| Title : 4-Substituted boro-proline dipeptides: synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities - Wu_2012_Bioorg.Med.Chem.Lett_22_5536 |
| Author(s) : Wu W , Liu Y , Milo LJ, Jr. , Shu Y , Zhao P , Li Y , Woznica I , Yu G , Sanford DG , Zhou Y , Poplawski SE , Connolly BA , Sudmeier JL , Bachovchin WW , Lai JH |
| Ref : Bioorganic & Medicinal Chemistry Lett , 22 :5536 , 2012 |
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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. |
| PubMedSearch : Wu_2012_Bioorg.Med.Chem.Lett_22_5536 |
| PubMedID: 22853995 |
| Inhibitor | Talabostat |
Wu W, Liu Y, Milo LJ, Jr., Shu Y, Zhao P, Li Y, Woznica I, Yu G, Sanford DG, Zhou Y, Poplawski SE, Connolly BA, Sudmeier JL, Bachovchin WW, Lai JH (2012)
4-Substituted boro-proline dipeptides: synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities
Bioorganic & Medicinal Chemistry Lett
22 :5536
Wu W, Liu Y, Milo LJ, Jr., Shu Y, Zhao P, Li Y, Woznica I, Yu G, Sanford DG, Zhou Y, Poplawski SE, Connolly BA, Sudmeier JL, Bachovchin WW, Lai JH (2012)
Bioorganic & Medicinal Chemistry Lett
22 :5536