二肽基肽酶IV的仲脯氨腈抑制剂确定了P1处的最小药效团要求。
Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1.
作者信息
Magnin David R, Taunk Prakash C, Robertson James G, Wang Aiying, Marcinkeviciene Jovita, Kirby Mark S, Hamann Lawrence G
机构信息
Department of Discovery Chemistry, Bristol-Myers Squibb, Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA.
出版信息
Bioorg Med Chem Lett. 2006 Mar 15;16(6):1731-4. doi: 10.1016/j.bmcl.2005.11.098. Epub 2005 Dec 20.
A series of seco-prolinenitrile-containing dipeptides were synthesized and assayed as inhibitors of the N-terminal sequence-specific serine protease dipeptidyl peptidase IV, a promising new target for treatment of type 2 diabetes. The inhibitors described herein assess the minimum structural requirements at P1 for this enzyme, resulting in the identification of inhibitors with low nM potency.
合成了一系列含亚甲基脯氨腈的二肽，并将其作为N端序列特异性丝氨酸蛋白酶二肽基肽酶IV的抑制剂进行测定，该酶是治疗2型糖尿病的一个有前景的新靶点。本文所述的抑制剂评估了该酶在P1位点的最低结构要求，从而鉴定出了具有低纳摩尔效力的抑制剂。
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