330 results
The AF-2 cofactor binding region is key for the selective SUMOylation of estrogen receptor alpha by antiestrogens.
Vallet A, El Ezzy M, Diennet M, Haidar S, Bouvier M, Mader S
J Biol Chem
2023-01-01
;299(
1
):102757.
Visualization of real-time receptor endocytosis in dopamine neurons enabled by NTSR1-Venus knock-in mice.
Ehrlich AT, Couvineau P, Schamiloglu S, Wojcik S, Da Fonte D, Mezni A, von Zastrow M, Bender KJ, Bouvier M, Kieffer BL
Front Cell Neurosci
2022-11-29
;16:1076599.
The adhesion G-protein-coupled receptor Gpr116 is essential to maintain the skeletal muscle stem cell pool.
Sénéchal C, Fujita R, Jamet S, Maiga A, Dort J, Orfi Z, Dumont NA, Bouvier M, Crist C
Cell Rep
2022-11-15
;41(
7
):111645.
Computationally designed GPCR quaternary structures bias signaling pathway activation.
Paradis JS, Feng X, Murat B, Jefferson RE, Sokrat B, Szpakowska M, Hogue M, Bergkamp ND, Heydenreich FM, Smit MJ, Chevigné A, Bouvier M, Barth P
Nat Commun
2022-11-11
;13(
1
):6826.
Molecular Mechanisms of Desensitization Underlying the Differential Effects of Formyl Peptide Receptor 2 Agonists on Cardiac Structure-Function Post Myocardial Infarction.
Lupisella J, St-Onge S, Carrier M, Cook EM, Wang T, Sum C, Fernando G, Apgar K, Zhang R, Carson N, Snyder BJ, Ryan CS, Ma X, Dierks EA, Little S, Kick EK, Wurtz NR, Bouvier M, Héroux M, Garcia RA
ACS Pharmacol Transl Sci
2022-10-14
;5(
10
):892-906.
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
2022-10-03
;33(
7
):969-978.
Structure-based discovery of nonopioid analgesics acting through the α2A-adrenergic receptor.
Fink EA, Xu J, Hübner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P
Science
2022-09-30
;377(
6614
):eabn7065.
From a Cone Snail Toxin to a Competitive MC4R Antagonist.
Reynaud S, Laurin SA, Ciolek J, Barbe P, Van Baelen AC, Susset M, Blondel F, Ghazarian M, Boeri J, Vanden Driessche M, Upert G, Mourier G, Kessler P, Konnert L, Beroud R, Keck M, Servent D, Bouvier M, Gilles N
J Med Chem
2022-09-22
;65(
18
):12084-12094.
Michaelis-Menten Quantification of Ligand Signaling Bias Applied to the Promiscuous Vasopressin V2 Receptor.
Heydenreich FM, Plouffe B, Rizk A, Milić D, Zhou J, Breton B, Le Gouill C, Inoue A, Bouvier M, Veprintsev DB
Mol Pharmacol
2022-09-01
;102(
3
):139-149.
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
2022-07-14
;65(
13
):8843-8854.
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.
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.
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.
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.
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.
Structural Elements Directing G Proteins and β-Arrestin Interactions with the Human Melatonin Type 2 Receptor Revealed by Natural Variants.
Plouffe B, Karamitri A, Flock T, Gallion JM, Houston S, Daly CA, Bonnefond A, Guillaume JL, Le Gouill C, Froguel P, Lichtarge O, Deupi X, Jockers R, Bouvier M
ACS Pharmacol Transl Sci
2022-02-11
;5(
2
):89-101.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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
):.
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.
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.
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
):.
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.
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.
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.
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.
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
):.
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
):.
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.
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.
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.
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.
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.
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.
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.
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.
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.