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首页> 外文期刊>Drug discovery today >PTP1B as a drug target: recent developments in PTP1B inhibitor discovery.
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PTP1B as a drug target: recent developments in PTP1B inhibitor discovery.

机译：PTP1B作为药物靶标：PTP1B抑制剂发现的最新进展。

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摘要

Protein tyrosine phosphatase 1B (PTP1B) is an effective target for the treatment of both type 2 diabetes and obesity; however, targeting PTP1B for drug discovery is challenging because of the highly conserved and positively charged active-site pocket. Tremendous progress has been made in the development of potent and selective PTP1B inhibitors that engage both the active site and no catalytic sites. Several strategies are being pursued to improve the pharmacological properties of PTP1B inhibitors. These new developments suggest that it is feasible to acquire PTP1B-based, small-molecule therapeutics with the requisite potency and selectivity. Future efforts will probably transform the potent and selective PTP1B inhibitors into orally available drugs with desirable physicochemical properties and in vivo efficacies.
机译：蛋白酪氨酸磷酸酶1B（PTP1B）是治疗2型糖尿病和肥胖症的有效靶点;然而，由于高度保守且带正电荷的活性位点口袋，靶向PTP1B进行药物发现具有挑战性。在有效和选择性的PTP1B抑制剂的开发中取得了巨大的进展，这些抑制剂既与活性位点结合，也没有催化位点。正在采取几种策略来改善PTP1B抑制剂的药理特性。这些新进展表明，以所需的效能和选择性获得基于PTP1B的小分子疗法是可行的。未来的努力可能会将有效的和选择性的PTP1B抑制剂转变为具有理想的理化性质和体内功效的口服药物。

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