Home »

Peer-reviewed publications

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   Journal    PubMedCentral    Full-Text Article


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   Journal    PubMedCentral    Full-Text Article


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    Journal    PubMedCentral    Full-Text Article


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    Journal    PubMedCentral    Full-Text Article


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    Journal    PubMedCentral    Full-Text Article


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    Journal    PubMedCentral    Full-Text Article


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


*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    Free Full-Text Article (arXiv.org)


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 (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    Journal   Free Full-Text Article (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 (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


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


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 (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 (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 (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


*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 (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


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    Journal    Full-text article


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

PubMed    Journal    Full-text article

Follow us on Twitter

Excited to share work by Kai Song, the Graeber lab & collaborators, interrogating the interplay of BRAF focal amplification modes (extrachromosomal DNA (#ecDNA) & homogenously staining regions (#HSR)) in the context of MAPK inhibitor #cancer regiments. https://bit.ly/2ZqHWrK 1/2

Ga-68 FAPi imaging reflects tissue FAP expression: Emergence of a new pan-cancer biomarker? http://ow.ly/MoAx50GICuq

#PrecisionMedicine #PETCT #Cancer

Load More...