1q6k
From Proteopedia
Cathepsin K complexed with t-butyl(1S)-1-cyclohexyl-2-oxoethylcarbamate
Structural highlights
DiseaseCATK_HUMAN Defects in CTSK are the cause of pycnodysostosis (PKND) [MIM:265800. PKND is an autosomal recessive osteochondrodysplasia characterized by osteosclerosis and short stature.[1] [2] [3] [4] FunctionCATK_HUMAN Closely involved in osteoclastic bone resorption and may participate partially in the disorder of bone remodeling. Displays potent endoprotease activity against fibrinogen at acid pH. May play an important role in extracellular matrix degradation. Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMedThe synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and 15 nM. Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.,Catalano JG, Deaton DN, Furfine ES, Hassell AM, McFadyen RB, Miller AB, Miller LR, Shewchuk LM, Willard DH Jr, Wright LL Bioorg Med Chem Lett. 2004 Jan 5;14(1):275-8. PMID:14684342[5] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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Categories: Homo sapiens | Large Structures | Catalano JG | Deaton DN | Furfine ES | Hassell AM | McFadyen RB | Miller AB | Miller LR | Shewchuk LM | Willard DH | Wright LL
