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322 results


Publications — IRIC July 2, 2022

Michaelis-Menten quantification of ligand signalling bias applied to the promiscuous Vasopressin V2 receptor.

Heydenreich FM, Plouffe B, Rizk A, Milic D, Zhou J, Breton B, Le Gouill C, Inoue A, Bouvier M, Veprintsev D
Mol Pharmacol 2022-07-02 ;.


Publications — IRIC July 1, 2022

Community guidelines for GPCR ligand bias: IUPHAR review 32.

Kolb P, Kenakin T, Alexander SPH, Bermudez M, Bohn LM, Breinholt CS, Bouvier M, Hill SJ, Kostenis E, Martemyanov KA, Neubig RR, Onaran HO, Rajagopal S, Roth BL, Selent J, Shukla AK, Sommer ME, Gloriam DE
Br J Pharmacol 2022-07-01 ;179( 14 ):3651-3674.


Publications — IRIC June 26, 2022

New oral protease-activated receptor 4 antagonist BMS-986120: tolerability, pharmacokinetics, pharmacodynamics, and gene variant effects in humans.

Merali S, Wang Z, Frost C, Callejo M, Hedrick M, Hui L, Meadows Shropshire S, Xu K, Bouvier M, DeSouza MM, Yang J
Platelets 2022-06-26 ;1-10.


Publications — IRIC June 21, 2022

Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.

Priestley ES, Banville J, Deon D, Dubé L, Gagnon M, Guy J, Lapointe P, Lavallée JF, Martel A, Plamondon S, Rémillard R, Ruediger E, Tremblay F, Posy SL, Guarino VR, Richter JM, Li J, Gupta A, Vetrichelvan M, Balapragalathan TJ, Mathur A, Hua J, Callejo M, Guay J, Sum CS, Cvijic ME, Watson C, Wong P, Yang J, Bouvier M, Gordon DA, Wexler RR, Marinier A
J Med Chem 2022-06-21 ;.


Publications — IRIC June 6, 2022

Interphase microtubule disassembly is a signaling cue that drives cell rounding at mitotic entry.

Leguay K, Decelle B, Elkholi IE, Bouvier M, Côté JF, Carréno S
J Cell Biol 2022-06-06 ;221( 6 )::e202109065.


Publications — IRIC May 10, 2022

The pocketome of G-protein-coupled receptors reveals previously untargeted allosteric sites.

Hedderich JB, Persechino M, Becker K, Heydenreich FM, Gutermuth T, Bouvier M, Bünemann M, Kolb P
Nat Commun 2022-05-10 ;13( 1 ):2567.


Publications — IRIC March 18, 2022

Common coupling map advances GPCR-G protein selectivity.

Hauser AS, Avet C, Normand C, Mancini A, Inoue A, Bouvier M, Gloriam DE
Elife 2022-03-18 ;11:e74107.


Publications — IRIC March 18, 2022

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

Avet C, Mancini A, Breton B, Le Gouill C, Hauser AS, Normand C, Kobayashi H, Gross F, Hogue M, Lukasheva V, St-Onge S, Carrier M, Héroux M, Morissette S, Fauman EB, Fortin JP, Schann S, Leroy X, Gloriam DE, Bouvier M
Elife 2022-03-18 ;11:e74101.


Publications — IRIC January 13, 2022

Size-Reduced Macrocyclic Analogues of [Pyr1]-apelin-13 Showing Negative Gα12 Bias Still Produce Prolonged Cardiac Effects.

Tran K, Sainsily X, Côté J, Coquerel D, Couvineau P, Saibi S, Haroune L, Besserer-Offroy E, Flynn-Robitaille J, Resua Rojas M, Murza A, Longpré JM, Auger-Messier M, Lesur O, Bouvier M, Marsault E, Boudreault PL, Sarret P
J Med Chem 2022-01-13 ;65( 1 ):531-551.


Publications — IRIC January 1, 2022

Angiotensin II Type 1 Receptor Tachyphylaxis Is Defined by Agonist Residence Time.

Duarte DA, Parreiras-E-Silva LT, Oliveira EB, Bouvier M, Costa-Neto CM
Hypertension 2022-01-01 ;79( 1 ):115-125.


Publications — IRIC December 1, 2021

Cryo-EM structure of constitutively active human Frizzled 7 in complex with heterotrimeric Gs.

