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Items: 1 to 20 of 315

1.

Phase-plate cryo-EM structure of a class B GPCR-G-protein complex.

Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, Wootten D, Skiniotis G, Sexton PM.

Nature. 2017 Apr 24. doi: 10.1038/nature22327. [Epub ahead of print]

PMID:
28437792
2.

Structural features embedded in G protein-coupled receptor co-crystal structures are key to their success in virtual screening.

Coudrat T, Christopoulos A, Sexton PM, Wootten D.

PLoS One. 2017 Apr 5;12(4):e0174719. doi: 10.1371/journal.pone.0174719. eCollection 2017.

3.

Co-expressed class B G protein-coupled secretin and GLP-1 receptors self- and cross-associate: Impact on pancreatic islets.

Harikumar KG, Lau S, Sexton PM, Wootten D, Miller LJ.

Endocrinology. 2017 Mar 29. doi: 10.1210/en.2017-00023. [Epub ahead of print]

PMID:
28368447
4.

Characterization of signal bias at the GLP-1 receptor induced by backbone modification of GLP-1.

Hager MV, Clydesdale L, Gellman SH, Sexton PM, Wootten D.

Biochem Pharmacol. 2017 Mar 29. pii: S0006-2952(17)30165-X. doi: 10.1016/j.bcp.2017.03.018. [Epub ahead of print]

PMID:
28363772
5.

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.

6.

Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity.

Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jörg M, Scammells PJ, May LT, Sexton PM, Christopoulos A.

Cell. 2017 Feb 23;168(5):867-877.e13. doi: 10.1016/j.cell.2017.01.042.

PMID:
28235198
7.

Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice.

Qin CX, May LT, Li R, Cao N, Rosli S, Deo M, Alexander AE, Horlock D, Bourke JE, Yang YH, Stewart AG, Kaye DM, Du XJ, Sexton PM, Christopoulos A, Gao XM, Ritchie RH.

Nat Commun. 2017 Feb 7;8:14232. doi: 10.1038/ncomms14232.

8.

What determines the magnitude of cellular response for activation of G protein-coupled receptors?

Furness SG, Wootten D, Sexton PM.

Cell Cycle. 2017 Mar 4;16(5):392-394. doi: 10.1080/15384101.2016.1271634. Epub 2017 Jan 5. No abstract available.

PMID:
28055294
9.

M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss.

Bradley SJ, Bourgognon JM, Sanger HE, Verity N, Mogg AJ, White DJ, Butcher AJ, Moreno JA, Molloy C, Macedo-Hatch T, Edwards JM, Wess J, Pawlak R, Read DJ, Sexton PM, Broad LM, Steinert JR, Mallucci GR, Christopoulos A, Felder CC, Tobin AB.

J Clin Invest. 2017 Feb 1;127(2):487-499. doi: 10.1172/JCI87526. Epub 2016 Dec 19.

10.

High throughput, quantitative analysis of human osteoclast differentiation and activity.

Diepenhorst NA, Nowell CJ, Rueda P, Henriksen K, Pierce T, Cook AE, Pastoureau P, Sabatini M, Charman WN, Christopoulos A, Summers RJ, Sexton PM, Langmead CJ.

Anal Biochem. 2017 Feb 15;519:51-56. doi: 10.1016/j.ab.2016.12.010. Epub 2016 Dec 14.

PMID:
27988276
11.

Novel Irreversible Agonists Acting at the A1 Adenosine Receptor.

Jörg M, Glukhova A, Abdul-Ridha A, Vecchio EA, Nguyen AT, Sexton PM, White PJ, May LT, Christopoulos A, Scammells PJ.

J Med Chem. 2016 Dec 22;59(24):11182-11194. doi: 10.1021/acs.jmedchem.6b01561. Epub 2016 Dec 13.

PMID:
27958734
12.

Monotreme glucagon-like peptide-1 in venom and gut: one gene - two very different functions.

Tsend-Ayush E, He C, Myers MA, Andrikopoulos S, Wong N, Sexton PM, Wootten D, Forbes BE, Grutzner F.

Sci Rep. 2016 Nov 29;6:37744. doi: 10.1038/srep37744.

13.

Isoform-Specific Biased Agonism of Histamine H3 Receptor Agonists.

Riddy DM, Cook AE, Diepenhorst NA, Bosnyak S, Brady R, Mannoury la Cour C, Mocaer E, Summers RJ, Charman WN, Sexton PM, Christopoulos A, Langmead CJ.

Mol Pharmacol. 2017 Feb;91(2):87-99. doi: 10.1124/mol.116.106153. Epub 2016 Nov 18. Erratum in: Mol Pharmacol. 2017 Mar;91(3):263.

PMID:
27864425
14.

β-Arrestin-Biased Agonists of the GLP-1 Receptor from β-Amino Acid Residue Incorporation into GLP-1 Analogues.

Hager MV, Johnson LM, Wootten D, Sexton PM, Gellman SH.

J Am Chem Soc. 2016 Nov 16;138(45):14970-14979. Epub 2016 Nov 4.

PMID:
27813409
15.

Extracellular Loop 2 of the Adenosine A1 Receptor Has a Key Role in Orthosteric Ligand Affinity and Agonist Efficacy.

Nguyen AT, Baltos JA, Thomas T, Nguyen TD, Muñoz LL, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT.

Mol Pharmacol. 2016 Dec;90(6):703-714. Epub 2016 Sep 28.

PMID:
27683014
16.

Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

Nguyen AT, Vecchio EA, Thomas T, Nguyen TD, Aurelio L, Scammells PJ, White PJ, Sexton PM, Gregory KJ, May LT, Christopoulos A.

Mol Pharmacol. 2016 Dec;90(6):715-725. Epub 2016 Sep 28.

PMID:
27683013
17.

Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy.

Furness SG, Liang YL, Nowell CJ, Halls ML, Wookey PJ, Dal Maso E, Inoue A, Christopoulos A, Wootten D, Sexton PM.

Cell. 2016 Oct 20;167(3):739-749.e11. doi: 10.1016/j.cell.2016.09.021. Epub 2016 Oct 6.

PMID:
27720449
18.

Positive Allosteric Modulation of the Muscarinic M1 Receptor Improves Efficacy of Antipsychotics in Mouse Glutamatergic Deficit Models of Behavior.

Choy KH, Shackleford DM, Malone DT, Mistry SN, Patil RT, Scammells PJ, Langmead CJ, Pantelis C, Sexton PM, Lane JR, Christopoulos A.

J Pharmacol Exp Ther. 2016 Nov;359(2):354-365. Epub 2016 Sep 14.

PMID:
27630144
19.

Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes.

Graaf Cd, Donnelly D, Wootten D, Lau J, Sexton PM, Miller LJ, Ahn JM, Liao J, Fletcher MM, Yang D, Brown AJ, Zhou C, Deng J, Wang MW.

Pharmacol Rev. 2016 Oct;68(4):954-1013. doi: 10.1124/pr.115.011395. Review.

20.

Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor.

Miao Y, Goldfeld DA, Moo EV, Sexton PM, Christopoulos A, McCammon JA, Valant C.

Proc Natl Acad Sci U S A. 2016 Sep 20;113(38):E5675-84. doi: 10.1073/pnas.1612353113. Epub 2016 Sep 6.

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