DPP7
gene geneOn this page
Also known as DPPIIDPP2
Summary
DPP7 (dipeptidyl peptidase 7, HGNC:14892) is a protein-coding gene on chromosome 9q34.3, encoding Dipeptidyl peptidase 2 (Q9UHL4). Plays an important role in the degradation of some oligopeptides.
The protein encoded by this gene is a post-proline cleaving aminopeptidase expressed in quiescent lymphocytes. The resting lymphocytes are maintained through suppression of apoptosis, a state which is disrupted by inhibition of this novel serine protease. The enzyme has strong sequence homology with prolylcarboxypeptidase and is active at both acidic and neutral pH.
Source: NCBI Gene 29952 — RefSeq curated summary.
At a glance
- GWAS associations: 1
- Clinical variants (ClinVar): 176 total
- GTEx eGene: eQTL in 45 tissues, sQTL in 50 (q < 0.05)
- ChEMBL bioactivity: 3 clinical-phase molecules tested; no curated mechanism-of-action drug
- Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 1.71 (unconstrained)
- MANE Select transcript:
NM_013379 - Notable: 176 clinical variants but no curated precision-oncology (CIViC) evidence yet
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:14892 |
| Approved symbol | DPP7 |
| Name | dipeptidyl peptidase 7 |
| Location | 9q34.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | DPPII, DPP2 |
| Ensembl gene | ENSG00000176978 |
| Ensembl biotype | protein_coding |
| OMIM | 610537 |
| Entrez | 29952 |
Gene structure
Transcript identifiers
Ensembl transcripts: 65 — 28 nonsense_mediated_decay, 19 protein_coding, 13 retained_intron, 5 protein_coding_CDS_not_defined
MANE Select: ENST00000371579
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 1, TSL 2: 4, TSL 3: 4, TSL 5: 4
ENST00000371579, ENST00000460830, ENST00000463619, ENST00000470766, ENST00000472306, ENST00000473532, ENST00000473703, ENST00000478597, ENST00000482088, ENST00000483783, ENST00000485456, ENST00000491807, ENST00000497375, ENST00000706871, ENST00000706872, ENST00000706873, ENST00000706874, ENST00000706875, ENST00000706876, ENST00000706877, ENST00000706878, ENST00000706879, ENST00000706880, ENST00000706881, ENST00000706882, ENST00000718334, ENST00000718335, ENST00000894943, ENST00000894944, ENST00000894945, ENST00000894946, ENST00000894947, ENST00000894948, ENST00000894949, ENST00000894950, ENST00000960839, ENST00000960840, ENST00000960841, ENST00000974671, ENST00000974674, ENST00000974676, ENST00001043763, ENST00001043764, ENST00001043765, ENST00001043766, ENST00001043767, ENST00001043768, ENST00001043770, ENST00001043771, ENST00001043772, ENST00001043775, ENST00001043777, ENST00001043778, ENST00001043779, ENST00001043780, ENST00001043781, ENST00001043782, ENST00001043783, ENST00001043784, ENST00001043785, ENST00001043786, ENST00001074124, ENST00001119542, ENST00001128159, ENST00001133320
RefSeq mRNA: 4 — MANE Select: NM_013379
NM_001438108, NM_001438109, NM_001438110, NM_013379
CCDS: CCDS7030
Canonical transcript exons
ENST00000371579 — 13 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001455574 | 137114647 | 137114733 |
| ENSE00001923377 | 137114463 | 137114576 |
| ENSE00003495678 | 137114243 | 137114382 |
| ENSE00003538243 | 137113361 | 137113496 |
| ENSE00003567909 | 137113206 | 137113287 |
| ENSE00003570670 | 137112953 | 137113119 |
| ENSE00003576072 | 137112112 | 137112230 |
| ENSE00003609068 | 137113865 | 137114028 |
| ENSE00003670167 | 137112745 | 137112805 |
| ENSE00004034807 | 137111690 | 137111754 |
| ENSE00004034808 | 137111873 | 137112029 |
| ENSE00004034809 | 137110546 | 137110783 |
| ENSE00004034810 | 137110880 | 137110950 |
Expression profiles
Bgee: expression breadth ubiquitous, 243 present calls, max score 99.31.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 61.1705 / max 398.7661, expressed in 1755 samples.
Highest expression (Bgee): adenohypophysis, hemisphere of cerebellum, uterine tube, granulocyte, lobe of thyroid gland.
Genetic regulation across tissues (GTEx eQTL / sQTL)
DPP7 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 45 tissues and its splicing (sQTL) in 50 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
showing 20 of 95 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Thyroid | sqtl | 2.0e-122 | -1.05 | 9:137111973:C:G |
| Adipose Subcutaneous | sqtl | 4.4e-121 | -0.91 | 9:137111973:C:G |
| Skin Not Sun Exposed Suprapubic | sqtl | 3.4e-112 | -1.00 | 9:137111973:C:G |
| Cells Cultured fibroblasts | sqtl | 2.1e-103 | -1.20 | 9:137111973:C:G |
| Skin Sun Exposed Lower leg | sqtl | 9.4e-79 | -0.92 | 9:137111973:C:G |
| Muscle Skeletal | sqtl | 3.4e-77 | -0.73 | 9:137111973:C:G |
| Testis | sqtl | 9.8e-77 | -1.24 | 9:137111973:C:G |
| Artery Tibial | sqtl | 2.3e-72 | -0.80 | 9:137111973:C:G |
| Heart Atrial Appendage | sqtl | 1.3e-69 | -1.07 | 9:137111973:C:G |
| Nerve Tibial | sqtl | 6.8e-67 | -0.76 | 9:137111973:C:G |
| Whole Blood | sqtl | 1.9e-66 | -0.83 | 9:137111973:C:G |
| Adipose Visceral Omentum | sqtl | 2.0e-66 | -0.93 | 9:137111973:C:G |
| Esophagus Muscularis | sqtl | 1.5e-65 | -0.83 | 9:137111973:C:G |
| Cells EBV-transformed lymphocytes | sqtl | 2.7e-59 | -1.33 | 9:137111973:C:G |
| Artery Aorta | sqtl | 6.2e-59 | -0.92 | 9:137111973:C:G |
| Breast Mammary Tissue | sqtl | 8.6e-53 | -0.95 | 9:137111973:C:G |
| Adrenal Gland | sqtl | 1.0e-52 | -1.21 | 9:137111973:C:G |
| Colon Transverse | sqtl | 2.2e-47 | -0.85 | 9:137111973:C:G |
| Heart Left Ventricle | sqtl | 9.6e-46 | -0.94 | 9:137111973:C:G |
| Cells Cultured fibroblasts | eqtl | 5.0e-44 | -0.40 | 9:137114298:G:C |
FANTOM5 promoters
1 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 103305 | 61.1705 | 1755 |
Top tissues by expression
showing 100 of 251 tissues by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| adenohypophysis | UBERON:0002196 | 99.31 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 99.14 | gold quality |
| right uterine tube | UBERON:0001302 | 99.07 | gold quality |
