Target Information
| Target General Information | Top | |||||
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| Target ID |
T45287
(Former ID: TTDI03026)
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| Target Name |
Aspartyl aminopeptidase (DNPEP)
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| Synonyms |
DAP; ASPEP
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| Gene Name |
DNPEP
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Hypertension [ICD-11: BA00-BA04] | |||||
| Function |
Likely to play an important role in intracellular protein and peptide metabolism. Aminopeptidase with specificity towards an acidic amino acid at the N-terminus.
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| BioChemical Class |
Peptidase
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| UniProt ID | ||||||
| EC Number |
EC 3.4.11.21
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| Sequence |
MSGHSPTRGAMQVAMNGKARKEAVQTAAKELLKFVNRSPSPFHAVAECRNRLLQAGFSEL
KETEKWNIKPESKYFMTRNSSTIIAFAVGGQYVPGNGFSLIGAHTDSPCLRVKRRSRRSQ VGFQQVGVETYGGGIWSTWFDRDLTLAGRVIVKCPTSGRLEQQLVHVERPILRIPHLAIH LQRNINENFGPNTEMHLVPILATAIQEELEKGTPEPGPLNAVDERHHSVLMSLLCAHLGL SPKDIVEMELCLADTQPAVLGGAYDEFIFAPRLDNLHSCFCALQALIDSCAGPGSLATEP HVRMVTLYDNEEVGSESAQGAQSLLTELVLRRISASCQHPTAFEEAIPKSFMISADMAHA VHPNYLDKHEENHRPLFHKGPVIKVNSKQRYASNAVSEALIREVANKVKVPLQDLMVRND TPCGTTIGPILASRLGLRVLDLGSPQLAMHSIREMACTTGVLQTLTLFKGFFELFPSLSH NLLVD Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | QGC-001 | Drug Info | Phase 2 | Hypertension | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 2 Inhibitor drugs | + | ||||
| 1 | QGC-001 | Drug Info | [1] | |||
| 2 | PMID1738140C9 | Drug Info | [3] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Hydroxylated lecithin | Ligand Info | |||||
| Structure Description | Crystal Structure of Human Aspartyl Aminopeptidase (DNPEP) in complex with Aspartic acid Hydroxamate | PDB:4DYO | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [4] |
| PDB Sequence |
GKARKEAVQT
16 AAKELLKFVN26 RSPSPFHAVA36 ECRNRLLQAG46 FSELKETEKW56 NIKPESKYFM 66 TRNSSTIIAF76 AVGGQYVPGN86 GFSLIGAHTD96 SPCLRVKRRS106 RRSQVGFQQV 116 GVETYGGGIW126 STWFDRDLTL136 AGRVIVKCPT146 SGRLEQQLVH156 VERPILRIPH 166 LAIHLQRNIN176 ENFGPNTEMH186 LVPILATAIQ196 EELEKGTERH216 HSVLMSLLCA 226 HLGLSPKDIV236 EMELCLADTQ246 PAVLGGAYDE256 FIFAPRLDNL266 HSCFCALQAL 276 IDSCAGPGSL286 ATEPHVRMVT296 LYDNEEVGSE306 SAQGAQSLLT316 ELVLRRISAS 326 CQHPTAFEEA336 IPKSFMISAD346 MAHAVHPNYL356 DKHEENHRPL366 FHKGPVIKVN 376 SKQRYASNAV386 SEALIREVAN396 KVKVPLQDLM406 VRNDTPCGTT416 IGPILASRLG 426 LRVLDLGSPQ436 LAMHSIREMA446 CTTGVLQTLT456 LFKGFFELFP466 SLAENLY |
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Similarity Proteins
Human Tissue Distribution
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| Chemical Structure based Activity Landscape of Target | Top |
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| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| References | Top | |||||
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| REF 1 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 2 | ClinicalTrials.gov (NCT02322450) Phase IIa Study of the Product QGC001 Compared With Placebo in Patients With Essential Hypertension. U.S. National Institutes of Health. | |||||
| REF 3 | Alpha-Keto amide inhibitors of aminopeptidases. J Med Chem. 1992 Feb 7;35(3):451-6. | |||||
| REF 4 | Structure of human aspartyl aminopeptidase complexed with substrate analogue: insight into catalytic mechanism, substrate specificity and M18 peptidase family. BMC Struct Biol. 2012 Jun 21;12:14. | |||||
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