Properties of vasoactive-intestinal-peptide receptors and beta-adrenoceptors in the murine radiation leukemia-virus-induced lymphoma cell line BL/VL3.
1. Based on radioligand binding and adenylate cyclase activation, functional receptors to vasoactive intestinal peptide(VIP)/helodermin, were shown to coexist with beta 2-adrenoceptors and prostaglandin receptors in membranes from a cultured cloned BL/VL3 cell line of murine T-cell lymphoma induced by a radiation leukemia virus. 2. The relative potency of VIP-related peptides to stimulate adenylate cyclase activity was: helodermin greater than VIP greater than peptide histidine isoleucinamide. Five VIP analogs inhibited 125I-iodo-VIP binding and stimulated adenylate cyclase activity, their decreasing order of potency being: VIP greater than [D-Asp3]VIP greater than [D-Ser2]VIP greater than [D-Ala4]VIP = [D-His1]VIP = [D-Phe2]VIP. [D-Phe2]VIP acted as a partial agonist (with an intrinsic activity of 0.1 as compared to that of VIP = 1.0) and competitively inhibited helodermin- and VIP-stimulated adenylate cyclase activity with a similar Ki (0.07-0.10 microM). These data suggest the existence, in this murine T-cell lymphoma, of VIP receptors of the 'helodermin-preferring' subtype that are coupled to adenylate cyclase.
Abello
J
J
Department of Biochemistry and Nutrition, Medical School, Université Libre de Bruxelles.
Damien
C
C
De Neef
P
P
Tastenoy
M
M
Hooghe
R
R
Robberecht
P
P
Christophe
J
J
D000262:Adenylyl Cyclases / Q000378:metabolism; D000527:Alprostadil / Q000494:pharmacology; D000818:Animals; D002395:Catecholamines / Q000494:pharmacology; D002462:Cell Membrane / Q000378:metabolism; D004789:Enzyme Activation / Q000187:drug effects; D036341:Intercellular Signaling Peptides and Proteins; D007953:Leukemia, Radiation-Induced; D008223:Lymphoma / Q000209:etiology / Q000378:metabolism*; D051379:Mice; D010451:Peptide PHI / Q000494:pharmacology; D010455:Peptides / Q000494:pharmacology; D011943:Receptors, Adrenergic, beta / Q000502:physiology*; D011964:Receptors, Gastrointestinal Hormone / Q000502:physiology*; D011982:Receptors, Prostaglandin / Q000502:physiology; D018005:Receptors, Vasoactive Intestinal Peptide; D012190:Retroviridae; D013601:T-Lymphocytes; D014407:Tumor Cells, Cultured; D014660:Vasoactive Intestinal Peptide / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology
D002395:Catecholamines; D036341:Intercellular Signaling Peptides and Proteins; D010451:Peptide PHI; D010455:Peptides; D011943:Receptors, Adrenergic, beta; D011964:Receptors, Gastrointestinal Hormone; D011982:Receptors, Prostaglandin; D018005:Receptors, Vasoactive Intestinal Peptide; D014660:Vasoactive Intestinal Peptide; C040442:heliodermin; D000262:Adenylyl Cyclases; D000527:Alprostadil