沙沙利汀
化学
立体化学
对接(动物)
组合化学
磷酸西他列汀
医学
护理部
二甲双胍
糖尿病
内分泌学
作者
Jizhe Dong,Yanchun Gong,Jun Liu,Xiangfeng Chen,Xiaoan Wen,Hongbin Sun
标识
DOI:10.1016/j.bmc.2013.12.061
摘要
All eight stereoisomers of saxagliptin have been synthesized and evaluated for their inhibitory activity against DPP-IV. It was unambiguously confirmed that the configuration of saxagliptin was critical to potent inhibition of DPP-IV. Docking study was performed to elucidate the configuration–activity relationship of saxagliptin stereoisomers. Tyr662 and Tyr470 have been suggested as the key residues of DPP-IV interacting with the inhibitors. This work provides valuable information for further inhibitor design against DPP-IV.
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