β细胞高亲和力磺酰脲受体的克隆：胰岛素分泌的调节因子

Cloning of the beta cell high-affinity sulfonylurea receptor: a regulator of insulin secretion.

作者信息

Aguilar-Bryan L, Nichols C G, Wechsler S W, Clement J P, Boyd A E, González G, Herrera-Sosa H, Nguy K, Bryan J, Nelson D A

机构信息

Department of Cell Biology, Baylor College of Medicine, Houston, TX 77030, USA.

出版信息

Science. 1995 Apr 21;268(5209):423-6. doi: 10.1126/science.7716547.

DOI:10.1126/science.7716547

PMID:7716547

Abstract

Sulfonylureas are a class of drugs widely used to promote insulin secretion in the treatment of non-insulin-dependent diabetes mellitus. These drugs interact with the sulfonylurea receptor of pancreatic beta cells and inhibit the conductance of adenosine triphosphate (ATP)-dependent potassium (KATP) channels. Cloning of complementary DNAs for the high-affinity sulfonylurea receptor indicates that it is a member of the ATP-binding cassette or traffic ATPase superfamily with multiple membrane-spanning domains and two nucleotide binding folds. The results suggest that the sulfonylurea receptor may sense changes in ATP and ADP concentration, affect KATP channel activity, and thereby modulate insulin release.

摘要

磺脲类药物是一类广泛用于促进胰岛素分泌以治疗非胰岛素依赖型糖尿病的药物。这些药物与胰腺β细胞的磺脲类受体相互作用，并抑制三磷酸腺苷（ATP）依赖性钾（KATP）通道的电导。高亲和力磺脲类受体互补DNA的克隆表明，它是ATP结合盒或转运ATP酶超家族的成员，具有多个跨膜结构域和两个核苷酸结合折叠。结果表明，磺脲类受体可能感知ATP和ADP浓度的变化，影响KATP通道活性，从而调节胰岛素释放。