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Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure- based drug design.
O'Brien A, Andrews SP, Baig AH, Bortolato A, Brown AJH, Brown GA, Brown SH, Christopher JA, Congreve M, Cooke RM, De Graaf C, Errey JC, Fieldhouse C, Jazayeri A, Marshall FH, Mason JS, Mobarec JC, Okrasa K, Steele KN, Southall SM, Teobald I, Watson SP, Weir M. O'Brien A, et al. Among authors: mobarec jc. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126611. doi: 10.1016/j.bmcl.2019.08.015. Epub 2019 Aug 9. Bioorg Med Chem Lett. 2019. PMID: 31447084
Rational development of a high-affinity secretin receptor antagonist.
Dong M, Harikumar KG, Raval SR, Milburn JE, Clark C, Alcala-Torano R, Mobarec JC, Reynolds CA, Ghirlanda G, Christopoulos A, Wootten D, Sexton PM, Miller LJ. Dong M, et al. Among authors: mobarec jc. Biochem Pharmacol. 2020 Jul;177:113929. doi: 10.1016/j.bcp.2020.113929. Epub 2020 Mar 23. Biochem Pharmacol. 2020. PMID: 32217097 Free PMC article.
Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptor.
Wootten D, Reynolds CA, Smith KJ, Mobarec JC, Furness SG, Miller LJ, Christopoulos A, Sexton PM. Wootten D, et al. Among authors: mobarec jc. Biochem Pharmacol. 2016 Oct 15;118:68-87. doi: 10.1016/j.bcp.2016.08.015. Epub 2016 Aug 26. Biochem Pharmacol. 2016. PMID: 27569426 Free PMC article.
Receptor Activity-modifying Protein-directed G Protein Signaling Specificity for the Calcitonin Gene-related Peptide Family of Receptors.
Weston C, Winfield I, Harris M, Hodgson R, Shah A, Dowell SJ, Mobarec JC, Woodlock DA, Reynolds CA, Poyner DR, Watkins HA, Ladds G. Weston C, et al. Among authors: mobarec jc. J Biol Chem. 2016 Oct 14;291(42):21925-21944. doi: 10.1074/jbc.M116.751362. Epub 2016 Aug 26. J Biol Chem. 2016. PMID: 27566546 Free PMC article.
26 results