Target Information

Target General Infomation
Target ID
T61746
Former ID
TTDR00886
Target Name
Cathepsin B
Gene Name
CTSB
Synonyms
APP secretase; APPS; Cathepsin B1; Cathepsin-B; Cathepsins B; Ctsb; CTSB
Target Type
Discontinued
Disease Asthma [ICD10: J45]
Function
Thiol protease which is believed to participate in intracellular degradation and turnover of proteins. Has also been implicated in tumor invasion and metastasis.
BioChemical Class
Peptidase
Target Validation
T61746
UniProt ID
P07858
EC Number
EC 3.4.22.1
Sequence
MWQLWASLCCLLVLANARSRPSFHPLSDELVNYVNKRNTTWQAGHNFYNVDMSYLKRLCG
TFLGGPKPPQRVMFTEDLKLPASFDAREQWPQCPTIKEIRDQGSCGSCWAFGAVEAISDR
ICIHTNAHVSVEVSAEDLLTCCGSMCGDGCNGGYPAEAWNFWTRKGLVSGGLYESHVGCR
PYSIPPCEHHVNGSRPPCTGEGDTPKCSKICEPGYSPTYKQDKHYGYNSYSVSNSEKDIM
AEIYKNGPVEGAFSVYSDFLLYKSGVYQHVTGEMMGGHAIRILGWGVENGTPYWLVANSW
NTDWGDNGFFKILRGQDHCGIESEVVAGIPRTDQYWEKI
Drugs and Mode of Action
Drug(s) MDL-2170 Drug Info Terminated Discovery agent [1]
Inhibitor (S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate Drug Info [2]
1-(phenyl(p-tolyl)methylene)thiosemicarbazide Drug Info [3]
2-Aminoethanimidic Acid Drug Info [4]
2-Pyridinethiol Drug Info [5]
3-Amino-4-Oxybenzyl-2-Butanone Drug Info [4]
3-Methylphenylalanine Drug Info [4]
Ac-hPhe-Leu-Ala-LeuVSMe Drug Info [6]
Ac-hPhe-Leu-Phe-LeuVSMe Drug Info [6]
Bis(3-bromophenyl)(4-hydroxy)thiosemicarbazone Drug Info [7]
Cbz-Ile-Leu-Ala-LeuVSMe Drug Info [6]
Cbz-Ile-t-ButylhomoGlu-Ala-LeuVSMe Drug Info [6]
Diphenylacetic Acid Drug Info [4]
GNF-PF-5434 Drug Info [8]
Gold trichloride sodium chloride Drug Info [9]
L-006235-1 Drug Info [10]
L-873724 Drug Info [11]
MDL-2170 Drug Info [12]
PTosyl-Glu(OtBu)-Ala-LeuVSMe Drug Info [6]
Z-Ala-Leu-His-Agly-Ile-Val-OMe Drug Info [13]
Z-Ala-Leu-lle-Agly-Ile-Val-NHBzl Drug Info [13]
Z-Ala-Leu-lle-Agly-Ile-Val-OMe Drug Info [13]
Z-Ala-Leu-Nal-Agly-Ile-Val-OMe Drug Info [13]
Z-Ala-Leu-Phe-Agly-Ile-Val-OMe Drug Info [13]
Z-Ala-Leu-Tyr(Me)-Agly-Ile-Val-OMe Drug Info [13]
Z-Arg-Leu-Val-Agly-Ala-Gly-NH2 Drug Info [13]
Z-Arg-Leu-Val-Agly-Ile-Val-OMe Drug Info [13]
Z-Arg-Leu-Val-Agly-Ile-Val-Trp-NH2 Drug Info [13]
Z-Arg-Leu-Val-Agly-Ileu-Val-OMe Drug Info [13]
Z-Arg-Leu-Val-Agly-Trp-Val-Ala-NH2 Drug Info [13]
Z-Arg-Leu-Val-Agly-Val-Ala-NH2 Drug Info [13]
Z-leu-Val-Agly-Val-OBzl Drug Info [13]
[(3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone Drug Info [14]
Pathways
KEGG Pathway Lysosome
Antigen processing and presentation
NetPath Pathway TCR Signaling Pathway
IL2 Signaling Pathway
Reactome Collagen degradation
Trafficking and processing of endosomal TLR
Assembly of collagen fibrils and other multimeric structures
MHC class II antigen presentation
References
REF 1Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003692)
REF 2Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83. Epub 2005 Nov 15.Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?.
REF 3Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5. Epub 2008 Apr 8.Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
REF 4How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 5DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
REF 6J Med Chem. 2006 May 18;49(10):2953-68.Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
REF 7Bioorg Med Chem Lett. 2010 Nov 15;20(22):6610-5. Epub 2010 Sep 15.Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.
REF 8Bioorg Med Chem. 2009 Feb 1;17(3):1064-70. Epub 2008 Feb 7.Substrate optimization for monitoring cathepsin C activity in live cells.
REF 9Bioorg Med Chem Lett. 2004 Oct 18;14(20):5113-6.Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).
REF 10J Med Chem. 2005 Dec 1;48(24):7535-43.Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
REF 11Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33. Epub 2007 Jun 10.The identification of potent, selective, and bioavailable cathepsin S inhibitors.
REF 12J Med Chem. 2009 May 14;52(9):3093-7.Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
REF 13J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.
REF 14Bioorg Med Chem Lett. 2010 Feb 15;20(4):1415-9. Epub 2010 Jan 6.Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.

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