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cathepsin D

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Target not currently curated in GtoImmuPdb

Target id: 2345

Nomenclature: cathepsin D

Family: A1: Pepsin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 412 11p15.5 CTSD cathepsin D
Mouse - 410 7 F5 Ctsd cathepsin D
Rat - 407 1q41 Ctsd cathepsin D
Previous and Unofficial Names Click here for help
CatD | CD | ceroid-lipofuscinosis, neuronal 10 | CLN10 | CPSD
Database Links Click here for help
Specialist databases
MEROPS A01.009 (Hs)
Other databases
Alphafold P07339 (Hs), P18242 (Mm), P24268 (Rn)
BRENDA 3.4.23.5
CATH/Gene3D 2.40.70.10
ChEMBL Target CHEMBL2581 (Hs)
Ensembl Gene ENSG00000117984 (Hs), ENSMUSG00000007891 (Mm), ENSRNOG00000020206 (Rn)
Entrez Gene 1509 (Hs), 13033 (Mm), 171293 (Rn)
Human Protein Atlas ENSG00000117984 (Hs)
KEGG Enzyme 3.4.23.5
KEGG Gene hsa:1509 (Hs), mmu:13033 (Mm), rno:171293 (Rn)
OMIM 116840 (Hs)
Orphanet ORPHA159489 (Hs)
Pharos P07339 (Hs)
RefSeq Nucleotide NM_001909 (Hs), NM_009983 (Mm), NM_134334 (Rn)
RefSeq Protein NP_001900 (Hs), NP_034113 (Mm), NP_599161 (Rn)
UniProtKB P07339 (Hs), P18242 (Mm), P24268 (Rn)
Wikipedia CTSD (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human cathepsin D in complex with macrocyclic inhibitor 33
PDB Id:  6QBH
Ligand:  compound 33 [PMID: 32003991]
Resolution:  1.85Å
Species:  Human
References:  3
Enzyme Reaction Click here for help
EC Number: 3.4.23.5

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 3 [PMID: 8410973] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pKi 5
⤷ pKi 7.7 (Ki 1.8x10-8 M) [5]
β-secretase inhibitor IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pKi 2
⤷ pKi 6.3 (Ki 4.48x10-7 M) [2]
compound 1 [PMID: 10498202] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 9.2 pIC50 1
⤷ pIC50 9.2 (IC50 7x10-10 M) [1]
compound 33 [PMID: 32003991] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 8.6 pIC50 3
⤷ pIC50 8.6 (IC50 2.5x10-9 M) [3]
grassystatin A Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 4
⤷ pIC50 7.6 (IC50 2.65x10-8 M) [4]
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
Immuno Process:  Cellular signalling
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Ceroid lipofuscinosis, neuronal, 10
Synonyms: Cathepsin D deficiency
CLN10 disease [Orphanet: ORPHA228337]
Neuronal ceroid lipofuscinosis [Disease Ontology: DOID:14503]
Disease Ontology: DOID:14503
OMIM: 610127
Orphanet: ORPHA228337

References

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1. Dumas J, Brittelli D, Chen J, Dixon B, Hatoum-Mokdad H, König G, Sibley R, Witowsky J, Wong S. (1999) Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors. Bioorg Med Chem Lett, 9 (17): 2531-6. [PMID:10498202]

2. Ghosh AK, Kumaragurubaran N, Hong L, Kulkarni SS, Xu X, Chang W, Weerasena V, Turner R, Koelsch G, Bilcer G et al.. (2007) Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands. J Med Chem, 50 (10): 2399-407. [PMID:17432843]

3. Houštecká R, Hadzima M, Fanfrlík J, Brynda J, Pallová L, Hánová I, Mertlíková-Kaiserová H, Lepšík M, Horn M, Smrčina M et al.. (2020) Biomimetic Macrocyclic Inhibitors of Human Cathepsin D: Structure-Activity Relationship and Binding Mode Analysis. J Med Chem, 63 (4): 1576-1596. [PMID:32003991]

4. Kwan JC, Eksioglu EA, Liu C, Paul VJ, Luesch H. (2009) Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem, 52 (18): 5732-47. [PMID:19715320]

5. Rao CM, Scarborough PE, Kay J, Batley B, Rapundalo S, Klutchko S, Taylor MD, Lunney EA, Humblet CC, Dunn BM. (1993) Specificity in the binding of inhibitors to the active site of human/primate aspartic proteinases: analysis of P2-P1-P1'-P2' variation. J Med Chem, 36 (18): 2614-20. [PMID:8410973]

How to cite this page

A1: Pepsin: cathepsin D. Last modified on 02/09/2021. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2345.