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Items: 21


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.

Biochem Pharmacol. 2020 Mar 23:113929. doi: 10.1016/j.bcp.2020.113929. [Epub ahead of print]


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.

Bioorg Med Chem Lett. 2019 Oct 15;29(20):126611. doi: 10.1016/j.bmcl.2019.08.015. Epub 2019 Aug 9.


Receptor activity-modifying protein dependent and independent activation mechanisms in the coupling of calcitonin gene-related peptide and adrenomedullin receptors to Gs.

Woolley MJ, Reynolds CA, Simms J, Walker CS, Mobarec JC, Garelja ML, Conner AC, Poyner DR, Hay DL.

Biochem Pharmacol. 2017 Oct 15;142:96-110. doi: 10.1016/j.bcp.2017.07.005. Epub 2017 Jul 11.


Understanding the molecular functions of the second extracellular loop (ECL2) of the calcitonin gene-related peptide (CGRP) receptor using a comprehensive mutagenesis approach.

Woolley MJ, Simms J, Mobarec JC, Reynolds CA, Poyner DR, Conner AC.

Mol Cell Endocrinol. 2017 Oct 15;454:39-49. doi: 10.1016/j.mce.2017.05.034. Epub 2017 May 30.


Genetically encoded photocross-linkers determine the biological binding site of exendin-4 peptide in the N-terminal domain of the intact human glucagon-like peptide-1 receptor (GLP-1R).

Koole C, Reynolds CA, Mobarec JC, Hick C, Sexton PM, Sakmar TP.

J Biol Chem. 2017 Apr 28;292(17):7131-7144. doi: 10.1074/jbc.M117.779496. Epub 2017 Mar 10.


High affinity binding of the peptide agonist TIP-39 to the parathyroid hormone 2 (PTH2) receptor requires the hydroxyl group of Tyr-318 on transmembrane helix 5.

Weaver RE, Mobarec JC, Wigglesworth MJ, Reynolds CA, Donnelly D.

Biochem Pharmacol. 2017 Mar 1;127:71-81. doi: 10.1016/j.bcp.2016.12.013. Epub 2016 Dec 22.


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, Woodcock DA, Reynolds CA, Poyner DR, Watkins HA, Ladds G.

J Biol Chem. 2016 Dec 2;291(49):25763. No abstract available.


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.

Biochem Pharmacol. 2016 Oct 15;118:68-87. doi: 10.1016/j.bcp.2016.08.015. Epub 2016 Aug 26.


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.

J Biol Chem. 2016 Oct 14;291(42):21925-21944. Epub 2016 Aug 26. Erratum in: J Biol Chem. 2016 Dec 2;291(49):25763.


The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism.

Wootten D, Reynolds CA, Smith KJ, Mobarec JC, Koole C, Savage EE, Pabreja K, Simms J, Sridhar R, Furness SGB, Liu M, Thompson PE, Miller LJ, Christopoulos A, Sexton PM.

Cell. 2016 Jun 16;165(7):1632-1643. doi: 10.1016/j.cell.2016.05.023.


A Hydrogen-Bonded Polar Network in the Core of the Glucagon-Like Peptide-1 Receptor Is a Fulcrum for Biased Agonism: Lessons from Class B Crystal Structures.

Wootten D, Reynolds CA, Koole C, Smith KJ, Mobarec JC, Simms J, Quon T, Coudrat T, Furness SG, Miller LJ, Christopoulos A, Sexton PM.

Mol Pharmacol. 2016 Mar;89(3):335-47. doi: 10.1124/mol.115.101246. Epub 2015 Dec 23.


The quorum-sensing regulator ComA from Bacillus subtilis activates transcription using topologically distinct DNA motifs.

Wolf D, Rippa V, Mobarec JC, Sauer P, Adlung L, Kolb P, Bischofs IB.

Nucleic Acids Res. 2016 Mar 18;44(5):2160-72. doi: 10.1093/nar/gkv1242. Epub 2015 Nov 17.


The mode of agonist binding to a G protein-coupled receptor switches the effect that voltage changes have on signaling.

Rinne A, Mobarec JC, Mahaut-Smith M, Kolb P, B√ľnemann M.

Sci Signal. 2015 Nov 3;8(401):ra110. doi: 10.1126/scisignal.aac7419.


Crystal structure of the human OX2 orexin receptor bound to the insomnia drug suvorexant.

Yin J, Mobarec JC, Kolb P, Rosenbaum DM.

Nature. 2015 Mar 12;519(7542):247-50. doi: 10.1038/nature14035. Epub 2014 Dec 22.


Ligand-induced modulation of the free-energy landscape of G protein-coupled receptors explored by adaptive biasing techniques.

Provasi D, Artacho MC, Negri A, Mobarec JC, Filizola M.

PLoS Comput Biol. 2011 Oct;7(10):e1002193. doi: 10.1371/journal.pcbi.1002193. Epub 2011 Oct 13.


Life in blue: copper resistance mechanisms of bacteria and archaea used in industrial biomining of minerals.

Orell A, Navarro CA, Arancibia R, Mobarec JC, Jerez CA.

Biotechnol Adv. 2010 Nov-Dec;28(6):839-48. doi: 10.1016/j.biotechadv.2010.07.003. Epub 2010 Jul 11. Review.


Progress in elucidating the structural and dynamic character of G Protein-Coupled Receptor oligomers for use in drug discovery.

Bortolato A, Mobarec JC, Provasi D, Filizola M.

Curr Pharm Des. 2009;15(35):4017-25. Review.


Modern homology modeling of G-protein coupled receptors: which structural template to use?

Mobarec JC, Sanchez R, Filizola M.

J Med Chem. 2009 Aug 27;52(16):5207-16. doi: 10.1021/jm9005252.


Dopamine D2 receptors form higher order oligomers at physiological expression levels.

Guo W, Urizar E, Kralikova M, Mobarec JC, Shi L, Filizola M, Javitch JA.

EMBO J. 2008 Sep 3;27(17):2293-304. doi: 10.1038/emboj.2008.153.


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