4-Substituted boro-proline dipeptides: Synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities |
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| Authors: | Wengen Wu Yuxin Liu Lawrence J Milo Ying Shu Peng Zhao Youhua Li Iwona Woznica Gengli Yu David G Sanford Yuhong Zhou Sarah E Poplawski Beth A Connolly James L Sudmeier William W Bachovchin Jack H Lai |
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| Institution: | Tufts University School of Medicine, Department of Biochemistry, 136 Harrison Ave., Boston, MA 02111, United States. |
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| Abstract: | The boroProline-based dipeptidyl boronic acids were among the first DPP-IV inhibitors identified, and remain the most potent known. We introduced various substitutions at the 4-position of the boroProline ring regioselectively and stereoselectively, and incorporated these aminoboronic acids into a series of 4-substituted boroPro-based dipeptides. Among these dipeptidyl boronic acids, Arg-(4S)-boroHyp (4q) was the most potent inhibitor of DPP-IV, DPP8 and DPP9, while (4S)-Hyp-(4R)-boroHyp (4o) exhibited the most selectivity for DPP-IV over DPP8 and DPP9. |
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