Monocyclic thiophenes as protein tyrosine phosphatase 1B inhibitors: capturing interactions with Asp48 |
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| Authors: | Wan Zhao-Kui Lee Jinbo Xu Weixin Erbe David V Joseph-McCarthy Diane Follows Bruce C Zhang Yan-Ling |
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| Institution: | Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA. |
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| Abstract: | A series of monocyclic thiophenes was designed and synthesized as PTP1B inhibitors. Guided by X-ray co-crystal structural information and computational modeling, rational design led to key interactions with Asp48 and improved inhibitory potency against PTP1B. |
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