Gourlet P, Vandermeers A, Vandermeers-Piret M C, Rathé J, De Neef P, Robberecht P
Department of Biochemistry and Nutrition, School of Medicine, Université Libre de Bruxelles, Belgium.
Regul Pept. 1996 Apr 23;62(2-3):125-30. doi: 10.1016/0167-0115(96)00010-9.
Pituitary adenylate cyclase-activating polypeptide (PACAP) analogues were tested for their ability to occupy the recombinant selective PACAP receptors (PACAP type I receptors) and the non-selective PACAP-vasoactive intestinal polypeptide (VIP) receptors (PACAP type II, VIP1 and PACAP type II, VIP2 receptors), stably transfected and expressed in Chinese hamster ovary cells. Their capacity to stimulate the adenylate cyclase activity was also measured. The synthetic analogues tested were peptides shortened at the carboxyl terminus by the removal of 1-4 amino acids (PACAP-26 to PACAP-23). All the peptides discriminated the 3 receptor subtypes and had the highest affinity for the VIP1 receptors, and the lowest affinity for the VIP2 receptors; PACAP-25 having the highest ability to discriminate the VIP1 and VIP2 receptors. All the peptides tested were full agonists on the PACAP I and VIP1 receptors; PACAP-25 and -26 were partial agonists on VIP2 receptors and may be appropriate tools to establish the receptor subtype involved in a given cellular response.
对垂体腺苷酸环化酶激活多肽（PACAP）类似物进行了测试，以检测它们占据稳定转染并在中国仓鼠卵巢细胞中表达的重组选择性PACAP受体（I型PACAP受体）和非选择性PACAP-血管活性肠肽（VIP）受体（II型PACAP、VIP1和II型PACAP、VIP2受体）的能力。还测量了它们刺激腺苷酸环化酶活性的能力。所测试的合成类似物是通过去除1-4个氨基酸在羧基末端缩短的肽（PACAP-26至PACAP-23）。所有肽都能区分3种受体亚型，对VIP1受体具有最高亲和力，对VIP2受体具有最低亲和力；PACAP-25区分VIP1和VIP2受体的能力最强。所有测试的肽对PACAP I和VIP1受体都是完全激动剂；PACAP-25和-26对VIP2受体是部分激动剂，可能是确定参与特定细胞反应的受体亚型的合适工具。