| granulocyte | CL:0000094 | 99.00 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 98.95 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 98.93 | gold quality |
| left testis | UBERON:0004533 | 98.93 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 98.91 | gold quality |
| apex of heart | UBERON:0002098 | 98.91 | gold quality |
| right testis | UBERON:0004534 | 98.91 | gold quality |
| right frontal lobe | UBERON:0002810 | 98.88 | gold quality |
| cerebellar cortex | UBERON:0002129 | 98.84 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 98.72 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 98.69 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 98.64 | gold quality |
| pituitary gland | UBERON:0000007 | 98.62 | gold quality |
| left adrenal gland | UBERON:0001234 | 98.61 | gold quality |
| right atrium auricular region | UBERON:0006631 | 98.59 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 98.58 | gold quality |
| C1 segment of cervical spinal cord | UBERON:0006469 | 98.54 | gold quality |
| right adrenal gland | UBERON:0001233 | 98.50 | gold quality |
| minor salivary gland | UBERON:0001830 | 98.49 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 98.44 | gold quality |
| body of stomach | UBERON:0001161 | 98.32 | gold quality |
| metanephros cortex | UBERON:0010533 | 98.32 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 98.31 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 98.23 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 98.20 | gold quality |
| right coronary artery | UBERON:0001625 | 98.19 | gold quality |
| lower esophagus | UBERON:0013473 | 98.19 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 98.19 | gold quality |
| skin of abdomen | UBERON:0001416 | 98.17 | gold quality |
| spleen | UBERON:0002106 | 98.15 | gold quality |
| mucosa of stomach | UBERON:0001199 | 98.13 | gold quality |
| thyroid gland | UBERON:0002046 | 98.13 | gold quality |
| body of pancreas | UBERON:0001150 | 98.11 | gold quality |
| skin of leg | UBERON:0001511 | 98.09 | gold quality |
| cardiac atrium | UBERON:0002081 | 98.02 | gold quality |
| adrenal cortex | UBERON:0001235 | 98.00 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 98.00 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 97.96 | gold quality |
| ascending aorta | UBERON:0001496 | 97.94 | gold quality |
| left coronary artery | UBERON:0001626 | 97.92 | gold quality |
| thoracic aorta | UBERON:0001515 | 97.89 | gold quality |
| tibial nerve | UBERON:0001323 | 97.88 | gold quality |
| hypothalamus | UBERON:0001898 | 97.83 | gold quality |
| right lung | UBERON:0002167 | 97.83 | gold quality |
| nucleus accumbens | UBERON:0001882 | 97.76 | gold quality |
| omental fat pad | UBERON:0010414 | 97.76 | gold quality |
| left uterine tube | UBERON:0001303 | 97.75 | gold quality |
| peritoneum | UBERON:0002358 | 97.70 | gold quality |
| right ovary | UBERON:0002118 | 97.67 | gold quality |
| putamen | UBERON:0001874 | 97.63 | gold quality |
| saliva-secreting gland | UBERON:0001044 | 97.55 | gold quality |
| caudate nucleus | UBERON:0001873 | 97.54 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 97.52 | gold quality |
| cerebellum | UBERON:0002037 | 97.51 | gold quality |
| right lobe of liver | UBERON:0001114 | 97.49 | gold quality |
| coronary artery | UBERON:0001621 | 97.46 | gold quality |
| endocervix | UBERON:0000458 | 97.43 | gold quality |
| left ovary | UBERON:0002119 | 97.33 | gold quality |
| vermiform appendix | UBERON:0001154 | 97.29 | gold quality |
| stromal cell of endometrium | CL:0002255 | 97.25 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 97.16 | gold quality |
| amygdala | UBERON:0001876 | 97.13 | gold quality |
| prefrontal cortex | UBERON:0000451 | 97.05 | gold quality |
| adrenal gland | UBERON:0002369 | 97.05 | gold quality |
| heart left ventricle | UBERON:0002084 | 97.03 | gold quality |
| spinal cord | UBERON:0002240 | 97.00 | gold quality |
| esophagus | UBERON:0001043 | 96.96 | gold quality |
| body of uterus | UBERON:0009853 | 96.91 | gold quality |
| transverse colon | UBERON:0001157 | 96.86 | gold quality |
| upper lobe of lung | UBERON:0008948 | 96.84 | gold quality |
| testis | UBERON:0000473 | 96.82 | gold quality |
| mouth mucosa | UBERON:0003729 | 96.73 | gold quality |
| lymph node | UBERON:0000029 | 96.70 | gold quality |
| cardiac ventricle | UBERON:0002082 | 96.56 | gold quality |
| esophagus mucosa | UBERON:0002469 | 96.31 | gold quality |
| ectocervix | UBERON:0012249 | 96.28 | gold quality |
| leukocyte | CL:0000738 | 96.10 | gold quality |
| monocyte | CL:0000576 | 96.09 | gold quality |
| heart | UBERON:0000948 | 96.06 | gold quality |
| aorta | UBERON:0000947 | 95.99 | gold quality |
| small intestine | UBERON:0002108 | 95.98 | gold quality |
| zone of skin | UBERON:0000014 | 95.93 | gold quality |
| gall bladder | UBERON:0002110 | 95.81 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 95.79 | gold quality |
| stomach | UBERON:0000945 | 95.76 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 95.75 | gold quality |
| gastrocnemius | UBERON:0001388 | 95.71 | gold quality |
| cortex of kidney | UBERON:0001225 | 95.44 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 95.34 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 95.31 | gold quality |
| neocortex | UBERON:0001950 | 95.22 | gold quality |
| muscle of leg | UBERON:0001383 | 95.14 | gold quality |
| bone marrow cell | CL:0002092 | 95.09 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 95.04 | gold quality |
| fundus of stomach | UBERON:0001160 | 94.87 | gold quality |
| frontal cortex | UBERON:0001870 | 94.84 | gold quality |
| prostate gland | UBERON:0002367 | 94.83 | gold quality |
Single-cell (SCXA)
Detected in 4 experiment(s), a significant marker in 3.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-HCAD-13 | yes | 11.77 |
| E-GEOD-93593 | yes | 4.01 |
| E-MTAB-9221 | no | 685.06 |
| E-ANND-3 | no | 0.00 |
HPA expression
RNA tissue specificity: Low tissue specificity
