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Biased antagonism of CXCR4 avoids antagonist tolerance.
Hitchinson B, Eby JM, Gao X, Guite-Vinet F, Ziarek JJ, Abdelkarim H, Lee Y, Okamoto Y, Shikano S, Majetschak M, Heveker N, Volkman BF, Tarasova NI, Gaponenko V. Hitchinson B, et al. Among authors: heveker n. Sci Signal. 2018 Oct 16;11(552):eaat2214. doi: 10.1126/scisignal.aat2214. Sci Signal. 2018. PMID: 30327409 Free PMC article.
Structural basis for chemokine recognition by a G protein-coupled receptor and implications for receptor activation.
Ziarek JJ, Kleist AB, London N, Raveh B, Montpas N, Bonneterre J, St-Onge G, DiCosmo-Ponticello CJ, Koplinski CA, Roy I, Stephens B, Thelen S, Veldkamp CT, Coffman FD, Cohen MC, Dwinell MB, Thelen M, Peterson FC, Heveker N, Volkman BF. Ziarek JJ, et al. Among authors: heveker n. Sci Signal. 2017 Mar 21;10(471):eaah5756. doi: 10.1126/scisignal.aah5756. Sci Signal. 2017. PMID: 28325822 Free PMC article.
Different contributions of chemokine N-terminal features attest to a different ligand binding mode and a bias towards activation of ACKR3/CXCR7 compared with CXCR4 and CXCR3.
Szpakowska M, Nevins AM, Meyrath M, Rhainds D, D'huys T, Guité-Vinet F, Dupuis N, Gauthier PA, Counson M, Kleist A, St-Onge G, Hanson J, Schols D, Volkman BF, Heveker N, Chevigné A. Szpakowska M, et al. Among authors: heveker n. Br J Pharmacol. 2018 May;175(9):1419-1438. doi: 10.1111/bph.14132. Epub 2018 Mar 23. Br J Pharmacol. 2018. PMID: 29272550 Free PMC article.
AMD3100 is a CXCR7 ligand with allosteric agonist properties.
Kalatskaya I, Berchiche YA, Gravel S, Limberg BJ, Rosenbaum JS, Heveker N. Kalatskaya I, et al. Among authors: heveker n. Mol Pharmacol. 2009 May;75(5):1240-7. doi: 10.1124/mol.108.053389. Epub 2009 Mar 2. Mol Pharmacol. 2009. PMID: 19255243
Design, synthesis, and biological evaluation of CXCR4 ligands.
Mona CE, Besserer-Offroy É, Cabana J, Leduc R, Lavigne P, Heveker N, Marsault É, Escher E. Mona CE, et al. Among authors: heveker n. Org Biomol Chem. 2016 Nov 2;14(43):10298-10311. doi: 10.1039/c6ob01484d. Org Biomol Chem. 2016. PMID: 27752700
Structure-Activity Relationship and Signaling of New Chimeric CXCR4 Agonists.
Mona CE, Besserer-Offroy É, Cabana J, Lefrançois M, Boulais PE, Lefebvre MR, Leduc R, Lavigne P, Heveker N, Marsault É, Escher E. Mona CE, et al. Among authors: heveker n. J Med Chem. 2016 Aug 25;59(16):7512-24. doi: 10.1021/acs.jmedchem.6b00566. Epub 2016 Aug 11. J Med Chem. 2016. PMID: 27434274
67 results