Pétigny C, Dumont A-A, Giguère H, Collette A, Holleran BJ, Iftinca M, Altier C, Besserer-Offroy É, Auger-Messier M, Leduc R.
Monitoring TRPC7 Conformational Changes by BRET Following GPCR Activation.
International Journal of Molecular Sciences. 2022; 23(5):2502
PMID: TBD
PubMed PubMed Central Journal Full-text article (PDF)
Tran K, Sainsily X, Côté J, Coquerel D, Couvineau P, Saibi S, Haroune L, Besserer-Offroy É, Flynn-Robitaille J, Resua Rojas M, Murza A, Longpré JM, Auger-Messier M, Lesur O, Bouvier M, Marsault É, Boudreault PL, Sarret P.
Size-Reduced Macrocyclic Analogues of [Pyr1]-apelin-13 Showing Negative Gα12 Bias Still Produce Prolonged Cardiac Effects.
Journal of medicinal chemistry. 2022; 65(1):531-551.
PMID: 34982553
PubMed Journal Free Full-text article (on ACS website)
Michaelian N, Sadybekov A, Besserer-Offroy É, Han GW, Krishnamurthy H, Zamlynny B, Fradera X, Siliphaivanh P, Prestland J, Spencer K, Soisson S, Popov P, Sarret P, Katritch V, Cherezov V.
Structural Insights on Ligand Recognition at the Human Leukotriene B4 Receptor 1.
Nature Communications. 2021; (12):2971
PMID: 34016973
PubMed PubMed Central Journal Full-text article (PDF)
Vivancos M, Fanelli R, Besserer-Offroy É, Beaulieu S, Chartier M, Resua-Rojas M, Mona CE, Previti S, Rémond E, Longpré JM, Cavelier F, Sarret P.
Metabolically stable neurotensin analogs exert potent and long-acting analgesia without hypothermia.
Behavioural Brain Research. 2021; 405:113189
PMID: 33607165
PubMed Journal Free Full-text article (arXiv.org)
Sadybekov AA, Brouillette RL, Marin E, Sadybekov AV, Luginina A, Gusach A, Mishin A, Besserer-Offroy É, Longpré JM, Borshchevskiy V, Cherezov V, Sarret P, Katritch V.
Structure-based virtual screening of ultra-large library yields potent antagonists for a lipid GPCR.
Biomolecules. 2020; 10(12):1634
PMID: 33287369
PubMed PubMed Central Journal Full-text article (PDF)
Besserer-Offroy É*, Brouillette RL, Longpré JM, Sarret P.
Assessing Gαq/15-signaling with IP-One: Single plate transfection and assay protocol for cell-based high-throughput assay.
Bio-Protocol. 2020; 10(16):e3715
PMID: 33659379
*Corresponding Author
PubMed PubMed Central Journal Full-text article (PDF)
Besserer-Offroy É*, Tétreault P*, Brouillette RL, René A, Murza A, Fanelli R, Kirby K, Parent AJ, Dubuc I, Beaudet N, Côté J, Longpré JM, Martinez J, Cavelier F, Sarret P.
Data set describing the in vitro biological activity of JMV2009, a novel silylated neurotensin(8-13) analog.
Data in Brief. 2020; 31C:105884
PMID: 32637491
*Co-First Authors
PubMed PubMed Central Journal Full-text article (PDF)
Besserer-Offroy É*, Tétreault P*, Brouillette RL, René A, Murza A, Fanelli R, Kirby K, Parent AJ, Dubuc I, Beaudet N, Côté J, Longpré JM, Martinez J, Cavelier F, Sarret P.
Pain relief devoid of opioid side effects following central action of a silylated neurotensin analog.
European Journal of Pharmacology. 2020; 882C:173174
PMID: 32534076
*Co-First Authors
PubMed Journal Free Full-text article (arXiv.org)
Besserer-Offroy É*°, Brouillette RL*, Mona CE, Chartier M, Lavenus S, Sousbie M, Belleville K, Longpré JM, Marsault É, Grandbois M, Sarret P°.
Cell-penetrating pepducins targeting the neurotensin receptor type 1 relieve pain.
Pharmacological research. 2020; 155C:104750
PMID: 32151680
*Co-First Authors
°Co-Corresponding Authors
PubMed Journal Free Full-text article (arXiv.org)
Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy É, Longpré JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, B Stauch, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V.
Structural basis of ligand selectivity and disease mutations in cysteinyl leukotriene receptors.
Nature Communications. 2019; (10):5573
PMID: 31811124
PubMed PubMed Central Journal Full-text article (PDF)
Luginina A, Gusach A, Marin E, Mishin A, Brouillette RL, Popov P, Shiriaeva A, Besserer-Offroy É, Longpré JM, Lyapina E, Ishchenko A, Patel N, Polovinkin V, Safronova N, Bogorodskiy A, Edelweiss E, Hu H, Weierstall U, Liu W, Batyuk A, Gordeliy V, Han GW, Sarret P, Katritch V, Borshchevskiy V, Cherezov V.
