Literature DB >> 31038950

Substituted Pyridazin-3(2 H)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists.

Girdhar Singh Deora1, Cheng Xue Qin2,3, Elizabeth A Vecchio2, Aaron J Debono1, Daniel L Priebbenow1, Ryan M Brady1, Julia Beveridge1, Silvia C Teguh1, Minh Deo2, Lauren T May4, Guy Krippner2, Rebecca H Ritchie2,3,5, Jonathan B Baell6,1,7.   

Abstract

Herein we describe the development of a focused series of functionalized pyridazin-3(2 H)-one-based formyl peptide receptor (FPR) agonists that demonstrate high potency and biased agonism. The compounds described demonstrated biased activation of prosurvival signaling, ERK1/2 phosphorylation, through diminution of the detrimental FPR1/2-mediated intracellular calcium (Cai2+) mobilization. Compound 50 showed an EC50 of 0.083 μM for phosphorylation of ERK1/2 and an approximate 20-fold bias away from Cai2+ mobilization at the hFPR1.

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Year:  2019        PMID： 31038950     DOI： 10.1021/acs.jmedchem.8b01912

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  5 in total

1.  Pyridazinones and Structurally Related Derivatives with Anti-Inflammatory Activity.

Authors:  Niccolo Cantini; Igor A Schepetkin; Nadezhda V Danilenko; Andrei I Khlebnikov; Letizia Crocetti; Maria Paola Giovannoni; Liliya N Kirpotina; Mark T Quinn
Journal:  Molecules       Date:  2022-06-10       Impact factor: 4.927

2.  Molecular Mechanisms of Class B GPCR Activation: Insights from Adrenomedullin Receptors.

Authors:  Michael L Garelja; Maggie Au; Margaret A Brimble; Joseph J Gingell; Erica R Hendrikse; Annie Lovell; Nicole Prodan; Patrick M Sexton; Andrew Siow; Christopher S Walker; Harriet A Watkins; Geoffrey M Williams; Denise Wootten; Sung H Yang; Paul W R Harris; Debbie L Hay
Journal:  ACS Pharmacol Transl Sci       Date:  2020-02-26

3.  Hit Identification of New Potent PqsR Antagonists as Inhibitors of Quorum Sensing in Planktonic and Biofilm Grown Pseudomonas aeruginosa.

Authors:  Fadi Soukarieh; Ruiling Liu; Manuel Romero; Shaun N Roberston; William Richardson; Simone Lucanto; Eduard Vico Oton; Naim Ruhul Qudus; Alaa Mashabi; Scott Grossman; Sadiqur Ali; Tomás Sou; Irena Kukavica-Ibrulj; Roger C Levesque; Christel A S Bergström; Nigel Halliday; Shailesh N Mistry; Jonas Emsley; Stephan Heeb; Paul Williams; Miguel Cámara; Michael J Stocks
Journal:  Front Chem       Date:  2020-05-04       Impact factor: 5.221

Review 4.  Formylpeptide receptor 2: Nomenclature, structure, signalling and translational perspectives: IUPHAR review 35.

Authors:  Cheng Xue Qin; Lucy V Norling; Elizabeth A Vecchio; Eoin P Brennan; Lauren T May; Denise Wootten; Catherine Godson; Mauro Perretti; Rebecca H Ritchie
Journal:  Br J Pharmacol       Date:  2022-07-29       Impact factor: 9.473

5.  Antibiotic-chemoattractants enhance neutrophil clearance of Staphylococcus aureus.

Authors:  Jennifer A E Payne; Julien Tailhades; Felix Ellett; Xenia Kostoulias; Alex J Fulcher; Ting Fu; Ryan Leung; Stephanie Louch; Amy Tran; Severin A Weber; Ralf B Schittenhelm; Graham J Lieschke; Chengxue Helena Qin; Daniel Irima; Anton Y Peleg; Max J Cryle
Journal:  Nat Commun       Date:  2021-10-25       Impact factor: 14.919
  5 in total

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