showing 60 of 80 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM | Protein (IHC) |
|---|---|---|---|
| Choroid plexus | tissue | 132.4 | |
| Pituitary gland | tissue | 101.2 | |
| Salivary gland | tissue | 73.1 | medium |
| Pancreas | tissue | 54.9 | medium |
| Locus coeruleus | tissue | 49.3 | |
| Parathyroid gland | tissue | 46.9 | medium |
| Nucleus accumbens | tissue | 44.7 | |
| Vagina | tissue | 43.0 | low |
| Heart muscle | tissue | 39.8 | low |
| Hippocampus | tissue | 39.3 | low |
| Seminal vesicle | tissue | 38.4 | medium |
| Postcentral gyrus | tissue | 37.3 | |
| Adrenal gland | tissue | 34.0 | high |
| Bone marrow | tissue | 31.3 | high |
| Adipose tissue | tissue | 30.0 | medium |
| Thyroid gland | tissue | 27.4 | medium |
| Spinal cord | tissue | 25.6 | |
| Spleen | tissue | 24.7 | medium |
| Fallopian tube | tissue | 24.5 | medium |
| Prostate | tissue | 24.4 | medium |
| Skeletal muscle | tissue | 24.2 | not detected |
| Superior colliculi | tissue | 24.1 | |
| Stomach 1 | tissue | 23.9 | medium |
| Medulla oblongata | tissue | 23.0 | |
| Lung | tissue | 22.9 | high |
| Thalamus | tissue | 22.7 | |
| Substantia nigra | tissue | 22.7 | |
| Pons | tissue | 22.6 | |
| Midbrain | tissue | 22.2 | |
| Duodenum | tissue | 22.2 | low |
| Liver | tissue | 21.6 | medium |
| Corpus callosum | tissue | 21.2 | |
| Cervix | tissue | 20.1 | not detected |
| Lymph node | tissue | 20.1 | medium |
| Ovary | tissue | 20.1 | low |
| Gallbladder | tissue | 19.5 | medium |
| Testis | tissue | 19.3 | high |
| Tongue | tissue | 18.8 | |
| Hypothalamus | tissue | 18.7 | |
| Urinary bladder | tissue | 18.5 | medium |
| Cerebral cortex | tissue | 18.1 | medium |
| Somatosensory cortex | tissue | 18.1 | |
| Hippocampal formation | tissue | 18.0 | |
| Skin 1 | tissue | 17.7 | high |
| Motor cortex | tissue | 17.4 | |
| Putamen | tissue | 17.2 | |
| Periaqueductal gray | tissue | 16.8 | |
| Prefrontal cortex | tissue | 16.7 | |
| Ventral forebrain | tissue | 16.6 | |
| Breast | tissue | 16.5 | high |
| Entorhinal cortex | tissue | 16.3 | |
| Septum | tissue | 16.3 | |
| Retrosplenial and cingulate cortex | tissue | 16.1 | |
| Placenta | tissue | 16.0 | high |
| Retrosplenial cortex | tissue | 16.0 | |
| Basal ganglia | tissue | 15.9 | medium |
| Kidney | tissue | 15.9 | high |
| Temporal cortex | tissue | 15.8 | |
| Occipital cortex | tissue | 15.8 | |
| Insular cortex | tissue | 15.2 |
Brain sub-regions (HPA Brain Atlas): detected in 191; highest nTPM — Blood vessel (71.1), Arcuate nucleus (65.6), Nucleus ambiguus (59.9), Habenula (58.8), Lateral funiculus (white matter) (58.2).
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): KLF2
Functional genomics
gnomAD constraint: pLI 5.69e-33, LOEUF 1.71, missense Z -2.25 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD)
ENST00000371579 splits into 3 regions with different missense tolerance; 0 are missense-constrained. Missense variants in a constrained region (low observed/expected) are more likely to be pathogenic. gnomAD
| Region (GRCh38) | Missense obs / exp | o/e | Constrained |
|---|---|---|---|
| 9:137,110,651–137,114,006 | 624 / 531.2 | 1.17 | no |
| 9:137,114,007–137,114,296 | 15 / 37.0 | 0.41 | no |
| 9:137,114,297–137,114,713 | 168 / 124.1 | 1.35 | no |
Literature-anchored findings (GeneRIF, showing 5)
- catalytic properties and inhibition of this proline-specific enzyme (PMID:12529175)
- DPP II plays a minor role in the progression of malignant melanocytic lesions (PMID:18823758)
- DPP2 is essential for maintaining lymphocytes and fibroblasts in G(0), and its inhibition results in apoptosis mediated by induction of c-Myc and p53. (PMID:19556882)
- The constitutive expression of dipeptidyl peptidase II mRNA in chronic lymphocytic leukemia was demonstrated. (PMID:20534982)
- human DPP7 structures reveal the molecular basis of specific inhibition and the architectural diversity of proline-specific peptidases (PMID:22952628)
Cross-species orthologs
8 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | dpp7 | ENSDARG00000027750 |
| mus_musculus | Dpp7 | ENSMUSG00000026958 |
| rattus_norvegicus | Dpp7 | ENSRNOG00000012640 |
| drosophila_melanogaster | CG3734 | FBGN0038700 |
| drosophila_melanogaster | CG18493 | FBGN0038701 |
| drosophila_melanogaster | CG3739 | FBGN0038702 |
| drosophila_melanogaster | CG11626 | FBGN0038705 |
| caenorhabditis_elegans | WBGENE00019682 |
Paralogs (2): PRSS16 (ENSG00000112812), PRCP (ENSG00000137509)
Mouse-model phenotypes
Observed phenotypes of the mouse ortholog (MGI:1933213) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 11 distinct phenotype terms.
| Mouse phenotype (MP) | Records |
|---|---|
| abnormal eating behavior | 1 |
| hyperglycemia | 1 |
| increased circulating insulin level | 1 |
| hepatic steatosis | 1 |
| increased liver weight | 1 |
| impaired glucose tolerance | 1 |
| insulin resistance | 1 |
| increased percent body fat/body weight | 1 |
| increased circulating glucose level | 1 |
| increased abdominal fat pad weight | 1 |
| increased epididymal fat pad weight | 1 |
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 |
|---|---|---|---|
| Pongo abelii | Q5RBU7 | 99.2% | Diamond |
| Bos taurus | Q2TA14 | 78.3% | 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 |
|---|---|---|
| MIR3621 | ncRNA | 100500811 |
| TMEM210 | protein-coding | 100505993 |
| GRIN1 | protein-coding | 2902 |
| LRRC26 | protein-coding | 389816 |
| MAN1B1-DT | ncRNA | 100289341 |
| UAP1L1 | protein-coding | 91373 |
| MAN1B1 | protein-coding | 11253 |
Protein
Protein identifiers
Dipeptidyl peptidase 2 — Q9UHL4 (reviewed: Q9UHL4)
Alternative names: Dipeptidyl aminopeptidase II, Dipeptidyl peptidase 7, Dipeptidyl peptidase II, Quiescent cell proline dipeptidase
All UniProt accessions (8): A0A9L9PXE7, A0A9L9PXM1, A0A9L9PY12, A0ABB0MVF0, A0ABB0MVF1, Q9UHL4, R4GMV4, R4GN05
UniProt curated annotations — full annotation on UniProt →
Function. Plays an important role in the degradation of some oligopeptides.
