Jensen R T, Coy D H
Cell Biology Section, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
Trends Pharmacol Sci. 1991 Jan;12(1):13-9. doi: 10.1016/0165-6147(91)90483-9.
Bombesin and the mammalian-related peptides gastrin-releasing peptide (GRP), GRP and neuromedin B have been shown to have numerous actions in the CNS, gastrointestinal tract and on growth. However, the role of the peptides in various physiological processes has remained unclear because of the lack of potent antagonists. Recent in vitro studies have described four different classes of bombesin receptor antagonist, some of which are active in the nanomolar range and in vivo. Robert Jensen and David Coy describe recent insights into peptide structural determinants of biological activity. Evidence from structure-function studies have resulted in identification of some analogues that function as potent antagonists in all systems examined. Furthermore, various subtypes of bombesin receptors can now be differentiated by these various classes of antagonist.
蛙皮素以及与哺乳动物相关的肽类，如胃泌素释放肽（GRP）、GRP和神经降压素B，已被证明在中枢神经系统、胃肠道以及生长方面具有多种作用。然而，由于缺乏有效的拮抗剂，这些肽在各种生理过程中的作用仍不明确。最近的体外研究描述了四类不同的蛙皮素受体拮抗剂，其中一些在纳摩尔范围内具有活性且在体内也有活性。罗伯特·詹森和大卫·科伊描述了对生物活性肽结构决定因素的最新见解。结构-功能研究的证据导致鉴定出一些在所有检测系统中都起有效拮抗剂作用的类似物。此外，现在可以通过这些不同类别的拮抗剂来区分蛙皮素受体的各种亚型。
