PRESENCE OF HIGHLY SELECTIVE RECEPTORS FOR PACAP (PITUITARY ADENYLATE-CYCLASE ACTIVATING PEPTIDE) IN MEMBRANES FROM THE RAT PANCREATIC ACINAR CELL-LINE AR-4-2J
PRESENCE OF HIGHLY SELECTIVE RECEPTORS FOR PACAP (PITUITARY ADENYLATE-CYCLASE ACTIVATING PEPTIDE) IN MEMBRANES FROM THE RAT PANCREATIC ACINAR CELL-LINE AR-4-2J
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DOI：
10.1016/0014-5793(90)80158-f
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发表时间：
1990-03-12
期刊：
影响因子：
3.5
通讯作者：
CHRISTOPHE, J
中科院分区：
文献类型：
--
作者：
BUSCAIL, L;GOURLET, P;CHRISTOPHE, J
我们在来自大鼠胰腺的肿瘤腺泡细胞系AR 4-2J中鉴定了PACAP的高选择性受体。PACAP是一种与血管活性肠肽(VIP)相关的新的下丘脑多肽，经鉴定为天然38个残基的全肽(PACAP-38)和N端酰胺化的27个残基的衍生物(PACAP-27)。这些结合部位与[125I]PACAP-27(Kd=0.4 nM)和PACAP-38有相当大的亲和力，而与VIP和亲和肽Helodemin的亲和力则低1000倍。PACAP-38和PACAP-27(Kact=0.2 nM)的活性明显高于VIP(Kact=100 nM)和Helodemin(Kact=30 nM)。将[125I]PACAP-27进行化学交联，然后进行十二烷基硫酸钠-PAGE和放射自显影，发现了一种特异性的交联肽，其相对分子质量为68000(其中一个PACAP-27分子为3000)。
We characterized highly selective receptors for PACAP, the pituitary adenylate cyclase activating peptide, in the tumoral acinar cell line AR 4-2J derived from the rat pancreas. PACAP, a novel hypothalamic peptide related to vasoactive intestinal peptide (VIP), was tested as the full natural 38-residue peptide (PACAP-38) and as an N-terminal amidated 27-residue derivative (PACAP-27). The binding sites showed considerable affinity for [125I]PACAP-27 (Kd=0.4 nM) and PACAP-38, while their affiity for VIP and the parent peptide helodemin was 1000-fold lower. These receptors were coupled to adenylate cyclase, the potency of PACAP-38 and PACAP-27 (Kact= 0.2 nM) being much higher than that of VIP (Kact= 100 nM) and helodemin (Kact= 30 nM). Chemical cross-linking of [125I]PACAP-27 followed by SDS-PAGE and autoradiography revealed a specifically cross-linked peptide with anMr, of 68000 (including 3000 for one PACAP-27 molecule).