Subunit / interactions. Homodimer.
Subcellular location. Lysosome. Cytoplasmic vesicle. Secreted.
Tissue specificity. Detected in seminal plasma (at protein level).
Post-translational modifications. N-glycosylated.
Similarity. Belongs to the peptidase S28 family.
RefSeq proteins (4): NP_001425037, NP_001425038, NP_001425039, NP_037511* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR008758 | Peptidase_S28 | Family |
| IPR029058 | AB_hydrolase_fold | Homologous_superfamily |
| IPR042269 | Ser_carbopepase_S28_SKS | Homologous_superfamily |
Pfam: PF05577
Enzyme classification (BRENDA)
- EC 3.4.14.2 — dipeptidyl-peptidase II (BRENDA: 10 organisms, 103 substrates, 205 inhibitors, 54 Km, 32 kcat entries)
Substrate kinetics (BRENDA)
37 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| GLY-PRO-4-NITROANILIDE | 0.018–0.59 | 5 |
| LYS-ALA-2-NAPHTHYLAMIDE | 0.087–0.555 | 4 |
| ALA-PRO-P-NITROANILIDE | 0.009–0.041 | 3 |
| GLY-PRO-P-NITROANILIDE | 0.07–0.227 | 3 |
| ALA-ALA-4-NITROANILIDE | 0.487–1.22 | 2 |
| ARG-PRO-4-NITROANILIDE | 0.068–0.086 | 2 |
| GLY-L-PRO-4-NITROANILIDE | 0.36–1.1 | 2 |
| L-LYS-L-ALA-7-AMIDO-4-METHYLCOUMARIN | 0.36–0.93 | 2 |
| LYS-ALA-P-NITROANILIDE | 0.04–0.57 | 2 |
| LYS-PRO-P-NITROANILIDE | 0.019 | 2 |
| ALA-ALA-ALA | 1.67 | 1 |
| ALA-PRO-4-NITROANILIDE | 0.0457 | 1 |
| ALA-PRO-AMINO-4-TRIFLUOROMETHYLCOUMARIN | 0.032 | 1 |
| ARG-PRO-2-NAPHTHYLAMIDE | 0.0086 | 1 |
| ARG-PRO-P-NITROANILIDE | 0.04 | 1 |
UniProt features (50 total): helix 19, strand 13, glycosylation site 6, turn 4, active site 3, signal peptide 1, propeptide 1, sequence variant 1, sequence conflict 1, chain 1
Structure
Experimental structures (PDB)
3 structures by resolution:
| PDB | Title | Method | Resolution (Å) |
|---|---|---|---|
| 4EBB | Structure of DPP2 | X-RAY DIFFRACTION | 2 |
| 3JYH | Human dipeptidyl peptidase DPP7 | X-RAY DIFFRACTION | 2.19 |
| 3N0T | Human dipeptidil peptidase DPP7 complexed with inhibitor GSK237826A | X-RAY DIFFRACTION | 2.45 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9UHL4-F1 | 94.44 | 0.92 |
Human Protein Atlas
Protein class: Enzymes, ENZYME proteins, Hydrolases, Peptidases, Serine-type peptidases, Predicted secreted proteins, Plasma proteins
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): vesicles; golgi apparatus
Antibody reliability (HPA): IH enhanced · IF supported
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 (3)
| Position | Role |
|---|---|
| 162 | charge relay system |
| 418 | charge relay system |
| 443 | charge relay system |
Glycosylation sites (6)
| Type | Positions |
|---|---|
| N-linked (glcnac…) asparagine | 363, 428, 50, 86, 315, 356 |
Function
Pathways and Gene Ontology
Reactome pathways
1 curated (TAS) of 3; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
3 pathways:
| ID | Pathway | Evidence |
|---|---|---|
| R-HSA-6798695 | Neutrophil degranulation | curated |
| R-HSA-168256 | Immune System | — |
| R-HSA-168249 | Innate Immune System | — |
MSigDB gene sets: 145 (showing top):
REACTOME_INNATE_IMMUNE_SYSTEM, GOCC_SECRETORY_GRANULE, MODULE_151, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM1, GROSS_HYPOXIA_VIA_ELK3_UP, BYSTRYKH_HEMATOPOIESIS_STEM_CELL_AND_BRAIN_QTL_CIS, KINSEY_TARGETS_OF_EWSR1_FLII_FUSION_DN, GOBP_PROTEIN_CATABOLIC_PROCESS, BURTON_ADIPOGENESIS_9, MODULE_114, GOCC_SECRETORY_VESICLE, GOCC_VESICLE_LUMEN
GO Biological Process (2): proteolysis (GO:0006508), protein catabolic process (GO:0030163)
GO Molecular Function (6): aminopeptidase activity (GO:0004177), serine-type peptidase activity (GO:0008236), dipeptidyl-peptidase activity (GO:0008239), serine-type exopeptidase activity (GO:0070008), peptidase activity (GO:0008233), hydrolase activity (GO:0016787)
GO Cellular Component (6): extracellular region (GO:0005576), vesicle (GO:0031982), azurophil granule lumen (GO:0035578), extracellular exosome (GO:0070062), lysosome (GO:0005764), cytoplasmic vesicle (GO:0031410)
Reactome top-level categories
2 top-level categories:
| Category | Pathways |
|---|---|
| Innate Immune System | 1 |
| Immune System | 1 |
GO top-level categories
18 GO namespaces:
| Category | Terms |
|---|---|
| exopeptidase activity | 3 |
| protein metabolic process | 2 |
| macromolecule catabolic process | 1 |
| peptidase activity | 1 |
| serine hydrolase activity | 1 |
| serine-type peptidase activity | 1 |
| hydrolase activity | 1 |
| catalytic activity, acting on a protein | 1 |
| catalytic activity | 1 |
| cellular anatomical structure | 1 |
| membrane-bounded organelle | 1 |
| vacuolar lumen | 1 |
| secretory granule lumen | 1 |
| azurophil granule | 1 |
| extracellular vesicle | 1 |
| lytic vacuole | 1 |
| cytoplasm | 1 |
| intracellular vesicle | 1 |
Experimentally-supported GO annotations
GO terms backed by direct experimental evidence (ECO experimental codes) — 2 of 14 annotations. The rest are phylogenetic / computational / electronic (IEA).
