Literature DB >> 18272364

Discovery and SAR of hydrazide antagonists of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC1-R).

Xenia Beebe1, Daria Darczak, Rachel A Davis-Taber, Marie E Uchic, Victoria E Scott, Michael F Jarvis, Andrew O Stewart.   

Abstract

Potent small molecule antagonists for the PAC(1)-R have been discovered. Previously known antagonists for the PAC(1)-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR.

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Year:  2008        PMID： 18272364     DOI： 10.1016/j.bmcl.2008.01.052

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  14 in total

1.  Allosteric antagonist binding sites in class B GPCRs: corticotropin receptor 1.

Authors:  Supriyo Bhattacharya; Govindan Subramanian; Spencer Hall; Jianping Lin; Abdelazize Laoui; Nagarajan Vaidehi
Journal:  J Comput Aided Mol Des       Date:  2010-05-29       Impact factor: 3.686

Review 2.  Pharmacology and functions of receptors for vasoactive intestinal peptide and pituitary adenylate cyclase-activating polypeptide: IUPHAR review 1.

Authors:  Anthony J Harmar; Jan Fahrenkrug; Illana Gozes; Marc Laburthe; Victor May; Joseph R Pisegna; David Vaudry; Hubert Vaudry; James A Waschek; Sami I Said
Journal:  Br J Pharmacol       Date:  2012-05       Impact factor: 8.739

3.  Development of novel Asf1-H3/H4 inhibitors.

Authors:  Greg F Miknis; Sarah J Stevens; Luke E Smith; David A Ostrov; Mair E A Churchill
Journal:  Bioorg Med Chem Lett       Date:  2014-12-04       Impact factor: 2.823

Review 4.  Peptide-Liganded G Protein-Coupled Receptors as Neurotherapeutics.

Authors:  Lee E Eiden; Ki Ann Goosens; Kenneth A Jacobson; Lorenzo Leggio; Limei Zhang
Journal:  ACS Pharmacol Transl Sci       Date:  2020-03-18

Review 5.  Roles for pituitary adenylate cyclase-activating peptide (PACAP) expression and signaling in the bed nucleus of the stria terminalis (BNST) in mediating the behavioral consequences of chronic stress.

Authors:  Sayamwong E Hammack; Carolyn W Roman; Kimberly R Lezak; Margaret Kocho-Shellenberg; Bethany Grimmig; William A Falls; Karen Braas; Victor May
Journal:  J Mol Neurosci       Date:  2010-04-20       Impact factor: 3.444

Review 6.  Rhythmic control of activity and sleep by class B1 GPCRs.

Authors:  Michael Kunst; Matthew C F Tso; D Dipon Ghosh; Erik D Herzog; Michael N Nitabach
Journal:  Crit Rev Biochem Mol Biol       Date:  2014-11-20       Impact factor: 8.250

Review 7.  Inhibitory effect of PACAP on caspase activity in neuronal apoptosis: a better understanding towards therapeutic applications in neurodegenerative diseases.

Authors:  Agnieszka Dejda; Valérie Jolivel; Steve Bourgault; Tommy Seaborn; Alain Fournier; Hubert Vaudry; David Vaudry
Journal:  J Mol Neurosci       Date:  2008-05-28       Impact factor: 3.444

8.  Agonistic behavior of PACAP6-38 on sensory nerve terminals and cytotrophoblast cells.

Authors:  D Reglodi; R Borzsei; T Bagoly; A Boronkai; B Racz; A Tamas; P Kiss; G Horvath; R Brubel; J Nemeth; G Toth; Z Helyes
Journal:  J Mol Neurosci       Date:  2008-07-08       Impact factor: 3.444

Review 9.  Targeting VIP and PACAP receptor signalling: new therapeutic strategies in multiple sclerosis.

Authors:  Yossan-Var Tan; James A Waschek
Journal:  ASN Neuro       Date:  2011-10-06       Impact factor: 4.146

Review 10.  Pituitary Adenylate Cyclase-Activating Polypeptide in Learning and Memory.

Authors:  Marieke R Gilmartin; Nicole C Ferrara
Journal:  Front Cell Neurosci       Date:  2021-06-22       Impact factor: 6.147
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