Xu L, Chen B, Schihada H, Wright SC, Turku A, Wu Y, Han GW, Kowalski-Jahn M, Kozielewicz P, Bowin CF, Zhang X, Li C, Bouvier M, Schulte G, Xu F
Cell Res 2021-12-01 ;31( 12 ):1311-1314.


Publications — IRIC November 1, 2021

GPCR activation mechanisms across classes and macro/microscales.

Hauser AS, Kooistra AJ, Munk C, Heydenreich FM, Veprintsev DB, Bouvier M, Babu MM, Gloriam DE
Nat Struct Mol Biol 2021-11-01 ;28( 11 ):879-888.


Publications — IRIC October 8, 2021

Comprehensive Signaling Profiles Reveal Unsuspected Functional Selectivity of δ-Opioid Receptor Agonists and Allow the Identification of Ligands with the Greatest Potential for Inducing Cyclase Superactivation.

Mansour A, Nagi K, Dallaire P, Lukasheva V, Le Gouill C, Bouvier M, Pineyro G
ACS Pharmacol Transl Sci 2021-10-08 ;4( 5 ):1483-1498.


Publications — IRIC October 8, 2021

Identification of Key Regions Mediating Human Melatonin Type 1 Receptor Functional Selectivity Revealed by Natural Variants.

Hegron A, Huh E, Deupi X, Sokrat B, Gao W, Le Gouill C, Canouil M, Boissel M, Charpentier G, Roussel R, Balkau B, Froguel P, Plouffe B, Bonnefond A, Lichtarge O, Jockers R, Bouvier M
ACS Pharmacol Transl Sci 2021-10-08 ;4( 5 ):1614-1627.


Publications — IRIC September 28, 2021

Ackr3-Venus knock-in mouse lights up brain vasculature.

Ehrlich AT, Semache M, Couvineau P, Wojcik S, Kobayashi H, Thelen M, Gross F, Hogue M, Le Gouill C, Darcq E, Bouvier M, Kieffer BL
Mol Brain 2021-09-28 ;14( 1 ):151.


Publications — IRIC September 10, 2021

Bivalent ligands promote endosomal trafficking of the dopamine D3 receptor-neurotensin receptor 1 heterodimer.

Budzinski J, Maschauer S, Kobayashi H, Couvineau P, Vogt H, Gmeiner P, Roggenhofer A, Prante O, Bouvier M, Weikert D
Commun Biol 2021-09-10 ;4( 1 ):1062.


Publications — IRIC August 25, 2021

Mechanistic insights into dopaminergic and serotonergic neurotransmission - concerted interactions with helices 5 and 6 drive the functional outcome.

Stepniewski TM, Mancini A, Ågren R, Torrens-Fontanals M, Semache M, Bouvier M, Sahlholm K, Breton B, Selent J
Chem Sci 2021-08-25 ;12( 33 ):10990-11003.


Publications — IRIC August 7, 2021

Identifying Plasmodium falciparum receptor activation using bioluminescence resonance energy transfer (BRET)-based biosensors in HEK293 cells.

Pereira PHS, Garcia CRS, Bouvier M
Methods Cell Biol 2021-08-07 ;166:223-233.


Publications — IRIC August 3, 2021

Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen.

Giubilaro J, Schuetz DA, Stepniewski TM, Namkung Y, Khoury E, Lara-Márquez M, Campbell S, Beautrait A, Armando S, Radresa O, Duchaine J, Lamarche-Vane N, Claing A, Selent J, Bouvier M, Marinier A, Laporte SA
Nat Commun 2021-08-03 ;12( 1 ):4688.


Publications — IRIC August 1, 2021

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

García RA, Lupisella JA, Ito BR, Hsu MY, Fernando G, Carson NL, Allocco JJ, Ryan CS, Zhang R, Wang Z, Heroux M, Carrier M, St-Onge S, Bouvier M, Dudhgaonkar S, Nagar J, Bustamante-Pozo MM, Garate-Carrillo A, Chen J, Ma X, Search DJ, Dierks EA, Kick EK, Wexler RR, Gordon DA, Ostrowski J, Wurtz NR, Villarreal F
JACC Basic Transl Sci 2021-08-01 ;6( 8 ):676-689.