2 experimentally-supported GO terms:
| GO term | NS | Evidence |
|---|---|---|
| extracellular exosome | CC | high-throughput assay |
| vesicle | CC | direct assay |
Protein interactions and networks
STRING
showing 15 of 900 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| DPP7 | DPP4 | P27487 | 866 |
| DPP7 | TIMM8B | Q9Y5J9 | 843 |
| DPP7 | DPP8 | Q6V1X1 | 808 |
| DPP7 | DPP9 | Q86TI2 | 790 |
| DPP7 | TIMM8A | O60220 | 755 |
| DPP7 | DPP3 | Q9NY33 | 677 |
| DPP7 | SDHD | O14521 | 663 |
| DPP7 | SDHC | Q99643 | 660 |
| DPP7 | PREP | P48147 | 655 |
| DPP7 | CTSC | P53634 | 624 |
| DPP7 | FAP | Q12884 | 610 |
| DPP7 | SDHB | P21912 | 609 |
| DPP7 | PEPD | P12955 | 593 |
| DPP7 | GOLGA3 | Q08378 | 569 |
| DPP7 | DPP10 | Q8N608 | 554 |
IntAct
Human interaction partners of DPP7 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
4 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| CFTR | physical association | 0.370 | 1 |
| TFAP2A | physical association | 0.370 | 1 |
| TFAP2C | physical association | 0.370 | 1 |
| XRN1 | physical association | 0.000 | 1 |
BioGRID (41 interactions; top human partners by supporting records): ABI1 (Affinity Capture-MS), AIMP1 (Co-fractionation), CEP78 (Affinity Capture-MS), CFTR (PCA), CSK (Affinity Capture-MS), CSTB (Co-fractionation), DOK2 (Affinity Capture-MS), FBXO6 (Affinity Capture-MS), HCK (Affinity Capture-MS), KIAA1429 (Affinity Capture-MS), MAP2K1 (Affinity Capture-MS), MYCBP (Co-fractionation), MYL12B (Affinity Capture-MS), NUDT21 (Affinity Capture-RNA), OBSL1 (Affinity Capture-MS)
Disease & clinical
Genetic variants
Variant evidence for DPP7: 176 ClinVar records (0 pathogenic / likely pathogenic); 1 GWAS association.
ClinVar
176 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 137 |
| Likely benign | 8 |
| Benign | 0 |
SpliceAI
Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 22 predictions of 977):
| Position(s) | Effect | Δscore | Sites |
|---|---|---|---|
| 9:137110870 | donor_gain | 1.0000 | |
| 9:137110878–137110879 | donor_loss | 1.0000 | 4 |
| 9:137110959 | acceptor_gain | 1.0000 | |
| 9:137111921 | donor_gain | 1.0000 | |
| 9:137112951–137112952 | donor_loss | 1.0000 | 5 |
| 9:137113120–137113121 | acceptor_loss | 1.0000 | 3 |
| 9:137113124 | acceptor_gain | 1.0000 | |
| 9:137113208 | donor_gain | 1.0000 | |
| 9:137113498 | acceptor_loss | 1.0000 | 2 |
| 9:137113863–137113864 | donor_loss | 1.0000 | 3 |
AlphaMissense
1,208 missense substitutions predicted likely pathogenic (of 3,187 scored), across 293 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 |
|---|---|---|---|
| D418 | 8 | 0.990 | 0.993 |
| D137 | 8 | 0.977 | 0.987 |
| H443 | 8 | 0.976 | 0.996 |
| D446 | 8 | 0.968 | 0.978 |
| H107 | 8 | 0.966 | 0.989 |
| D334 | 8 | 0.964 | 0.982 |
| F368 | 8 | 0.963 | 0.997 |
| D366 | 8 | 0.961 | 0.987 |
| D454 | 8 | 0.961 | 0.983 |
| S162 | 8 | 0.960 | 0.991 |
| D348 | 8 | 0.953 | 0.987 |
| H444 | 8 | 0.947 | 0.981 |
| D41 | 8 | 0.941 | 0.969 |
| S186 | 8 | 0.933 | 0.993 |
| F104 | 8 | 0.924 | 0.987 |
| F412 | 8 | 0.907 | 0.977 |
| F43 | 8 | 0.891 | 0.974 |
| F84 | 8 | 0.890 | 0.977 |
| H42 | 8 | 0.874 | 0.956 |
| F266 | 8 | 0.866 | 0.964 |
HPA cancer prognostics
RNA cancer specificity: Low cancer specificity
Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.
4 prognostic cancer types:
| Cancer | Prognostic | p-value |
|---|---|---|
| Kidney Renal Clear Cell Carcinoma (TCGA) | favorable | 0.000116 |
| Colon Adenocarcinoma (TCGA) | unfavorable | 0.000188 |
| Colon Adenocarcinoma (validation) | unfavorable | 0.000506 |
| Pancreatic Adenocarcinoma (TCGA) | favorable | 0.000778 |
Disease associations
OMIM: gene MIM:610537 | disease phenotypes:
GWAS associations
1 associations:
| Study | Trait | p-value |
|---|---|---|
| GCST005024_111 | Pursuit maintenance gain | 2e-6 |
EFO canonical traits (from GWAS)
1 canonical traits:
| EFO ID | Trait name |
|---|---|
| EFO:0008433 | pursuit maintenance gain measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL2111469 (SELECTIVITY GROUP), CHEMBL3976 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 38,302 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
3 molecules by phase:
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL515387 | GOSOGLIPTIN | 4 | 823 |
| CHEMBL1422 | SITAGLIPTIN | 4 | 26,952 |
| CHEMBL67279 | TALABOSTAT | 3 | 10,527 |
PharmGKB: 1 entry (CPIC guideline: no)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — S28: Lysosomal Pro-Xaa carboxypeptidase
Most potent curated ligand interactions (1 total), top 1:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| UAMC00039 | Inhibition | 10.1 | pKi |
Binding affinities (BindingDB)
1097 measured of 1692 human assays (1707 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| [(2R)-1-[(2S)-2-aminopropanethioyl]pyrrolidin-2-yl]boronic acid | IC50 | 0.2 nM | US-11559537: Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists |
| Boronic acid derivative | IC50 | 0.2 nM | US-11559537: Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists |
| N4-(4-chlorobenzyl)-2,4-diaminobutanoylpiperidine | IC50 | 0.22 nM | |
| (S)-2-Amino-4-[(4-chloro-benzyl)-methyl-amino]-1-piperidin-1-yl-butan-1-one | IC50 | 0.22 nM | |
| 2-(S)-Amino-4-(2-chloro-benzylamino)-1-piperidin-1-yl-butan-1-one | IC50 | 0.23 nM | |
| 2-(S)-Amino-4-(2-benzyloxy-benzylamino)-1-piperidin-1-yl-butan-1-one | IC50 | 0.39 nM | |
