Formylchromone derivatives as irreversible and selective inhibitors of human protein tyrosine phosphatase 1B. Kinetic and modeling studies |
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Authors: | Shim Yi Sup Kim Ki Chul Lee Kyung A Shrestha Suja Lee Keun-Hyeung Kim Chan Kyung Cho Hyeongjin |
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Institution: | Department of Chemistry and Institute of Molecular Cell Biology, Inha University, Yonghyun-dong, Nam-ku, Incheon 402-751, Republic of Korea. |
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Abstract: | A series of formylchromone derivatives were synthesized as PTP1B inhibitors and some of them were potent against PTP1B with IC50 values as low as 1.0 microM. They exhibited remarkable selectivity for PTP1B over other human PTPases. Kinetic studies revealed that formylchromone derivatives are irreversible and active site-directed inhibitors. Molecular modeling study identified the orientation of the inhibitor bound at the active site of PTP1B. |
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