Publications — IRIC June 15, 2021

Extracellular succinate hyperpolarizes M2 macrophages through SUCNR1/GPR91-mediated Gq signaling.

Trauelsen M, Hiron TK, Lin D, Petersen JE, Breton B, Husted AS, Hjorth SA, Inoue A, Frimurer TM, Bouvier M, O'Callaghan CA, Schwartz TW
Cell Rep 2021-06-15 ;35( 11 ):109246.


Publications — IRIC May 29, 2021

Bioluminescence Resonance Energy Transfer (BRET) Imaging in Living Cells: Image Acquisition and Quantification.

Kobayashi H, Bouvier M
Methods Mol Biol 2021-05-29 ;2274:305-314.


Publications — IRIC May 25, 2021

Illuminating the complexity of GPCR pathway selectivity - advances in biosensor development.

Wright SC, Bouvier M
Curr Opin Struct Biol 2021-05-25 ;69:142-149.


Publications — IRIC May 18, 2021

BRET-based effector membrane translocation assay monitors GPCR-promoted and endocytosis-mediated Gq activation at early endosomes.

Wright SC, Lukasheva V, Le Gouill C, Kobayashi H, Breton B, Mailhot-Larouche S, Blondel-Tepaz E, Antunes Vieira N, Costa-Neto C, Héroux M, Lambert NA, Parreiras-E-Silva LT, Bouvier M
Proc Natl Acad Sci U S A 2021-05-18 ;118( 20 ):.


Publications — IRIC May 13, 2021

Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.

Trân K, Van Den Hauwe R, Sainsily X, Couvineau P, Côté J, Simard L, Echevarria M, Murza A, Serre A, Théroux L, Saibi S, Haroune L, Longpré JM, Lesur O, Auger-Messier M, Spino C, Bouvier M, Sarret P, Ballet S, Marsault E
J Med Chem 2021-05-13 ;64( 9 ):5345-5364.


Publications — IRIC April 9, 2021

Proadrenomedullin N-Terminal 20 Peptides (PAMPs) Are Agonists of the Chemokine Scavenger Receptor ACKR3/CXCR7.

Meyrath M, Palmer CB, Reynders N, Vanderplasschen A, Ollert M, Bouvier M, Szpakowska M, Chevigné A
ACS Pharmacol Transl Sci 2021-04-09 ;4( 2 ):813-823.


Publications — IRIC April 1, 2021

Development of conformational BRET biosensors that monitor ezrin, radixin and moesin activation in real time.

Leguay K, Decelle B, He YY, Pagniez A, Hogue M, Kobayashi H, Le Gouill C, Bouvier M, Carréno S
J Cell Sci 2021-04-01 ;134( 7 ):.


Publications — IRIC March 23, 2021

Human MC4R variants affect endocytosis, trafficking and dimerization revealing multiple cellular mechanisms involved in weight regulation.

Brouwers B, de Oliveira EM, Marti-Solano M, Monteiro FBF, Laurin SA, Keogh JM, Henning E, Bounds R, Daly CA, Houston S, Ayinampudi V, Wasiluk N, Clarke D, Plouffe B, Bouvier M, Babu MM, Farooqi IS, Mokrosiński J
Cell Rep 2021-03-23 ;34( 12 ):108862.


Publications — IRIC March 9, 2021

Selective release of gastrointestinal hormones induced by an orally active GPR39 agonist.

Grunddal KV, Diep TA, Petersen N, Tough IR, Skov LJ, Liu L, Buijink JA, Mende F, Jin C, Jepsen SL, Sørensen LME, Achiam MP, Strandby RB, Bach A, Hartmann B, Frimurer TM, Hjorth SA, Bouvier M, Cox H, Holst B
Mol Metab 2021-03-09 ;101207.


Publications — IRIC March 1, 2021

In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure.

Gargalovic P, Wong P, Onorato J, Finlay H, Wang T, Yan M, Crain E, St-Onge S, Héroux M, Bouvier M, Xu C, Chen XQ, Generaux C, Lawrence M, Wexler R, Gordon D
Circ Heart Fail 2021-03-01 ;14( 3 ):e007351.


Publications — IRIC March 1, 2021

The RanBP2/RanGAP1-SUMO complex gates β-arrestin2 nuclear entry to regulate the Mdm2-p53 signaling axis.

