- IDD388 Polyhalogenated Derivatives as Probes for an Improved Structure-Based Selectivity of AKR1B10 Inhibitors.
IDD388 Polyhalogenated Derivatives as Probes for an Improved Structure-Based Selectivity of AKR1B10 Inhibitors.
ACS chemical biology (2016-10-22)
Alexandra Cousido-Siah, Francesc X Ruiz, Jindřich Fanfrlík, Joan Giménez-Dejoz, André Mitschler, Martin Kamlar, Jan Veselý, Haresh Ajani, Xavier Parés, Jaume Farrés, Pavel Hobza, Alberto D Podjarny
PMID27359042
摘要
Human enzyme aldo-keto reductase family member 1B10 (AKR1B10) has evolved as a tumor marker and promising antineoplastic target. It shares high structural similarity with the diabetes target enzyme aldose reductase (AR). Starting from the potent AR inhibitor IDD388, we have synthesized a series of derivatives bearing the same halophenoxyacetic acid moiety with an increasing number of bromine (Br) atoms on its aryl moiety. Next, by means of IC
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