MK204 is a potent and selective inhibitor of aldo-keto reductase family member 1B10 (AKR1B10).
MK204 is a potent and selective inhibitor of aldo-keto reductase family member 1B10 (AKR1B10). AKR1B10 is induced in several cancer types, in particular, hepatocellular carcinoma, and may be involved with drug resistance. MK204 appears to target a distinct AKR1B10 inner specificity pocket not present in the closely related aldose reductase. MK204 had an IC50 value of 80 nM compared to an IC50 value of 21.7 μM for aldose reductase.
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ACS chemical biology, 11(10), 2693-2705 (2016-10-22)
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
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