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Issue 8, 2011
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Overcoming retinoic acid receptor-α based testicular toxicity in the optimisation of glucokinase activators

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Abstract

Small molecule activators of the glucokinase enzyme have the potential to deliver a level of glycaemic control that is superior to current oral agents and hence have great promise as new therapies for Type 2 Diabetes. As such, attempts to discover glucokinase activators suitable for clinical development have been the focus of many major pharmaceutical research programmes. Here we describe how we have overcome a testicular toxicological liability in our pyridine acid lead series, which we show can be ascribed to antagonism of the retinoic acid receptor-α.

Graphical abstract: Overcoming retinoic acid receptor-α based testicular toxicity in the optimisation of glucokinase activators

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Publication details

The article was received on 30 Mar 2011, accepted on 20 May 2011 and first published on 10 Jun 2011


Article type: Concise Article
DOI: 10.1039/C1MD00090J
Med. Chem. Commun., 2011,2, 771-774

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    Overcoming retinoic acid receptor-α based testicular toxicity in the optimisation of glucokinase activators

    M. J. Waring, I. J. Brogan, M. Coghlan, C. Johnstone, H. B. Jones, B. Leighton, D. McKerrecher, K. G. Pike and G. R. Robb, Med. Chem. Commun., 2011, 2, 771
    DOI: 10.1039/C1MD00090J

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