Target Information
Target General Infomation | |||||
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Target ID |
T67102
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Former ID |
TTDR00447
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Target Name |
Cathepsin D
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Gene Name |
CTSD
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Synonyms |
CD; CTSD
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Target Type |
Clinical Trial
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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.
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BioChemical Class |
Peptidase
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Target Validation |
T67102
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UniProt ID | |||||
EC Number |
EC 3.4.23.5
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Sequence |
MQPSSLLPLALCLLAAPASALVRIPLHKFTSIRRTMSEVGGSVEDLIAKGPVSKYSQAVP
AVTEGPIPEVLKNYMDAQYYGEIGIGTPPQCFTVVFDTGSSNLWVPSIHCKLLDIACWIH HKYNSDKSSTYVKNGTSFDIHYGSGSLSGYLSQDTVSVPCQSASSASALGGVKVERQVFG EATKQPGITFIAAKFDGILGMAYPRISVNNVLPVFDNLMQQKLVDQNIFSFYLSRDPDAQ PGGELMLGGTDSKYYKGSLSYLNVTRKAYWQVHLDQVEVASGLTLCKEGCEAIVDTGTSL MVGPVDEVRELQKAIGAVPLIQGEYMIPCEKVSTLPAITLKLGGKGYKLSPEDYTLKVSQ AGKTLCLSGFMGMDIPPPSGPLWILGDVFIGRYYTVFDRDNNRVGFAEAARL |
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Drugs and Mode of Action | |||||
Drug(s) | compound 1 | Drug Info | Clinical trial | Multiple scierosis | [1], [2] |
CI-992 | Drug Info | Terminated | Hypertension | [3] | |
Inhibitor | 1h-Benoximidazole-2-Carboxylic Acid | Drug Info | [4] | ||
Alpha-D-Mannose | Drug Info | [4] | |||
Carbocyclic Peptidomimetic | Drug Info | [5] | |||
CI-992 | Drug Info | [6] | |||
compound 1 | Drug Info | [1] | |||
compound 3 | Drug Info | [7] | |||
GRASSYSTATIN A | Drug Info | [8] | |||
GRL-7234 | Drug Info | [9] | |||
KNI-10006 | Drug Info | [10] | |||
N-Aminoethylmorpholine | Drug Info | [4] | |||
S-Methylcysteine | Drug Info | [4] | |||
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 1 | Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors. Bioorg Med Chem Lett. 1999 Sep 6;9(17):2531-6. | ||||
REF 2 | (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 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002298) | ||||
REF 4 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
REF 5 | J 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 6 | J Med Chem. 1992 Jul 10;35(14):2562-72.Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors. | ||||
REF 7 | 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. 1993 Sep 3;36(18):2614-20. | ||||
REF 8 | J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. | ||||
REF 9 | J 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 10 | Bioorg 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. |
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