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amideIC5010 nM
CHEMBL4636076IC5011 nM
CHEMBL4645201IC5013 nM
CHEMBL4643686IC5016 nM
(S)-2-Mercaptomethyl-hexanoic acid [(S)-5-amino-1-(4-nitro-phenylcarbamoyl)-pentyl]-amideKI19 nM
(R)-2-[(Formyl-hydroxy-amino)-methyl]-hex-5-enoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amideIC5020 nM
(S)-2-[(R)-2-Ethylsulfanylmethyl-3-(formyl-hydroxy-amino)-propionylamino]-3,3,N,N-tetramethyl-butyramideIC5020 nM
(S)-2-[(R)-2-Benzyl-3-(formyl-hydroxy-amino)-propionylamino]-3,3,N,N-tetramethyl-butyramideIC5020 nM
(R)-2-[(Formyl-hydroxy-amino)-methyl]-5-methyl-hexanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amideIC5020 nM
(S)-2-[(R)-2-Cyclopentyl-3-(formyl-hydroxy-amino)-propionylamino]-3,3,N,N-tetramethyl-butyramideIC5020 nM
CHEMBL4649755IC5029 nM
(R)-2-[(Formyl-hydroxy-amino)-methyl]-pent-4-enoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amideIC5030 nM
(R)-2-[(Formyl-hydroxy-amino)-methyl]-octanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amideIC5030 nM
(R)-2-[(Formyl-hydroxy-amino)-methyl]-hex-4-ynoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amideIC5030 nM
CHEMBL4641571IC5030 nM
CHEMBL5191348IC5030 nM
(R)-2-[(Formyl-hydroxy-amino)-methyl]-nonanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amideIC5040 nM
(R)-2-[(Formyl-hydroxy-amino)-methyl]-decanoic acid [1-((S)-dimethyl-carbamoyl)-2,2-dimethyl-propyl]-amideIC5050 nM
(R)-2-[(Formyl-hydroxy-amino)-methyl]-pentanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amideIC5050 nM
(R)-N-((S)-1-Dimethylcarbamoyl-2,2-dimethyl-propyl)-2-[(formyl-hydroxy-amino)-methyl]-3-methyl-butyramideIC5050 nM
(S)-2-{(R)-2-[(Formyl-hydroxy-amino)-methyl]-butyrylamino}-3,3,N,N-tetramethyl-butyramideIC5070 nM
(S)-2-[(Formyl-hydroxy-amino)-methyl]-hexanoic acid ((S)-1-dimethylcarbamoyl-2,2-dimethyl-propyl)-amideIC5070 nM

ChEMBL bioactivities

77 potent at pChembl≥5 of 87 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.52Ki0.3nMACTINONIN
9.00IC501nMCHEMBL122067
8.82IC501.5nMACTINONIN
8.56IC502.78nMCHEMBL4637933
8.52IC502.99nMCHEMBL4638057
8.45IC503.58nMCHEMBL4632607
8.42IC503.77nMCHEMBL4641062
8.39IC504.11nMCHEMBL4635911
8.37IC504.24nMCHEMBL4643984
8.31IC504.92nMCHEMBL4639327
8.31IC504.85nMCHEMBL4649534
8.30IC505.01nMCHEMBL4641416
8.30IC505.01nMCHEMBL4636545
8.26IC505.48nMCHEMBL4643967
8.23IC505.87nMCHEMBL4636221
8.23IC505.87nMCHEMBL4634572
8.22IC506nMCHEMBL90193
8.21IC506.12nMCHEMBL4637166
8.19IC506.42nMCHEMBL4640974
8.19IC506.47nMCHEMBL4645966
8.15IC507.15nMCHEMBL4642360
8.15IC507.01nMCHEMBL4635093
8.15IC507.08nMCHEMBL4637631
8.15IC507nMCHEMBL431210
8.14IC507.19nMCHEMBL4635263
8.10IC508nMCHEMBL316099
8.06IC508.74nMCHEMBL4645936
8.05IC508.94nMCHEMBL4641901
8.05IC508.81nMCHEMBL4646467
8.03IC509.42nMCHEMBL4644600
8.03IC509.26nMCHEMBL4640884
8.02IC509.53nMCHEMBL4638180
8.00IC5010nMCHEMBL96864
8.00IC5010nMCHEMBL413726
8.00IC5010nMACTINONIN
7.96IC5010.9nMCHEMBL4636076
7.88IC5013.1nMCHEMBL4645201
7.79IC5016.1nMCHEMBL4643686
7.72Ki19nMCHEMBL325246
7.70IC5020nMCHEMBL540441
7.70IC5020nMCHEMBL328502
7.70IC5020nMCHEMBL91882
7.70IC5020nMCHEMBL91835
7.70IC5020nMCHEMBL328688
7.53IC5029.3nMCHEMBL4649755
7.52IC5030nMACTINONIN
7.52IC5030.2nMCHEMBL4641571
7.52IC5030nMCHEMBL5191348
7.52IC5030nMCHEMBL91461
7.52IC5030nMCHEMBL93648

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.

