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Bioorg Med Chem Lett. 2013 Aug 1;23(15):4283-91. doi: 10.1016/j.bmcl.2013.05.088. Epub 2013 Jun 6.

Pin1 inhibitors: Pitfalls, progress and cellular pharmacology.

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Horizon Discovery, Cambridge Research Park, Cambridge CB25 9TL, UK.


Compelling data supports the hypothesis that Pin1 inhibitors will be useful for the therapy of cancer: Pin1 deficient mice resist the induction of breast cancers normally evoked by expression of MMTV-driven Ras or Erb2 alleles. While Pin1 poses challenges for drug discovery, several groups have identified potent antagonists by structure based drug design, significant progress has been made designing peptidic inhibitors and a number of natural products have been found that blockade Pin1, notably epigallocatchechin gallate (EGCG), a major flavonoid in green tea. Here we critically discuss the modes of action and likely specificity of these compounds, concluding that a suitable chemical biology tool for probing the function of Pin1 has yet to be found. We conclude by outlining some open questions regarding the target validation of Pin1 and the prospects for identification of improved inhibitors in the future.

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