cathepsin K | C1: Papain | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

cathepsin K

Target not currently curated in GtoImmuPdb

Target id: 2350

Nomenclature: cathepsin K

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 329 1q21 CTSK cathepsin K
Mouse - 329 3 F2.1 Ctsk cathepsin K
Rat - 329 2q34 Ctsk cathepsin K
Previous and Unofficial Names
Cat K | CTSO | CTSO2 | Ms10q | PKND | PYCD
Database Links
Specialist databases
MEROPS C01.036 (Hs)
Other databases
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.22.38

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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
relacatib Hs Inhibition 9.4 pKi 2
pKi 9.4 (Ki 4.1x10-10 M) [2]
compound 1b [PMID: 16290936] Hs Inhibition 8.7 pKi 1
pKi 8.7 (Ki 1.8x10-9 M) [1]
odanacatib Hs Inhibition 9.7 pIC50 4
pIC50 9.7 (IC50 2x10-10 M) [4]
L873724 Hs Inhibition 9.7 pIC50 3
pIC50 9.7 (IC50 2x10-10 M) [3]
balicatib Hs Inhibition 8.9 pIC50 2
pIC50 8.9 (IC50 1.4x10-9 M) [2]
Phenotypes, Alleles and Disease Models Mouse data from MGI

Show »

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Ctsk+|Ctsktm1(cre)Ska|Esr1tm1Mma Ctsktm1(cre)Ska/Ctsk+,Esr1tm1Mma/Esr1tm1Mma
involves: 129S2/SvPas * C57BL/6 * SJL
MGI:107823  MGI:1352467  MP:0002896 abnormal bone mineralization PMID: 17803905 
Ctsk+|Ctsktm1(cre)Ska|Esr1tm1Mma Ctsktm1(cre)Ska/Ctsk+,Esr1tm1Mma/Esr1tm1Mma
involves: 129S2/SvPas * C57BL/6 * SJL
MGI:107823  MGI:1352467  MP:0001541 abnormal osteoclast physiology PMID: 17803905 
Ctsk+|Ctsktm1(cre)Ska|Esr1tm1Mma Ctsktm1(cre)Ska/Ctsk+,Esr1tm1Mma/Esr1tm1Mma
involves: 129S2/SvPas * C57BL/6 * SJL
MGI:107823  MGI:1352467  MP:0010121 decreased bone mineral density PMID: 17803905 
Ctsk+|Ctsktm1(cre)Ska|Esr1tm1Mma Ctsktm1(cre)Ska/Ctsk+,Esr1tm1Mma/Esr1tm1Mma
involves: 129S2/SvPas * C57BL/6 * SJL
MGI:107823  MGI:1352467  MP:0004992 increased bone resorption PMID: 17803905 
Ctsk+|Ctsktm1(cre)Ska|Esr1tm1Mma Ctsktm1(cre)Ska/Ctsk+,Esr1tm1Mma/Esr1tm1Mma
involves: 129S2/SvPas * C57BL/6 * SJL
MGI:107823  MGI:1352467  MP:0004984 increased osteoclast cell number PMID: 17803905 
Ctsk+|Ctsktm1(cre)Ska|Esr1tm1Mma Ctsktm1(cre)Ska/Ctsk+,Esr1tm1Mma/Esr1tm1Mma
involves: 129S2/SvPas * C57BL/6 * SJL
MGI:107823  MGI:1352467  MP:0000066 osteoporosis PMID: 17803905 
Clinically-Relevant Mutations and Pathophysiology
Disease:  Pycnodysostosis
Disease Ontology: DOID:0080038
OMIM: 265800
Orphanet: ORPHA763

References

Show »

1. Adkison KK, Barrett DG, Deaton DN, Gampe RT, Hassell AM, Long ST, McFadyen RB, Miller AB, Miller LR, Payne JA et al.. (2006) Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?. Bioorg. Med. Chem. Lett., 16 (4): 978-83. [PMID:16290936]

2. Allen JG, Fotsch C, Babij P. (2010) Emerging targets in osteoporosis disease modification. J. Med. Chem., 53 (11): 4332-53. [PMID:20218623]

3. Desmarais S, Massé F, Percival MD. (2009) Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools. Biol. Chem., 390 (9): 941-8. [PMID:19453281]

4. 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]

How to cite this page

C1: Papain: cathepsin K. Last modified on 21/07/2015. Accessed on 20/08/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2350.