Blondel-Tepaz E, Leverve M, Sokrat B, Paradis JS, Kosic M, Saha K, Auffray C, Lima-Fernandes E, Zamborlini A, Poupon A, Gaboury L, Findlay J, Baillie GS, Enslen H, Bouvier M, Angers S, Marullo S, Scott MGH
Oncogene 2021-03-01 ;40( 12 ):2243-2257.


Publications — IRIC February 22, 2021

Pharmacological chaperone action in humanized mouse models of MC4R-linked obesity.

René P, Lanfray D, Richard D, Bouvier M
JCI Insight 2021-02-22 ;6( 4 ):.


Publications — IRIC February 17, 2021

Feedback control of the Gpr161-Gαs-PKA axis contributes to basal Hedgehog repression in zebrafish.

Tschaikner PM, Regele D, Röck R, Salvenmoser W, Meyer D, Bouvier M, Geley S, Stefan E, Aanstad P
Development 2021-02-17 ;148( 4 ):.


Publications — IRIC January 14, 2021

Structure-Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor.

Trân K, Murza A, Sainsily X, Delile E, Couvineau P, Côté J, Coquerel D, Peloquin M, Auger-Messier M, Bouvier M, Lesur O, Sarret P, Marsault E
J Med Chem 2021-01-14 ;64( 1 ):602-615.


Publications — IRIC December 23, 2020

How GPCR Phosphorylation Patterns Orchestrate Arrestin-Mediated Signaling.

Latorraca NR, Masureel M, Hollingsworth SA, Heydenreich FM, Suomivuori CM, Brinton C, Townshend RJL, Bouvier M, Kobilka BK, Dror RO
Cell 2020-12-23 ;183( 7 ):1813-1825.e18.


Publications — IRIC December 22, 2020

Signal Transduction Profiling of Angiotensin II Type 1 Receptor With Mutations Associated to Atrial Fibrillation in Humans.

Simões SC, Balico-Silva AL, Parreiras-E-Silva LT, Bitencourt ALB, Bouvier M, Costa-Neto CM
Front Pharmacol 2020-12-22 ;11:600132.


Publications — IRIC December 8, 2020

Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands - Functional characterization and modeling studies on H3 and H4 receptors.

Corrêa MF, Balico-Silva AL, Kiss DJ, Fernandes GAB, Maraschin JC, Parreiras-E-Silva LT, Varela MT, Simões SC, Bouvier M, Keserű GM, Costa-Neto CM, Fernandes JPS
Bioorg Med Chem 2020-12-08 ;30:115924.


Publications — IRIC December 1, 2020

Barbadin selectively modulates FPR2-mediated neutrophil functions independent of receptor endocytosis.

Sundqvist M, Holdfeldt A, Wright SC, Møller TC, Siaw E, Jennbacken K, Franzyk H, Bouvier M, Dahlgren C, Forsman H
Biochim Biophys Acta Mol Cell Res 2020-12-01 ;1867( 12 ):118849.


Publications — IRIC December 1, 2020

Beta-arrestins operate an on/off control switch for focal adhesion kinase activity.

Alexander RA, Lot I, Saha K, Abadie G, Lambert M, Decosta E, Kobayashi H, Beautrait A, Borrull A, Asnacios A, Bouvier M, Scott MGH, Marullo S, Enslen H
Cell Mol Life Sci 2020-12-01 ;77( 24 ):5259-5279.


Publications — IRIC November 27, 2020

The PAR2 inhibitor I-287 selectively targets Gαq and Gα12/13 signaling and has anti-inflammatory effects.

Avet C, Sturino C, Grastilleur S, Le Gouill C, Semache M, Gross F, Gendron L, Bennani Y, Mancini JA, Sayegh CE, Bouvier M
Commun Biol 2020-11-27 ;3( 1 ):719.


Publications — IRIC October 15, 2020

Dissecting the roles of GRK2 and GRK3 in μ-opioid receptor internalization and β-arrestin2 recruitment using CRISPR/Cas9-edited HEK293 cells.

Møller TC, Pedersen MF, van Senten JR, Seiersen SD, Mathiesen JM, Bouvier M, Bräuner-Osborne H
Sci Rep 2020-10-15 ;10( 1 ):17395.


Publications — IRIC October 9, 2020

Circadian, Sleep and Caloric Intake Phenotyping in Type 2 Diabetes Patients With Rare Melatonin Receptor 2 Mutations and Controls: A Pilot Study.

