cathepsin S | C1: Papain | IUPHAR Guide to IMMUNOPHARMACOLOGY

Top ▲

cathepsin S

Target id: 2353

Nomenclature: cathepsin S

Family: C1: Papain

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: ON :     cathepsin S has curated data in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 331 1q21 CTSS cathepsin S
Mouse - 340 3 F2.1 Ctss cathepsin S
Rat - 330 2q34 Ctss cathepsin S
Previous and Unofficial Names
Cat S
Database Links
Specialist databases
MEROPS C01.034 (Hs)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound (R)-26 [PMID: 22686657] Hs Inhibition 9.3 pKi 1
pKi 9.3 (Ki 5.5x10-10 M) [1]
petesicatib Hs Inhibition 10.0 pIC50 5
pIC50 10.0 (IC50 1x10-10 M) [5]
petesicatib Mm Inhibition 9.5 pIC50 5
pIC50 9.5 (IC50 3x10-10 M) [5]
LHVS Hs Inhibition 9.0 pIC50 4
pIC50 9.0 (IC50 1x10-9 M) [4]
odanacatib Hs Inhibition 7.2 pIC50 2
pIC50 7.2 (IC50 6x10-8 M) [2]
View species-specific inhibitor tables
General Comments
Cathepsin S, is a lysosomal cysteine protease, whch plays an important role in antigen presentation. Selective cathepsin S inhibitors are being developed for their therapeutic potential in autoimmune disorders, atherosclerosis, osteoporosis, osteoarthritis and cancer [3].


Show »

1. Frizler M, Schmitz J, Schulz-Fincke AC, Gütschow M. (2012) Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F. J. Med. Chem., 55 (12): 5982-6. [PMID:22686657]

2. Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong le T, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T et al.. (2008) The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg. Med. Chem. Lett., 18 (3): 923-8. [PMID:18226527]

3. Lee-Dutra A, Wiener DK, Sun S. (2011) Cathepsin S inhibitors: 2004-2010. Expert Opin Ther Pat, 21 (3): 311-37. [PMID:21342054]

4. Méthot N, Rubin J, Guay D, Beaulieu C, Ethier D, Reddy TJ, Riendeau D, Percival MD. (2007) Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. J. Biol. Chem., 282 (29): 20836-46. [PMID:17535802]

5. Tato M, Kumar SV, Liu Y, Mulay SR, Moll S, Popper B, Eberhard JN, Thomasova D, Rufer AC, Gruner S et al.. (2017) Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury. Sci Rep, 7 (1): 2775. [PMID:28584258]

6. Thurmond RL, Sun S, Karlsson L, Edwards JP. (2005) Cathepsin S inhibitors as novel immunomodulators. Curr Opin Investig Drugs, 6 (5): 473-82. [PMID:15912960]

How to cite this page

C1: Papain: cathepsin S. Last modified on 19/03/2018. Accessed on 18/01/2019. IUPHAR/BPS Guide to PHARMACOLOGY,