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Saxagliptin

沙格列汀
Mechanism of action:
Saxagliptin 是一種二肽基肽酶-4 抑制劑(dipeptidyl peptidase-4 inhibitor)。二肽基肽酶-4(DPP-4)是一種負責分解腸泌素的酵素,腸泌素比如胰高血糖素樣肽-1(glucagon-like peptide-1)和葡萄糖依賴性促胰島素多肽(glucose-dependent insulinotropic polypeptide)等。當 saxagliptin 抑制二肽基肽酶-4 後,使腸泌素不易被分解,在血中濃度與作用時間延長,能促進胰島 β 細胞分泌胰島素;抑制胰島 α 細胞分泌升糖素(glucagon)。
Reference(s):
1. Rosenstock J et al. (2008). Glucose-lowering activity of the dipeptidyl peptidase-4 inhibitor saxagliptin in drug-naive patients with type 2 diabetes. Diabetes Obes Metab.
2. Metzler WJ et al. (2008). Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation. Protein Sci.
3. Crepaldi G et al. (2007). Dipeptidyl peptidase 4 (DPP-4) inhibitors and their role in Type 2 diabetes management. J Endocrinol Invest.
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