发现一种具有低亲脂性、低极性表面积和强大体内疗效的强效游离脂肪酸 1 受体激动剂。
Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy.
机构信息
Department of Physics, Chemistry and Pharmacy, University of Southern Denmark , Campusvej 55, DK-5230 Odense M, Denmark.
Institute of Pharmaceutical and Medicinal Chemistry, University of Düsseldorf , Universitätsstrasse 1, D-40225 Düsseldorf, Germany.
出版信息
J Med Chem. 2016 Mar 24;59(6):2841-6. doi: 10.1021/acs.jmedchem.5b01962. Epub 2016 Mar 15.
The free fatty acid receptor 1 (FFA1 or GPR40) is established as an interesting potential target for treatment of type 2 diabetes. However, to obtain optimal ligands, it may be necessary to limit both lipophilicity and polar surface area, translating to a need for small compounds. We here describe the identification of 24, a potent FFA1 agonist with low lipophilicity and very high ligand efficiency that exhibit robust glucose lowering effect.
游离脂肪酸受体 1（FFA1 或 GPR40）已被确立为治疗 2 型糖尿病的一个有前途的潜在靶点。然而，为了获得最佳的配体，可能需要限制亲脂性和极性表面积，这就需要使用小分子化合物。我们在这里描述了 24 的鉴定，它是一种有效的 FFA1 激动剂，具有低亲脂性和非常高的配体效率，具有很强的降血糖作用。
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