期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 23, 期 4, 页码 849-854出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.12.030
关键词
Saccharin; Metalloenzyme; Carbonic anhydrase IX; CA IX-mimic; Structure-based drug design
资金
- Australian Research Council [DP110100071, FT10100185]
- EU
- National Institutes of Health [CA165284]
Carbonic anhydrase IX (CA IX) is a key modulator of aggressive tumor behavior and a prognostic marker and target for several cancers. Saccharin (SAC) based compounds may provide an avenue to overcome CA isoform specificity, as they display both nanomolar affinity and preferential binding, for CA IX compared to CA II (>50-fold for SAC and >1000-fold when SAC is conjugated to a carbohydrate moiety). The X-ray crystal structures of SAC and a SAC-carbohydrate conjugate bound to a CA IX-mimic are presented and compared to CA II. The structures provide substantial new insight into the mechanism of SAC selective CA isoform inhibition. Published by Elsevier Ltd.
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