血管活性肠肽及相关肽在人淋巴瘤SUP T1细胞系中诱导快速同源脱敏。

VIP and related peptides induce rapid homologous desensitization in the human lymphoma SUP T1 cell line.

作者信息

Robberecht P, De Neef P, Waelbroeck M, Tastenoy M, Christophe J

机构信息

Department of Biochemistry and Nutrition, Medical School, Université Libre de Bruxelles, Belgium.

出版信息

Peptides. 1989 Mar-Apr;10(2):441-6. doi: 10.1016/0196-9781(89)90056-9.

DOI:10.1016/0196-9781(89)90056-9

PMID:2474155

Abstract

Incubation of human SUP T1 lymphoblasts with VIP, helodermin and related peptides induced homologous desensitization within 5 min as indicated by: 1) a secondary decrease in cellular cyclic AMP levels, even in the presence of phosphodiesterase inhibitors, 2) a reduced capacity of cells to bind [125I]helodermin, 3) decreased helodermin stimulation of adenylate cyclase activity in membranes, and 4) unaffected NaF- and Gpp[NH]p-stimulated adenylate cyclase activities. The desensitizing ability of all peptides correlated with their efficacy to occupy cell receptors, except for [D-Phe2]VIP, a partial VIP agonist with low intrinsic activity, that did not desensitize.

摘要

用人SUP T1淋巴母细胞与血管活性肠肽（VIP）、蛙皮素及其相关肽一起孵育，5分钟内即可诱导同源脱敏，表现为：1）即使存在磷酸二酯酶抑制剂，细胞内环磷酸腺苷（cAMP）水平也会二次下降；2）细胞结合[125I]蛙皮素的能力降低；3）膜中腺苷酸环化酶活性受蛙皮素刺激的程度降低；4）氟化钠（NaF）和鸟苷-5'-O-(3-硫代三磷酸)（Gpp[NH]p）刺激的腺苷酸环化酶活性不受影响。除了[D-苯丙氨酸2]VIP（一种具有低内在活性的部分VIP激动剂，不产生脱敏作用）外，所有肽的脱敏能力与其占据细胞受体的效力相关。