Structure-Based Mechanism of Cysteinyl Leukotriene Receptor Inhibition by Antiasthmatic Drugs.
Science advances. 2019; 5(10):eaax2518
PMID: 31633023
PubMed PubMed Central Journal Full-text article (PDF)
Boulkeroua C, Ayari H, Khalfaoui T, Lafrance M, Besserer-Offroy É, Ekindi N, Sabbagh R, Dumaine R, Lesur O, Sarret P, Chraibi A.
Apelin-13 Regulates Vasopressin-Induced Aquaporin-2 Expression and Trafficking in Kidney Collecting Duct Cells.
Cellular physiology and biochemistry. 2019; 53(4):687-700
PMID: 31577078
PubMed Journal Full-text article (PDF)
*Besserer-Offroy É, Sarret P.
Sending out Biased Signals: An Appropriate Proposition for Pain?
Douleur et analgésie. 2019; 32(2):108-110.
*Corresponding Author
Journal Full-text article (PDF)
Lavenus S, Simard É, Besserer-Offroy É, Froehlich U, Leduc R, Grandbois M.
Label-free cell signaling pathway deconvolution of angiotensin type 1 receptor reveals time-resolved G-protein activity and distinct AngII and AngIII/IV responses.
Pharmacological research. 2018; 136:108-120.
PMID: 29959993
PubMed Journal Free Full-text article (arXiv.org)
Sousbie M, Vivancos M, Brouillette RL, Besserer-Offroy É, Longpré JM, Leduc R, Sarret P, Marsault É.
Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8-13).
Journal of medicinal chemistry. 2018; 61(16):7103-7115.
PMID: 30035538
PubMed Journal Free Full-text article (on ACS website)
St-Pierre D, Cabana J, Holleran BJ, Besserer-Offroy É, Escher E, Guillemette G, Lavigne P, Leduc R.
Angiotensin II cyclic analogs as tools to investigate AT<sub>1</sub>R biased signaling mechanisms.
Biochemical pharmacology. 2018; 154:104-117.
PMID: 29684376
PubMed Journal Free Full-text article (arXiv.org) Supporting Information
Besserer-Offroy É, Bérubé P, Côté J, Murza A, Longpré JM, Dumaine R, Lesur O, Auger-Messier M, Leduc R, Marsault É, Sarret P.
The hypotensive effect of activated apelin receptor is correlated with β-arrestin recruitment.
Pharmacological research. 2018; 131:7-16.
PMID: 29530600
PubMed Journal Free Full-text article (arXiv.org)
Sousbie M, Besserer-Offroy É, Brouillette RL, Longpré JM, Leduc R, Sarret P, Marsault É.
In Search of the Optimal Macrocyclization Site for Neurotensin.
ACS medicinal chemistry letters. 2018; 9(3):227-232.
PMID: 29541365, PMCID: PMC5846049
PubMed PubMed Central Journal Free Full-text article (on ACS website)
Besserer-Offroy É, Brouillette RL, Lavenus S, Froehlich U, Brumwell A, Murza A, Longpré JM, Marsault É, Grandbois M, Sarret P, Leduc R.
The signaling signature of the neurotensin type 1 receptor with endogenous ligands.
European journal of pharmacology. 2017; 805:1-13.
PMID: 28341345
PubMed Journal Free Full-text article (arXiv.org)
Fanelli R, Floquet N, Besserer-Offroy É, Delort B, Vivancos M, Longpré JM, Renault P, Martinez J, Sarret P, Cavelier F.
Use of Molecular Modeling to Design Selective NTS2 Neurotensin Analogues.
Journal of medicinal chemistry. 2017; 60(8):3303-3313.
PMID: 28368584
PubMed Journal Free Full-text article (on ACS website)
Murza A, Sainsily X, Côté J, Bruneau-Cossette L, Besserer-Offroy É, Longpré JM, Leduc R, Dumaine R, Lesur O, Auger-Messier M, Sarret P, Marsault É.
Structure-activity relationship of novel macrocyclic biased apelin receptor agonists.
Organic & biomolecular chemistry. 2017; 15(2):449-458.
PMID: 27924341
PubMed Journal Full-text article (PDF)
Mona CE, Besserer-Offroy É, Cabana J, Leduc R, Lavigne P, Heveker N, Marsault É, Escher E.
Design, synthesis, and biological evaluation of CXCR4 ligands.
Organic & biomolecular chemistry. 2016; 14(43):10298-10311.
PMID: 27752700
PubMed Journal Full-text article (PDF)
Thomas JB, Vivancos M, Giddings AM, Wiethe RW, Warner KR, Murza A, Besserer-Offroy É, Longpré JM, Runyon SP, Decker AM, Gilmour BP, Sarret P.
Identification of 2-({[1-(4-Fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)tricyclo[3.3.1.13,7]decane-2-carboxylic Acid (NTRC-844) as a Selective Antagonist for the Rat Neurotensin Receptor Type 2.
