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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: guite vinet f. Sci Signal. 2018 Oct 16;11(552):eaat2214. doi: 10.1126/scisignal.aat2214. Sci Signal. 2018. PMID: 30327409 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: guite vinet f. 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.