Target General Infomation
Target ID
T67102
Former ID
TTDR00447
Target Name
Cathepsin D
Gene Name
CTSD
Synonyms
CD; CTSD
Target Type
Clinical Trial
Disease Hypertension [ICD9: 401; ICD10: I10-I16]
Multiple scierosis [ICD9: 340; ICD10: G35]
Function
Acid protease active in intracellular protein breakdown. Involved in the pathogenesis of several diseases such as breast cancer and possibly Alzheimer disease.
BioChemical Class
Peptidase
Target Validation
T67102
UniProt ID
EC Number
EC 3.4.23.5
Sequence
MQPSSLLPLALCLLAAPASALVRIPLHKFTSIRRTMSEVGGSVEDLIAKGPVSKYSQAVP
AVTEGPIPEVLKNYMDAQYYGEIGIGTPPQCFTVVFDTGSSNLWVPSIHCKLLDIACWIH
HKYNSDKSSTYVKNGTSFDIHYGSGSLSGYLSQDTVSVPCQSASSASALGGVKVERQVFG
EATKQPGITFIAAKFDGILGMAYPRISVNNVLPVFDNLMQQKLVDQNIFSFYLSRDPDAQ
PGGELMLGGTDSKYYKGSLSYLNVTRKAYWQVHLDQVEVASGLTLCKEGCEAIVDTGTSL
MVGPVDEVRELQKAIGAVPLIQGEYMIPCEKVSTLPAITLKLGGKGYKLSPEDYTLKVSQ
AGKTLCLSGFMGMDIPPPSGPLWILGDVFIGRYYTVFDRDNNRVGFAEAARL
Drugs and Mode of Action
Drug(s) compound 1 Drug Info Clinical trial Multiple scierosis [525597], [541668]
CI-992 Drug Info Terminated Hypertension [545148]
Inhibitor 1h-Benoximidazole-2-Carboxylic Acid Drug Info [551393]
Alpha-D-Mannose Drug Info [551393]
Carbocyclic Peptidomimetic Drug Info [527675]
CI-992 Drug Info [527925]
compound 1 Drug Info [525597]
compound 3 Drug Info [534030]
GRASSYSTATIN A Drug Info [530345]
GRL-7234 Drug Info [528786]
KNI-10006 Drug Info [530280]
N-Aminoethylmorpholine Drug Info [551393]
S-Methylcysteine Drug Info [551393]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway Thyroid hormone biosynthesis
KEGG Pathway Sphingolipid signaling pathway
Lysosome
Tuberculosis
NetPath Pathway IL2 Signaling Pathway
Pathway Interaction Database LKB1 signaling events
Ceramide signaling pathway
Direct p53 effectors
Validated nuclear estrogen receptor alpha network
Reactome Collagen degradation
Metabolism of Angiotensinogen to Angiotensins
MHC class II antigen presentation
References
Ref 525597Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors. Bioorg Med Chem Lett. 1999 Sep 6;9(17):2531-6.
Ref 541668(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6541).
Ref 545148Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002298)
Ref 525597Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors. Bioorg Med Chem Lett. 1999 Sep 6;9(17):2531-6.
Ref 527675J Med Chem. 2005 Aug 11;48(16):5175-90.Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics.
Ref 527925J Med Chem. 1992 Jul 10;35(14):2562-72.Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.
Ref 528786J Med Chem. 2007 May 17;50(10):2399-407. Epub 2007 Apr 14.Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.
Ref 530280Bioorg Med Chem. 2009 Aug 15;17(16):5933-49. Epub 2009 Jul 3.alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases.
Ref 530345J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
Ref 534030Specificity in the binding of inhibitors to the active site of human/primate aspartic proteinases: analysis of P2-P1-P1'-P2' variation. J Med Chem. 1993 Sep 3;36(18):2614-20.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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