ACS chemical neuroscience. 2016; 7(9):1225-31.
PMID: 27359371
PubMed Journal Free Full-text article (on ACS website)
Mona CE, Besserer-Offroy É, Cabana J, Lefrançois M, Boulais PE, Lefebvre MR, Leduc R, Lavigne P, Heveker N, Marsault É, Escher E.
Structure-Activity Relationship and Signaling of New Chimeric CXCR4 Agonists.
Journal of medicinal chemistry. 2016; 59(16):7512-24.
PMID: 27434274
PubMed Journal Free Full-text article (on ACS website)
Murza A, Sainsily X, Coquerel D, Côté J, Marx P, Besserer-Offroy É, Longpré JM, Lainé J, Reversade B, Salvail D, Leduc R, Dumaine R, Lesur O, Auger-Messier M, Sarret P, Marsault É.
Discovery and Structure-Activity Relationship of a Bioactive Fragment of ELABELA that Modulates Vascular and Cardiac Functions.
Journal of medicinal chemistry. 2016; 59(7):2962-72.
PMID: 26986036
PubMed Journal Free Full-text article (on ACS website)
Hapău D, Rémond E, Fanelli R, Vivancos M, René A, Côté J, Besserer-Offroy É, Longpré JM, Martinez J, Zaharia V, Sarret P, Cavelier F.
Stereoselective Synthesis of β-(5-Arylthiazolyl) α-Amino Acids and Use in Neurotensin Analogues.
European journal of organic chemistry. 2016; 2016(5):1017-1024.
Journal Full-text article (PDF)
*Besserer-Offroy É, *Fanelli R, René A, Côté J, Tétreault P, Collerette-Tremblay J, Longpré JM, Leduc R, Martinez J, Sarret P, Cavelier F.
Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.
Journal of medicinal chemistry. 2015; 58(19):7785-95.
PMID: 26348111
* Co-First Authors
PubMed Journal Free Full-text article (on ACS website)
Murza A, Besserer-Offroy É, Côté J, Bérubé P, Longpré JM, Dumaine R, Lesur O, Auger-Messier M, Leduc R, Sarret P, Marsault É.
C-Terminal modifications of apelin-13 significantly change ligand binding, receptor signaling, and hypotensive action.
Journal of medicinal chemistry. 2015; 58(5):2431-40.
PMID: 25668242
PubMed Journal Full-text article (PDF)
Demeule M, Beaudet N, Régina A, Besserer-Offroy É, Murza A, Tétreault P, Belleville K, Ché C, Larocque A, Thiot C, Béliveau R, Longpré JM, Marsault É, Leduc R, Lachowicz JE, Gonias SL, Castaigne JP, Sarret P.
Conjugation of a brain-penetrant peptide with neurotensin provides antinociceptive properties.
The Journal of clinical investigation. 2014; 124(3):1199-213.
PMID: 24531547, PMCID: PMC3934173
PubMed PubMed Central Journal Full-text article (PDF)
Murza A, Parent A, Besserer-Offroy É, Tremblay H, Karadereye F, Beaudet N, Leduc R, Sarret P, Marsault É.
Elucidation of the structure-activity relationships of apelin: influence of unnatural amino acids on binding, signaling, and plasma stability.
ChemMedChem. 2012; 7(2):318-25.
PMID: 22170700
Marsault É, Sousbie M, Leduc R, Sarret P, Longpré JM, Besserer-Offroy É, Brouillette R, Desgagné M.
SOCPRA Sciences Santé et Humaines sec.
Macrocyclic compounds and methods of preventing or treating pain.
United States patent application US16/011,118. 2018 June; United States patent 11,591,366. 2023 February.
Google Patents EspaceNet (EPO) Full text (PDF)
Fanelli R, Floquet N, Vivancos M, Delort B, Besserer-Offroy É, Longpré JM, Martinez J, Sarret P, Cavelier F.
NTS1 an NTS2 diversity delineated by molecular modelling drives the synthesis of new selective neurotensin analogues.
34th European Peptide Symposium, Liepzig, Germany; 09/2016
Proceeding Book Full-Text Proceeding (PDF)
Mona C, Lefrançois M, Boulais PE, Besserer-Offroy É, Leduc R, Heveker N, Marsault É, Escher E.
Synthetic Agonists for the CXCR4 Receptor: SAR, Signaling Pathways and Peptidomimetic Transition.
23rd American Peptide Symposium (Peptides Across the Pacific), Waikoloa, Hawai’I, USA; 06/2013
Proceeding Book Full-Text Proceeding (PDF)
Murza A, Parent AJ, Besserer-Offroy É, Beaudet N, Sarret P, Marsault É.
Elucidation of the structure-activity relationships of Apelin: Influence of unnatural amino acids on binding, signaling and plasma stability.
32nd European Peptide Symposium, Athens, Greece; 09/2012
Proceeding Book Full-Text Proceeding (PDF)