An AlphaScreen Assay for the Discovery of Synthetic Chemical Inhibitors of Glucagon Production.
An AlphaScreen Assay for the Discovery of Synthetic Chemical Inhibitors of Glucagon Production.
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DOI：
10.1177/1087057115622201
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发表时间：
2016-04
影响因子：
--
通讯作者：
Roth MG
中科院分区：
文献类型：
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作者：
Evans MR;Wei S;Posner BA;Unger RH;Roth MG
葡萄糖稳态主要由两种相反的激素胰岛素和胰高血糖素控制，当胰岛素不能抑制胰高血糖素作用时，就会导致糖尿病。最近控制糖尿病中胰高血糖素的努力集中在拮抗胰高血糖素受体，其在降低血糖水平方面有效，但在啮齿动物中导致高胰高血糖素血症。另一种策略是用小分子控制胰高血糖素的产生。为了实现这一目标，我们开发了一种用于测量细胞培养基中胰高血糖素的均相AlphaScreen测定法，并将其用于高通量筛选，以发现抑制α细胞样细胞系胰高血糖素分泌的合成化合物。这些化合物中的一些抑制胰高血糖素基因的转录。
Glucose homeostasis is primarily controlled by two opposing hormones, insulin and glucagon, and diabetes results when insulin fails to inhibit glucagon action. Recent efforts to control glucagon in diabetes have focused on antagonizing the glucagon receptor, which is effective in lowering blood glucose levels but leads to hyperglucogonemia in rodents. An alternative strategy would be to control glucagon production with small molecules. In pursuit of this goal, we developed a homogeneous AlphaScreen assay for measuring glucagon in cell culture media and used this in a high-throughput screen to discover synthetic compounds that inhibited glucagon secretion from an alpha cell–like cell line. Some of these compounds inhibited transcription of the glucagon gene.
DOI：
10.1083/jcb.69.2.455
发表时间：
1976-05
期刊：
The Journal of cell biology
影响因子：
--
作者：
Baetens D;Rufener C;Srikant BC;Dobbs R;Unger R;Orci L
通讯作者：
Orci L