Imam A, Winnebeck EC, Buchholz N, Froguel P, Bonnefond A, Solimena M, Ivanova A, Bouvier M, Plouffe B, Charpentier G, Karamitri A, Jockers R, Roenneberg T, Vetter C
Front Physiol 2020-10-09 ;11:564140.


Publications — IRIC September 1, 2020

Agonist-induced formation of unproductive receptor-G12 complexes.

Okashah N, Wright SC, Kawakami K, Mathiasen S, Zhou J, Lu S, Javitch JA, Inoue A, Bouvier M, Lambert NA
Proc Natl Acad Sci U S A 2020-09-01 ;117( 35 ):21723-21730.


Publications — IRIC July 24, 2020

Genetically encoded intrabody sensors report the interaction and trafficking of β-arrestin 1 upon activation of G-protein-coupled receptors.

Baidya M, Kumari P, Dwivedi-Agnihotri H, Pandey S, Sokrat B, Sposini S, Chaturvedi M, Srivastava A, Roy D, Hanyaloglu AC, Bouvier M, Shukla AK
J. Biol. Chem. 2020-07-24 ;295( 30 ):10153-10167.


Publications — IRIC May 29, 2020

Signal profiling of the β1AR reveals coupling to novel signalling pathways and distinct phenotypic responses mediated by β1AR and β2AR.

Lukasheva V, Devost D, Le Gouill C, Namkung Y, Martin RD, Longpré JM, Amraei M, Shinjo Y, Hogue M, Lagacé M, Breton B, Aoki J, Tanny JC, Laporte SA, Pineyro G, Inoue A, Bouvier M, Hébert TE
Sci Rep 2020-05-29 ;10( 1 ):8779.


Publications — IRIC May 19, 2020

NF45 and NF90 Regulate Mitotic Gene Expression by Competing with Staufen-Mediated mRNA Decay.

Nourreddine S, Lavoie G, Paradis J, Ben El Kadhi K, Méant A, Aubert L, Grondin B, Gendron P, Chabot B, Bouvier M, Carréno S, Roux PP
Cell Rep 2020-05-19 ;31( 7 ):107660.


Publications — IRIC April 9, 2020

Structural Insight into G Protein-Coupled Receptor Signaling Efficacy and Bias between Gs and β-Arrestin.

Picard LP, Schonegge AM, Bouvier M
ACS Pharmacol Transl Sci 2020-04-09 ;2( 3 ):148-154.


Publications — IRIC January 9, 2020

Preservation of Post-Infarction Cardiac Structure and Function via Long-Term Oral Formyl Peptide Receptor Agonist Treatment.

García RA, Ito BR, Lupisella JA, Carson NA, Hsu MY, Fernando G, Heroux M, Bouvier M, Dierks E, Kick EK, Gordon DA, Chen J, Mintier G, Carrier M, St-Onge S, Shah H, Towne J, Bucardo MS, Ma X, Ryan CS, Wurtz NR, Ostrowski J, Villarreal FJ
JACC Basic Transl Sci 2020-01-09 ;4( 8 ):905-920.


Publications — IRIC September 9, 2019

Exploring use of unsupervised clustering to associate signaling profiles of GPCR ligands to clinical response.

Benredjem B, Gallion J, Pelletier D, Dallaire P, Charbonneau J, Cawkill D, Nagi K, Gosink M, Lukasheva V, Jenkinson S, Ren Y, Somps C, Murat B, Van Der Westhuizen E, Le Gouill C, Lichtarge O, Schmidt A, Bouvier M, Pineyro G
Nat Commun 2019-09-09 ;10( 1 ):4075.


Publications — IRIC August 22, 2019

Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.

Miller MM, Banville J, Friends TJ, Gagnon M, Hangeland JJ, Lavallée JF, Martel A, O'Grady H, Rémillard R, Ruediger E, Tremblay F, Posy SL, Allegretto NJ, Guarino VR, Harden DG, Harper TW, Hartl K, Josephs J, Malmstrom S, Watson C, Yang Y, Zhang G, Wong P, Yang J, Bouvier M, Seiffert DA, Wexler RR, Lawrence RM, Priestley ES, Marinier A
J. Med. Chem. 2019-08-22 ;62( 16 ):7400-7416.

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