Article

Structure of AKR1C3 with 3-phenoxybenzoic acid bound.

School of Biological Sciences, University of Auckland, Private Bag 92019, Victoria St. West, Auckland, New Zealand.
Acta Crystallographica Section F Structural Biology and Crystallization Communications (impact factor: 0.51). 04/2012; 68(Pt 4):409-13. DOI:10.1107/S1744309112009049 pp.409-13
Source: PubMed

ABSTRACT Aldo-keto reductase 1C3 (AKR1C3) is a human enzyme that catalyzes the NADPH-dependent reduction of steroids and prostaglandins. AKR1C3 overexpression is associated with the proliferation of hormone-dependent cancers, most notably breast and prostate cancers. Nonsteroidal anti-inflammatory drugs (NSAIDs) and their analogues are well characterized inhibitors of AKR1C3. Here, the X-ray crystal structure of 3-phenoxybenzoic acid in complex with AKR1C3 is presented. This structure provides useful information for the future development of new anticancer agents by structure-guided drug design.

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Keywords

3-phenoxybenzoic acid
 
Aldo-keto reductase 1C3
 
catalyzes
 
hormone-dependent cancers
 
inhibitors
 
new anticancer agents
 
Nonsteroidal anti-inflammatory drugs
 
prostaglandins
 
prostate cancers
 
useful information