CompoundAssayTypeValueUnit
(2R)-N’-hydroxy-N-[(2S)-1-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]-2-pentylbutanediamide157064: Binding affinity towards Peptide deformylaseki0.0003uM
(2R)-2-butyl-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-N’-hydroxybutanediamide156923: Compound was evaluated for inhibition of peptide deformylase, PDF.Ni of Escherichia coliic500.0010uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(5-methyl-1,3-thiazol-2-yl)-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0028uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(4-methyl-1,3-thiazol-2-yl)-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0030uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(4-methylphenyl)-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0036uM
(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]butanamide1658869: 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 assayic500.0038uM
(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-oxobutanamide1658869: 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 assayic500.0041uM
(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-oxobutanamide1658869: 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 assayic500.0042uM
(6S)-N-(5-fluoro-2-pyridinyl)-5-[(2R)-2-[2-(hydroxyamino)-2-oxoethyl]hexanoyl]-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0049uM
(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-oxobutanamide1658869: 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 assayic500.0049uM
(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-oxobutanamide1658869: 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 assayic500.0050uM
(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-oxobutanamide1658869: 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 assayic500.0050uM
(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-oxobutanamide1658869: 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 assayic500.0055uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-pyrazin-2-yl-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0059uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(5-fluoro-2-pyridinyl)-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0059uM
(2S)-2-[[(2R)-2-(cyclohexylmethyl)-3-[formyl(hydroxy)amino]propanoyl]amino]-N,N,3,3-tetramethylbutanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0060uM
(6S)-N-(4-bromophenyl)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0061uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-phenyl-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0064uM
(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-oxobutanamide1658869: 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 assayic500.0065uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-[4-fluoro-2-(trifluoromethyl)phenyl]-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0070uM
(2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]hexanamide156922: Antibacterial activity against Escherichia coli Peptide deformylase. Niic500.0070uM
(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]butanamide1658869: 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 assayic500.0071uM
(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]butanamide1658869: 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 assayic500.0072uM
(2S)-1-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(5-fluoro-2-pyridinyl)-4-methylidenepyrrolidine-2-carboxamide1658869: 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 assayic500.0072uM
(2S)-2-[[(2R)-2-(cyclopentylmethyl)-3-[formyl(hydroxy)amino]propanoyl]amino]-N,N,3,3-tetramethylbutanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0080uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(1,3-thiazol-2-yl)-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0087uM
(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-oxobutanamide1658869: 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 assayic500.0088uM
(2S)-1-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(5-methyl-1,3-thiazol-2-yl)pyrrolidine-2-carboxamide1658869: 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 assayic500.0089uM
(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-oxobutanamide1658869: 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 assayic500.0093uM
(6S)-5-[(2R)-2-[2-(hydroxyamino)-2-oxoethyl]hexanoyl]-N-(5-methyl-1,3-thiazol-2-yl)-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0094uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-pyrimidin-4-yl-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0095uM
(2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]heptanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0100uM
(2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]-4-methylpentanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0100uM
(2S)-1-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(5-fluoro-2-pyridinyl)pyrrolidine-2-carboxamide1658869: 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 assayic500.0109uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-pyridazin-3-yl-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0131uM
(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]butanamide1658869: 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 assayic500.0161uM
(2S)-N-[(2S)-6-amino-1-(4-nitroanilino)-1-oxohexan-2-yl]-2-(sulfanylmethyl)hexanamide156928: Compound was evaluated for inhibition of peptide deformylase, PDF.Fe of Escherichia coliki0.0190uM
(2S)-2-[[(2R)-2-benzyl-3-[formyl(hydroxy)amino]propanoyl]amino]-N,N,3,3-tetramethylbutanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0200uM
(2S)-2-[[(2R)-2-cyclopentyl-3-[formyl(hydroxy)amino]propanoyl]amino]-N,N,3,3-tetramethylbutanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0200uM
(2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]-5-methylhexanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0200uM
(2S)-2-[[(2R)-2-(ethylsulfanylmethyl)-3-[formyl(hydroxy)amino]propanoyl]amino]-N,N,3,3-tetramethylbutanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0200uM
(2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]hex-5-enamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0200uM
(3R)-3-(cyclopentylmethyl)-N-hydroxy-4-[(6S)-6-(3-methyl-1,2,4-oxadiazol-5-yl)-5-azaspiro[2.4]heptan-5-yl]-4-oxobutanamide1658869: 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 assayic500.0293uM
(2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]hex-4-ynamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0300uM
(2S)-2-[[(2R)-2-[[formyl(hydroxy)amino]methyl]pent-4-enoyl]amino]-N,N,3,3-tetramethylbutanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0300uM
(2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]octanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0300uM
(2R)-N’-hydroxy-N-[(2S)-1-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]-2-pentylbutanediamide1869130: Inhibition of human PDF by spectrophotometric analysisic500.0300uM
(6S)-5-[(2R)-2-(cyclopentylmethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-(1-methylpyrazol-4-yl)-5-azaspiro[2.4]heptane-6-carboxamide1658869: 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 assayic500.0302uM
(2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]nonanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0400uM
(2R)-N-[(2S)-1-(dimethylamino)-3,3-dimethyl-1-oxobutan-2-yl]-2-[[formyl(hydroxy)amino]methyl]decanamide156924: Inhibition against Escherichia coli peptide deformylaseic500.0500uM

CTD chemical–gene interactions

16 total (human), top 16 by PubMed support.

ChemicalActions (top 5)PubMed papers
aristolochic acid Idecreases expression1
lead acetatedecreases expression1
arseniteincreases methylation1
di-n-butylphosphoric acidaffects expression1
abrinedecreases expression1
Oxaliplatinincreases expression, decreases response to substance1
Sunitinibincreases expression1
Amiodaroneincreases expression1
Arsenicaffects methylation1
Benzo(a)pyreneincreases methylation1
Fluorouracilincreases expression, decreases response to substance1
Oxygendecreases expression1
Tobacco Smoke Pollutionincreases expression1
Urethanedecreases expression1
Cadmium Chloridedecreases expression1
Okadaic Acidincreases expression1

ChEMBL screening assays

22 unique, capped per target: 22 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1811207BindingInhibition of human peptide deformylase at 10 uM after 1 hr by fluorescence polarization based competition assayIdentification 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.