| (S)-2-Amino-4-(4-chloro-benzylamino)-1-(4-fluoro-piperidin-1-yl)-butan-1-one | IC50 | 0.39 nM | |
| 2-(S)-Amino-4-(4-benzyloxy-benzylamino)-1-piperidin-1-yl-butan-1-one | IC50 | 0.41 nM | |
| (S)-2,4-Diamino-N-((R)-1-boron-dihydroxide-pentyl)-butyramide | IC50 | 0.48 nM | |
| (R)-1-((S)-2,4-diaminobutanamido)pentylboronic acid | IC50 | 0.48 nM | |
| (S)-2-Amino-4-(4-chloro-benzylamino)-1-(4-methyl-piperidin-1-yl)-butan-1-one | IC50 | 0.55 nM | |
| (S)-2-Amino-4-dibenzylamino-1-piperidin-1-yl-butan-1-one | IC50 | 0.6 nM | |
| (S)-2-Amino-4-(4-chloro-benzylamino)-1-(3-fluoro-piperidin-1-yl)-butan-1-one | IC50 | 0.62 nM | |
| (2S,4S)-4-(4-chlorobenzylamino)-2-amino-1-(piperidin-1-yl)pentan-1-one | IC50 | 0.62 nM | |
| 2-(S)-Amino-4-(4-methoxy-benzylamino)-1-piperidin-1-yl-butan-1-one | IC50 | 0.66 nM | |
| (S)-2,4-Diamino-1-(2-boron-dihydroxide-pyrrolidin-1-yl)-butan-1-one | IC50 | 0.72 nM | |
| 2-(S)-Amino-1-piperidin-1-yl-4-[(pyridin-4-ylmethyl)-amino]-butan-1-one | IC50 | 0.75 nM | |
| Boronic acid derivative | IC50 | 0.8 nM | US-11559537: Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists |
| 2-(S)-Amino-1-piperidin-1-yl-4-[(thiophen-2-ylmethyl)-amino]-butan-1-one | IC50 | 0.8 nM | |
| (S)-2,4-diamino-1-((3aR,6aR)-hexahydrocyclopenta[b]pyrrol-1(2H)-yl)butan-1-one | IC50 | 0.88 nM | |
| 2-(S)-Amino-4-phenethylamino-1-piperidin-1-yl-butan-1-one | IC50 | 0.9 nM | |
| (R)-1-((S)-2-aminopropanoyl)pyrrolidin-2-ylboronic acid | IC50 | 1 nM | US-11559537: Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists |
| Boronic acid derivative | IC50 | 1 nM | US-11559537: Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists |
| N-alkyl Gly-boro-Pro derivative | IC50 | 1 nM | |
| 2-(S)-Amino-4-(cyclohexylmethyl-amino)-1-piperidin-1-yl-butan-1-one | IC50 | 1.1 nM | |
| (S)-2-Amino-4-(4-chloro-benzylamino)-1-(3,6-dihydro-2H-pyridin-1-yl)-butan-1-one | IC50 | 1.1 nM | |
| 2-(S)-Amino-4-[(naphthalen-2-ylmethyl)-amino]-1-piperidin-1-yl-butan-1-one | IC50 | 1.1 nM | |
| (S)-2-Amino-4-(4-chloro-benzylamino)-1-(3-methyl-piperidin-1-yl)-butan-1-one | IC50 | 1.13 nM | |
| 2-(S)-Amino-4-[(naphthalen-1-ylmethyl)-amino]-1-piperidin-1-yl-butan-1-one | IC50 | 1.31 nM | |
| 2-(S)-Amino-4-(3-chloro-benzylamino)-1-piperidin-1-yl-butan-1-one | IC50 | 1.34 nM | |
| (S)-2-Amino-4-phenylamino-1-piperidin-1-yl-butan-1-one | IC50 | 1.5 nM | |
| N-((S)-3-Amino-4-oxo-4-piperidin-1-yl-butyl)-acetamide | IC50 | 1.5 nM | |
| 2-(S)-Amino-4-(3-methoxy-benzylamino)-1-piperidin-1-yl-butan-1-one | IC50 | 1.77 nM | |
| N-((S)-3-Amino-4-oxo-4-piperidin-1-yl-butyl)-guanidine | IC50 | 1.8 nM | |
| N-alkyl Gly-boro-Pro derivative | IC50 | 1.8 nM | |
| 2-(S)-Amino-4-(3-phenyl-propylamino)-1-piperidin-1-yl-butan-1-one | IC50 | 1.91 nM | |
| (S)-2-(S)-Amino-1-(2-boron-dihydroxide-pyrrolidin-1-yl)-hexan-1-one | IC50 | 2 nM | |
| 2-(S)-Amino-4-benzylamino-1-piperidin-1-yl-butan-1-one | IC50 | 2.03 nM | |
| [(2R)-1-[(2S)-2-amino-2-cyclohexylacetyl]pyrrolidin-2-yl]boronic acid | IC50 | 2.1 nM | US-11559537: Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists |
| 2-Cyclodecylamino-1-pyrrolidin-1-yl–2-borandihydroxy-ethanone | IC50 | 2.2 nM | |
| (S)-2-Amino-4-(4-chloro-benzylamino)-1-(2-methyl-piperidin-1-yl)-butan-1-one | IC50 | 2.3 nM | |
| 3-[((S)-3-Amino-4-oxo-4-piperidin-1-yl-butylamino)-methyl]-benzonitrile | IC50 | 2.7 nM | |
| 2-(S)-Amino-4-(2,4-dimethoxy-benzylamino)-1-piperidin-1-yl-butan-1-one | IC50 | 2.7 nM | |
| (2S,3S)-2-amino-3-(4’-fluorobiphenyl-4-yl)-1-((S)-3-fluoropyrrolidin-1-yl)butan-1-one | IC50 | 2.7 nM | |
| Boronic acid derivative | IC50 | 2.9 nM | US-11559537: Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists |
| (2S,4S)-4-(4-chlorobenzylamino)-2-amino-1-(piperidin-1-yl)hexan-1-one | IC50 | 3.4 nM | |
| 2,6-Diamino-hexanoic acid ((R)-1-boron-dihydroxide-pentyl)-amide | IC50 | 3.7 nM | |
| (2S,4S)-4-(4-chlorobenzylamino)-2-amino-5-phenyl-1-(piperidin-1-yl)pentan-1-one | IC50 | 3.8 nM | |
| 1-((S)-2-Amino-4-benzylamino-butyryl)-piperidine-2-carbonitrile | IC50 | 4 nM | |
| 2-Cyclooctonylamino-1-pyrrolidin-1-yl–2-borandihydroxy-ethanone | IC50 | 4 nM |
ChEMBL bioactivities
647 potent at pChembl≥5 of 1214 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.09 | Ki | 0.082 | nM | CHEMBL98869 |
| 10.09 | Ki | 0.082 | nM | CHEMBL5723377 |
| 9.85 | IC50 | 0.14 | nM | CHEMBL5723377 |
| 9.68 | IC50 | 0.21 | nM | CHEMBL5723377 |
| 9.66 | IC50 | 0.22 | nM | CHEMBL98869 |
| 9.66 | IC50 | 0.22 | nM | CHEMBL98801 |
| 9.64 | IC50 | 0.23 | nM | CHEMBL98762 |
| 9.41 | IC50 | 0.39 | nM | CHEMBL99506 |
| 9.41 | IC50 | 0.39 | nM | CHEMBL418979 |
| 9.39 | IC50 | 0.41 | nM | CHEMBL99247 |
| 9.32 | IC50 | 0.48 | nM | CHEMBL194354 |
| 9.32 | IC50 | 0.48 | nM | CHEMBL398076 |
| 9.32 | IC50 | 0.48 | nM | CHEMBL5723377 |
| 9.32 | IC50 | 0.48 | nM | CHEMBL98869 |
| 9.26 | IC50 | 0.55 | nM | CHEMBL98148 |
| 9.22 | IC50 | 0.6 | nM | CHEMBL97970 |
| 9.21 | IC50 | 0.62 | nM | CHEMBL215299 |
| 9.21 | IC50 | 0.62 | nM | CHEMBL98060 |
| 9.18 | IC50 | 0.66 | nM | CHEMBL99047 |
| 9.14 | IC50 | 0.72 | nM | CHEMBL194428 |
| 9.12 | IC50 | 0.75 | nM | CHEMBL99111 |
| 9.10 | IC50 | 0.8 | nM | CHEMBL98423 |
| 9.06 | IC50 | 0.88 | nM | CHEMBL397057 |
| 9.05 | IC50 | 0.9 | nM | CHEMBL317312 |
| 9.00 | IC50 | 1 | nM | CHEMBL372180 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL98860 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL100370 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL97977 |
