par Hou, Xue;Vandermeers, André ;Gourlet, Philippe ;Vandermeers-Piret, Marie-Claire ;Robberecht, Patrick
Référence Neuropharmacology, 33, 10, page (1189-1195)
Publication Publié, 1994
Article révisé par les pairs
Résumé : N-terminally shortened analogues of PACAP(1-27) and PACAP(1-38), and analogues modified in position 1, 2 or 3 were compared for their ability to interact with PACAP receptors and to activate or inhibit adenylate cyclase in rat brain hippocampus membranes. In the PACAP(1-27) series, deletion of the first two amino acids decreased the potency 3000-fold. PACAP fragments (3-27) to (9-27) were inactive on the enzyme. N-terminally shortened PACAP(1-38) analogues showed a similar profile but were 70 to 300-fold more potent than their PACAP(1-27) equivalents. PACAP(6-27) and PACAP(6-38) were competitive inhibitors of the PACAP(1-27) stimulated enzyme. The K(d) values of PACAP((6-27) and PACAP(6-38) were of 1000 and 2 nM respectively. Surprisingly, the K(d) values of PACAP(6-31) and (6-35), that were also unable to stimulate adenylate cyclase activity, were of 3 and 300 nM respectively. Replacement of His1 by Phe1 in PACAP(1-27) reduced the potency 600-fold. Replacement of Ser2 by Ala2 in PACAP(1-27) and PACAP(1-38) was of little consequence. Substitution of Ser2 by Phe2, DPhe2, Arg2 or DArg2 reduced 60 to 1000-fold the PACAP(1-27) potency but only 7 to 30-fold the PACAP(1-38) potency. Phe2 derivatives were inactive on the enzyme. Replacement of Asp3 by Asn reduced 4000-fold the PACAP(1-27) potency. These results suggest that three domains of PACAP(1-38) were involved in binding to rat brain receptors: the N-terminal triplet His-Ser-Asp, the (11-27) area and the C-terminal (27-38) extension; the integrity of two out of three domains sufficed for high affinity interaction at the binding level while His1 and Ser2 and part of the 11-27 area were key elements in receptor-effector coupling.

Documents en relation

DI-fusion

  • Self-reported antibiotic stewardship and infection control measures from 57 intensive care units: An international ID-IRI survey
    par El-Sokkary, Rehab , Erdem, Hakan , Kullar, Ravina , Pekok, Abdullah Umut , Amer, Fatma , Grgić, Svjetlana , Carevic, Biljana , El-Kholy, Amani , Liskova, Anna , Özdemir, Mehmet , Khan, Ejaz Ahmed , Kizmaz, Yesim Uygun , Pandak, Nenad , Pandya, Nirav , Arapović, Jurica , Karaali, Rıdvan , Oztoprak, Nefise , Petrov, Michael M. , Alabadla, Rami , Alay, Handan , El Kholy, Jehan Ali , Landelle, Caroline , Khedr, Reham , Mamtora, Dhruv , Dragovac, Gorana , Fernandez, Ricardo , Evren, Emine Unal , Raka, Lul , Cascio, Antonio , Dauby, Nicolas , Oncul, Ahsen , Balin, Safak Ozer , Cag, Yasemin , Dirani, Natalia , Dogan, Mustafa , Dumitru, Irina Magdalena , Gad, Maha Ali , Darazam, Ilad Alavi , Naghili, Behrouz , Del Vecchio, Rosa Fontana , Licker, Monica , Marino, Andrea , Akhtar, Nasim , Kamal, Mostafa , Angioni, Goffredo , Medić, Deana , Esmaoğlu, Aliye , Gergely, Szabo Balint , Silva-Pinto, André , Santos, Lurdes , Miftode, Ionela Larisa , Tekin, Recep , Wongsurakiat, Phunsup , Khan, Mumtaz Ali , Kurekci, Yesim , Pilli, Hema Prakash , Grozdanovski, Krsto , Miftode, Egidia , Baljic, Rusmir , Uysal, Serhat , Vahabolgu, Haluk , Rello, Jordi
    Publication 2022-08-03
  • Reduced anticoagulation targets in extracorporeal life support (RATE): study protocol for a randomized controlled trial
    par van Minnen, Olivier , Oude Lansink-Hartgring, Annemieke , van den Boogaard, Bas , van den Brule, Judith Maria Dimphena , Bulpa, Pierre , Bunge, Jeroen J.J.H. , Delnoij, Thijs , Elzo Kraemer, Carlos C.V. , Kuijpers, Marijn , Lambermont, Bernard , Maas, Jacinta J.J. , de Metz, Jesse , Michaux, Isabelle , van de Pol, Ineke , van de Poll, Marcel M.C.G. , Raasveld, Senta Jorinde , Raes, Matthias , Dos Reis Miranda, Dinis , Scholten, Erik , Simonet, Olivier , Taccone, Fabio , Vallot, Frédéric , Vlaar, Alexander Petrus Johannes , van den Bergh, Walter Marcel
    Publication 2022-12
  • An optimized hydroponic pipeline for large-scale identification of wheat genotypes with resilient biological nitrification inhibition (BNI) capacity
    par Jauregui, Ivan , Vega-Mas, Izargi , Delaplace, Pierre , Vanderschuren, Hervé , Thonar, Cécile
    Publication 2022-08-01
  • Durability of tetanus seroprotection in people living with HIV.
    par Dauby, Nicolas , Gobert, Cathy , Benslimane, Asma , Nagant, Carole , Necsoi, Coca Valentina , Van den Wijngaert, Sigi , Corazza, Francis , Delforge, Marc , De Wit, Stéphane
    Publication 2022-06-01
  • Aquaporins: Unexpected actors in autoimmune diseases
    par Delporte, Christine , Soyfoo, Muhammad Shahnawaz
    Publication 2022-06-01