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(-)-CHANA, a fluorogenic probe for detecting amyloid binding alcohol dehydrogenase HSD10 activity in living cells.
MedLine Citation:
PMID:  20836522     Owner:  NLM     Status:  In-Process    
Abstract/OtherAbstract:
The association of 17β-hydroxysteroid dehydrogenase 10 (HSD10) with β-amyloid in the brain is known to contribute to the progression of Alzheimer's disease. Further, it has been shown that the interaction between the purified HSD10 and β-amyloid inhibits its enzymatic activity. However, to date no system has been developed to enable the study of HSD10 activity in intact living cells. To address this significant shortcoming, we have developed a novel fluorogenic probe, (-)-cyclohexenyl amino naphthalene alcohol [(-)-CHANA], to observe and measure the activity of HSD10 in living cells. The oxidation of (-)-CHANA by HSD10 results in the production and accumulation of a fluorescent product, which can be measured using real-time fluorescence microscopy. This compound permits the measurement of mitochondrial HSD10 activity and its inhibition by both a small molecule HSD10 inhibitor and by β-amyloid, in living cells. Herein, we define the parameters under which this probe can be used. This compound is likely to prove useful in future investigations aimed at developing therapeutic compounds targeting the HSD10-β-amyloid association.
Authors:
Kirsty E A Muirhead; Mary Froemming; Xiaoguang Li; Kamil Musilek; Stuart J Conway; Dalibor Sames; Frank J Gunn-Moore
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-10-08
Journal Detail:
Title:  ACS chemical biology     Volume:  5     ISSN:  1554-8937     ISO Abbreviation:  ACS Chem. Biol.     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2010-12-17     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101282906     Medline TA:  ACS Chem Biol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1105-14     Citation Subset:  IM    
Affiliation:
North Haugh, University, St. Andrews, United Kingdom.
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