| 8.95 | IC50 | 1.13 | nM | CHEMBL317950 |
| 8.88 | IC50 | 1.31 | nM | CHEMBL97884 |
| 8.87 | IC50 | 1.34 | nM | CHEMBL317949 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL98415 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL440325 |
| 8.75 | IC50 | 1.77 | nM | CHEMBL327499 |
| 8.74 | IC50 | 1.8 | nM | CHEMBL196933 |
| 8.74 | IC50 | 1.8 | nM | CHEMBL101401 |
| 8.72 | IC50 | 1.91 | nM | CHEMBL430661 |
| 8.70 | IC50 | 2 | nM | CHEMBL194852 |
| 8.69 | IC50 | 2.03 | nM | CHEMBL99263 |
| 8.66 | IC50 | 2.2 | nM | CHEMBL196267 |
| 8.64 | IC50 | 2.3 | nM | CHEMBL319520 |
| 8.57 | IC50 | 2.7 | nM | CHEMBL237336 |
| 8.57 | IC50 | 2.7 | nM | CHEMBL330600 |
| 8.57 | IC50 | 2.7 | nM | CHEMBL99260 |
| 8.47 | IC50 | 3.4 | nM | CHEMBL215244 |
| 8.43 | IC50 | 3.7 | nM | CHEMBL194517 |
| 8.42 | IC50 | 3.8 | nM | CHEMBL214630 |
| 8.40 | IC50 | 4 | nM | CHEMBL382974 |
| 8.40 | IC50 | 4 | nM | CHEMBL329314 |
| 8.39 | IC50 | 4.1 | nM | CHEMBL371130 |
PubChem BioAssay actives
728 with measured affinity, of 2395 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 |
|---|---|---|---|---|
| (2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-piperidin-1-ylbutan-1-one | 343975: Inhibition of DPP2 | ki | 0.0001 | uM |
| (2S)-2-amino-4-[(4-chlorophenyl)methyl-methylamino]-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0002 | uM |
| (2S)-2-amino-4-[(2-chlorophenyl)methylamino]-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0002 | uM |
| (2S)-2-amino-4-[(4-phenylmethoxyphenyl)methylamino]-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0004 | uM |
| (2S)-2-amino-4-[(2-phenylmethoxyphenyl)methylamino]-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0004 | uM |
| (2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(4-fluoropiperidin-1-yl)butan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0004 | uM |
| [(1R)-1-[[(2S)-2,4-diaminobutanoyl]amino]pentyl]boronic acid | 305098: Inhibition of human DPP2 | ic50 | 0.0005 | uM |
| [(1S)-1-[[(2S)-2,4-diaminobutanoyl]amino]pentyl]boronic acid | 254911: Inhibitory concentration against human dipeptidylpeptidase 7 | ic50 | 0.0005 | uM |
| (2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(4-methylpiperidin-1-yl)butan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0006 | uM |
| (2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(3-fluoropiperidin-1-yl)butan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0006 | uM |
| (2S)-2-amino-4-(dibenzylamino)-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0006 | uM |
| (2S,4S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-piperidin-1-ylpentan-1-one | 270815: Inhibition of DPP2 | ic50 | 0.0006 | uM |
| (2S)-2-amino-4-[(4-methoxyphenyl)methylamino]-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0007 | uM |
| [(2S)-1-[(2S)-2,4-diaminobutanoyl]pyrrolidin-2-yl]boronic acid | 254911: Inhibitory concentration against human dipeptidylpeptidase 7 | ic50 | 0.0007 | uM |
| (2S)-2-amino-1-piperidin-1-yl-4-(thiophen-2-ylmethylamino)butan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0008 | uM |
| (2S)-2-amino-1-piperidin-1-yl-4-(pyridin-4-ylmethylamino)butan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0008 | uM |
| (2S)-2-amino-4-(2-phenylethylamino)-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0009 | uM |
| (2S)-1-[(3aR,6aR)-3,3a,4,5,6,6a-hexahydro-2H-cyclopenta[b]pyrrol-1-yl]-2,4-diaminobutan-1-one | 305098: Inhibition of human DPP2 | ic50 | 0.0009 | uM |
| [(2R)-1-[2-[(4-pentyl-1-bicyclo[2.2.2]octanyl)amino]acetyl]pyrrolidin-2-yl]boronic acid | 255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay | ic50 | 0.0010 | uM |
| (2S)-2-amino-4-(naphthalen-2-ylmethylamino)-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0011 | uM |
| (2S)-2-amino-4-(cyclohexylmethylamino)-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0011 | uM |
| (2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(3,6-dihydro-2H-pyridin-1-yl)butan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0011 | uM |
| (2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(3-methylpiperidin-1-yl)butan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0011 | uM |
| (2S)-2-amino-4-(naphthalen-1-ylmethylamino)-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0013 | uM |
| (2S)-2-amino-4-[(3-chlorophenyl)methylamino]-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0013 | uM |
| N-[(3S)-3-amino-4-oxo-4-piperidin-1-ylbutyl]acetamide | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0015 | uM |
| (2S)-2-amino-4-anilino-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0015 | uM |
| 2-[(3S)-3-amino-4-oxo-4-piperidin-1-ylbutyl]guanidine | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0018 | uM |
| (2S)-2-amino-4-[(3-methoxyphenyl)methylamino]-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0018 | uM |
| [(2R)-1-[2-(cycloheptylamino)acetyl]pyrrolidin-2-yl]boronic acid | 255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay | ic50 | 0.0018 | uM |
| (2S)-2-amino-4-(3-phenylpropylamino)-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0019 | uM |
| [(2S)-1-[(2S)-2-aminohexanoyl]pyrrolidin-2-yl]boronic acid | 254911: Inhibitory concentration against human dipeptidylpeptidase 7 | ic50 | 0.0020 | uM |
| (2S)-2-amino-4-(benzylamino)-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0020 | uM |
