DPP4
DPP4 (Dipeptidyl peptidase-4) is an antigenic enzyme expressed on the surface of most cell types and is associated with immune regulation, signal transduction and apoptosis. It is a rather indiscriminate enzyme for which a diverse range of substrates are known. The substrates of CD26/DPPIV are proline(or alanine)-containing peptides and include growth factors, chemokines, neuropeptides, and vasoactive peptides. DPP4 plays a major role in glucose metabolism. It is responsible for the degradation of incretins such as GLP-1. Furthermore, it appears to work as a suppressor in the development of cancer and tumours.
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Sitagliptin(MK 0431)是DPP4高效抑制剂，在Caco-2细胞中IC50值为19nM。
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Linagliptin是高活性DPP-4抑制剂，IC50为1 nM，对hERG的亲和力较低。
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Vildagliptin (LAF-237)抑制DPP−4，IC50为2.3 nM。
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Saxagliptin是选择性可逆的DPP4抑制剂，IC50和Ki分别为26 nM和1.3 nM。
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