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Article ; Online: Enhancement of Inhibitory Activity by Combining Allosteric Inhibitors Putatively Binding to Different Allosteric Sites on Cathepsin K.

Sato, Shun / Yamamoto, Kana / Ito, Moeno / Nishino, Katsutoshi / Otsuka, Takanao / Irie, Kazuhiro / Nagao, Masaya

Molecules (Basel, Switzerland)

2023  Volume 28, Issue 10

Abstract: Background: Cathepsin K, which is involved in bone resorption, is a good target for treating osteoporosis, but no clinically approved medicine has been developed. Recently, allosteric inhibitors with high specificity and few side effects have been ... ...

Abstract Background: Cathepsin K, which is involved in bone resorption, is a good target for treating osteoporosis, but no clinically approved medicine has been developed. Recently, allosteric inhibitors with high specificity and few side effects have been attracting attention for use in new medicines.
Methods: Cathepsin K inhibitors were isolated from the methanol extract of
Results: Two types of cathepsin K inhibitors were identified in the methanol extract of
Conclusions: Different allosteric inhibitors that bind to different sites in combination, as shown in this study, may be useful for designing new allosteric inhibitory drugs with high specificity and few side effects.
MeSH term(s) Humans ; Cathepsin K/metabolism ; Allosteric Site ; Kinetics ; Methanol ; Bone Resorption ; Cathepsins/metabolism
Chemical Substances Cathepsin K (EC 3.4.22.38) ; Methanol (Y4S76JWI15) ; Cathepsins (EC 3.4.-)
Language English
Publishing date 2023-05-19
Publishing country Switzerland
Document type Journal Article
ZDB-ID 1413402-0
ISSN 1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online) 1420-3049
ISSN 1431-5165 ; 1420-3049
DOI 10.3390/molecules28104197
Shelf mark
Zs.MO 81: Show issues
Database MEDical Literature Analysis and Retrieval System OnLINE

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