| [(2R)-1-[2-(cyclodecylamino)acetyl]pyrrolidin-2-yl]boronic acid | 255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay | ic50 | 0.0022 | uM |
| (2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(2-methylpiperidin-1-yl)butan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0023 | uM |
| 3-[[[(3S)-3-amino-4-oxo-4-piperidin-1-ylbutyl]amino]methyl]benzonitrile | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0027 | uM |
| (2S)-2-amino-4-[(2,4-dimethoxyphenyl)methylamino]-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0027 | uM |
| (2S,3S)-2-amino-3-[4-(4-fluorophenyl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]butan-1-one | 393710: Inhibition of QPP | ic50 | 0.0027 | uM |
| (2S,4S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-piperidin-1-ylhexan-1-one | 270815: Inhibition of DPP2 | ic50 | 0.0034 | uM |
| [(1S)-1-[[(2S)-2,6-diaminohexanoyl]amino]pentyl]boronic acid | 254911: Inhibitory concentration against human dipeptidylpeptidase 7 | ic50 | 0.0037 | uM |
| (2S,4S)-2-amino-4-[(4-chlorophenyl)methylamino]-5-phenyl-1-piperidin-1-ylpentan-1-one | 270815: Inhibition of DPP2 | ic50 | 0.0038 | uM |
| 1-[(2S)-2-amino-4-(benzylamino)butanoyl]piperidine-2-carbonitrile | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0040 | uM |
| [(2R)-1-[2-(cyclooctylamino)acetyl]pyrrolidin-2-yl]boronic acid | 255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay | ic50 | 0.0040 | uM |
| [(2R)-1-[2-(cyclohexylamino)acetyl]pyrrolidin-2-yl]boronic acid | 255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay | ic50 | 0.0041 | uM |
| (2S)-2-amino-4-[bis[(4-chlorophenyl)methyl]amino]-1-piperidin-1-ylbutan-1-one | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0042 | uM |
| 6-[[(3S)-3-amino-4-oxo-4-piperidin-1-ylbutyl]amino]pyridine-3-carbonitrile | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0046 | uM |
| [(1S)-1-[[(2S)-2,5-diaminopentanoyl]amino]pentyl]boronic acid | 254911: Inhibitory concentration against human dipeptidylpeptidase 7 | ic50 | 0.0047 | uM |
| 4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2148261: Binding affinity to human DPP7 incubated for 45 mins by Kinobead based pull down assay | kd | 0.0053 | uM |
| [(2R)-1-[(2R)-2-aminopropanoyl]pyrrolidin-2-yl]boronic acid | 255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay | ic50 | 0.0063 | uM |
| 1-[(2S)-2-amino-4-[(4-chlorophenyl)methylamino]butanoyl]piperidine-2-carbonitrile | 56221: Inhibition of human Dipeptidylpeptidase II (DPP II) | ic50 | 0.0065 | uM |
CTD chemical–gene interactions
40 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sodium arsenite | decreases expression, increases expression | 2 |
| UAMC00039 | decreases reaction, increases cleavage, increases abundance, decreases activity | 2 |
| Valproic Acid | decreases expression, increases methylation | 2 |
| bisphenol F | increases expression | 1 |
| methylmercuric chloride | decreases expression | 1 |
| sodium arsenate | increases abundance, increases expression | 1 |
| 4-nitroaniline | increases abundance, increases cleavage, increases reaction, decreases reaction | 1 |
| ferrous chloride | decreases expression | 1 |
| nickel sulfate | decreases expression | 1 |
| benzyloxycarbonylleucyl-leucyl-leucine aldehyde | increases abundance, increases cleavage, increases reaction | 1 |
| alanylproline-4-nitroanilide | increases cleavage, decreases reaction | 1 |
| ICG 001 | increases expression | 1 |
| bisphenol B | increases expression | 1 |
| bisphenol S | increases expression | 1 |
| jinfukang | affects cotreatment, increases expression | 1 |
| (+)-JQ1 compound | decreases expression | 1 |
| bisphenol AF | increases expression | 1 |
| Temozolomide | decreases expression | 1 |
| Sunitinib | increases expression | 1 |
| Air Pollutants | affects expression, increases abundance | 1 |
| Arbutin | decreases expression | 1 |
| Arsenic | increases abundance, increases expression | 1 |
| Benzo(a)pyrene | increases expression | 1 |
| Cisplatin | affects cotreatment, increases expression | 1 |
| Diazinon | increases methylation | 1 |
| Dipeptides | increases abundance, increases cleavage, increases reaction, decreases reaction | 1 |
| Estradiol | increases expression | 1 |
| Ethyl Methanesulfonate | decreases expression | 1 |
| Etoposide | increases abundance, increases cleavage, increases reaction | 1 |
| Formaldehyde | decreases expression | 1 |
ChEMBL screening assays
147 unique, capped per target: 142 binding, 4 functional, 1 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL665781 | Binding | Selectivity index of compound was determined for human Dipeptidylpeptidase IV to that of Dipeptidyl-peptidase II | Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases. — *J Med Chem* |
| CHEMBL4617710 | ADMET | Inhibition of mammalian DPP7 (unknown origin) using H-Lys-Pro-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. — *J Med Chem* |
| CHEMBL5723296 | Functional | Affinity Biochemical interaction: (enzymatic assay (fluorogenic substrate cleavage)) EUB0002750aCl DPP7 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
Clinical trials (associated diseases)
Via MONDO — disease-level, not drug-specific.
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for DPP7 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): neurodevelopmental disorder with or without hyperkinetic movements and seizures, autosomal dominant