Solid-phase assembly and in situ screening of protein tyrosine phosphatase inhibitors |
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| Authors: | Srinivasan Rajavel Tan Lay Pheng Wu Hao Yao Shao Q |
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| Institution: | Department of Chemistry and Biological Sciences, NUS MedChem Program of the Office of Life Sciences, National University of Singapore, Singapore. |
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| Abstract: | A highly efficient solid-phase strategy for assembly of small molecule inhibitors against protein tyrosine phosphatase 1B (PTP1B) is described. The method is highlighted by its simplicity and product purity. A 70-member combinatorial library of analogues of a known PTP1B inhibitor has been synthesized, which upon direct in situ screening revealed a potent inhibitor ( Ki = 7.0 microM) against PTP1B. |
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