Molecular Mechanisms of Desensitization Underlying the Differential Effects of Formyl Peptide Receptor 2 Agonists on Cardiac Structure-Function Post Myocardial Infarction

Autor: John Lupisella, Stéphane St-Onge, Marilyn Carrier, Erica M. Cook, Tao Wang, Chi Sum, Gayani Fernando, Kendra Apgar, Rongan Zhang, Nancy Carson, Bradley J. Snyder, Carol S. Ryan, Xiuying Ma, Elizabeth A. Dierks, Sean Little, Ellen K. Kick, Nicholas R. Wurtz, Michel Bouvier, Madeleine Héroux, Ricardo A. Garcia

Publikováno v: ACS pharmacologytranslational science. 5(10)

Formyl peptide receptor 2 (FPR2) plays an integral role in the transition of macrophages from a pro-inflammatory program to one that is pro-resolving. FPR2-mediated stimulation of resolution post myocardial infarction has demonstrated efficacy in rod

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2b88f9437b178647894ccc435a7eb5d
https://pubmed.ncbi.nlm.nih.gov/36268126

Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs

Autor: Madeleine Héroux, Hiroyuki Kobayashi, Christian Le Gouill, Arturo Mancini, Stephan Schann, Alexander S. Hauser, Stéphane St-Onge, Florence Gross, Marilyn Carrier, David E. Gloriam, Billy Breton, Sandra Morissette, Charlotte Avet, Viktoriya Lukasheva, Michel Bouvier, Claire Normand, Jean-Philippe Fortin, Eric B. Fauman, Mireille Hogue, Xavier Leroy

Publikováno v: Avet, C, Mancini, A, Breton, B, Le Gouill, C, Hauser, A S, Normand, C, Kobayashi, H, Gross, F, Hogue, M, Lukasheva, V, St-Onge, S, Carrier, M, Héroux, M, Morissette, S, Fauman, E B, Fortin, J P, Schann, S, Leroy, X, Gloriam, D E & Bouvier, M 2022, ' Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs ', eLife, vol. 11, e74101 . https://doi.org/10.7554/eLife.74101

The recognition that individual GPCRs can activate multiple signaling pathways has raised the possibility of developing drugs selectively targeting therapeutically relevant ones. This requires tools to determine which G proteins and βarrestins are a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::501df337f957ca6da7e698ba9197d354
https://curis.ku.dk/ws/files/305174048/elife_74101_v2.pdf

BRET-based effector membrane translocation assay monitors GPCR-promoted and endocytosis-mediated G

Autor: Shane C, Wright, Viktoriya, Lukasheva, Christian, Le Gouill, Hiroyuki, Kobayashi, Billy, Breton, Samuel, Mailhot-Larouche, Élodie, Blondel-Tepaz, Nichelle, Antunes Vieira, Claudio, Costa-Neto, Madeleine, Héroux, Nevin A, Lambert, Lucas Tabajara, Parreiras-E-Silva, Michel, Bouvier

Publikováno v: Proc Natl Acad Sci U S A

G protein–coupled receptors (GPCRs) are gatekeepers of cellular homeostasis and the targets of a large proportion of drugs. In addition to their signaling activity at the plasma membrane, it has been proposed that their actions may result from tran

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::2e6a24d2a9311fd3b8b2179d3c031b4b
https://pubmed.ncbi.nlm.nih.gov/33990469

Selective FPR2 Agonism Promotes a Proresolution Macrophage Phenotype and Improves Cardiac Structure-Function Post Myocardial Infarction

Autor: Moises Muratt Bustamante-Pozo, Rongan Zhang, Nancy L. Carson, Madeleine Héroux, Michel Bouvier, Jian Chen, David A. Gordon, Bruce R. Ito, Stéphane St.-Onge, Gayani Fernando, Marilyn Carrier, Francisco Villarreal, Zhaoqing Wang, Alejandra Garate-Carrillo, Carol S. Ryan, Jignesh Nagar, Jacek Ostrowski, John A. Lupisella, Ricardo Garcia, Shailesh Dudhgaonkar, Debra Search, Ellen K. Kick, Xiuying Ma, Ruth R. Wexler, Mei-Yin Hsu, Elizabeth A. Dierks, Nicholas R. Wurtz, John Allocco

Publikováno v: JACC: Basic to Translational Science

Visual Abstract
Highlights • MI leads to ischemic damage of myocardium and activation of inflammatory programs as part of the wound healing response. • Selective activation of FPR2 on macrophages potentiates key cellular activities that enab

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::23e8893e04bab7931d672cda68a46242
https://pubmed.ncbi.nlm.nih.gov/34466754

Tetrahydroisoquinoline CXCR4 Antagonists Adopt a Hybrid Binding Mode within the Peptide Subpocket of the CXCR4 Receptor

Autor: Yong Zhang, Madeleine Héroux, Bryan Cox, Brooke M Katzman, Brigitte Murat, Lawrence J. Wilson, Anthony R. Prosser, Ana A. Alcaraz, Dennis C. Liotta, Andrew J. Tebben, Gretchen M. Schroeder, James P. Snyder

[Image: see text] The rationale for the structural and mechanistic basis of a tetrahydroisoquinoline (THIQ) based series of CXCR4 antagonists is presented. Using the previously reported crystal structures which reveal two distinct binding sites of CX

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed94921ea08225465c7be2c6bdcf6758
https://europepmc.org/articles/PMC6331156/