Presence of highly selective receptors for PACAP (pituitary adenylate cyclase activating peptide) in membranes from the rat pancreatic acinar cell line AR 4‐2J

FEBS Letters

Gossen, Denis²  Miyata, Atsuro¹  Cauvin, Annick²  Buscail, Louis²  Christophe, Jean²  De Neef, Philippe²  Coy, David H.¹  Gourlet, Philippe²  Arimura, Akira¹  Robberecht, Patrick² 

[1] US-Japan Biomédical Research Laboratories, Tulane University, Hebert Center, Belle Chasse, LA 70037, USA;Department of Biochemistry and Nutrition. Medical School, Université Libre de Bruxelles, Brussels, Belgium

关键词: Pituitary adenylate cyclase activating peptide receptor;    Vasoactive intestinal peptide;    Helodennin;    Adenylate cyclase;    Pancreatic acinar cell line AR 4-2J;    (Rat);    K d;    concentration required for half-maximal inhibition of tracer binding to a given class of receptors;    PACAP-38 and PACAP-27;    pituitary adenylate cyclase activating peptides in full natural version (38 residues) and as an amidated N-terminal peptide (27 residues);    VIP;    vasoactive intestinal peptide;    rat PHI and PHV;    peptide histidine isoleucinamide (1-28) and peptide histidine valine (1-42) from rat;    GRF;    growth hormone releasing factor;    CCK;    cholecystokinin;    EGF;    epidermal growth factor;    FGF;    fibroblast growth factor;    KIU;    kallikrein inhibitor unit;   

DOI  :  10.1016/0014-5793(90)80158-F

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 (K _d =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 (K _act = 0.2 nM) being much higher than that of VIP (K _act= 100 nM) and helodemin (K _act = 30 nM). Chemical cross-linking of [¹²⁵I]PACAP-27 followed by SDS-PAGE and autoradiography revealed a specifically cross-linked peptide with an M _r, of 68000 (including 3000 for one PACAP-27 molecule).

【 授权许可】

Unknown