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Items: 1 to 50 of 279

1.

O-GlcNAc engineering of GPCR peptide-agonists improves their stability and in vivo activity.

Levine PM, Balana AJ, Sturchler E, Koole C, Noda H, Zarzycka B, Daley EJ, Truong TT, Katritch V, Gardella TJ, Wootten D, Sexton PM, McDonald P, Pratt MR.

J Am Chem Soc. 2019 Aug 16. doi: 10.1021/jacs.9b05365. [Epub ahead of print]

PMID:
31418572
2.

Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs.

Hollingsworth SA, Kelly B, Valant C, Michaelis JA, Mastromihalis O, Thompson G, Venkatakrishnan AJ, Hertig S, Scammells PJ, Sexton PM, Felder CC, Christopoulos A, Dror RO.

Nat Commun. 2019 Jul 23;10(1):3289. doi: 10.1038/s41467-019-11062-7.

3.

Light-activated chimeric GPCRs: limitations and opportunities.

Tichy AM, Gerrard EJ, Sexton PM, Janovjak H.

Curr Opin Struct Biol. 2019 Aug;57:196-203. doi: 10.1016/j.sbi.2019.05.006. Epub 2019 Jun 14. Review.

PMID:
31207383
4.

DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo.

Thompson KJ, Khajehali E, Bradley SJ, Navarrete JS, Huang XP, Slocum S, Jin J, Liu J, Xiong Y, Olsen RHJ, Diberto JF, Boyt KM, Pina MM, Pati D, Molloy C, Bundgaard C, Sexton PM, Kash TL, Krashes MJ, Christopoulos A, Roth BL, Tobin AB.

ACS Pharmacol Transl Sci. 2018 Sep 14;1(1):61-72. doi: 10.1021/acsptsci.8b00012. Epub 2018 Jul 27.

5.

Expression and activity of the calcitonin receptor family in a sample of primary human high-grade gliomas.

Ostrovskaya A, Hick C, Hutchinson DS, Stringer BW, Wookey PJ, Wootten D, Sexton PM, Furness SGB.

BMC Cancer. 2019 Feb 18;19(1):157. doi: 10.1186/s12885-019-5369-y.

6.

Molecular Basis of Action of a Small-Molecule Positive Allosteric Modulator Agonist at the Type 1 Cholecystokinin Holoreceptor.

Desai AJ, Mechin I, Nagarajan K, Valant C, Wootten D, Lam PCH, Orry A, Abagyan R, Nair A, Sexton PM, Christopoulos A, Miller LJ.

Mol Pharmacol. 2019 Mar;95(3):245-259. doi: 10.1124/mol.118.114082. Epub 2018 Dec 27.

PMID:
30591538
7.

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity.

Jörg M, van der Westhuizen ET, Khajehali E, Burger WAC, White JM, Choy KHC, Tobin AB, Sexton PM, Valant C, Capuano B, Christopoulos A, Scammells PJ.

ACS Chem Neurosci. 2019 Mar 20;10(3):1099-1114. doi: 10.1021/acschemneuro.8b00613. Epub 2018 Dec 28.

PMID:
30547573
8.

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists.

Riddy DM, Cook AE, Shackleford DM, Pierce TL, Mocaer E, Mannoury la Cour C, Sors A, Charman WN, Summers RJ, Sexton PM, Christopoulos A, Langmead CJ.

Neuropharmacology. 2019 Jan;144:244-255. doi: 10.1016/j.neuropharm.2018.10.028. Epub 2018 Oct 22.

PMID:
30359639
9.

Utility of an "Allosteric Site-Impaired" M2 Muscarinic Acetylcholine Receptor as a Novel Construct for Validating Mechanisms of Action of Synthetic and Putative Endogenous Allosteric Modulators.

Moo EV, Sexton PM, Christopoulos A, Valant C.

Mol Pharmacol. 2018 Nov;94(5):1298-1309. doi: 10.1124/mol.118.112490. Epub 2018 Sep 13.

PMID:
30213802
10.

Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor.

Liang YL, Khoshouei M, Deganutti G, Glukhova A, Koole C, Peat TS, Radjainia M, Plitzko JM, Baumeister W, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Wootten D, Sexton PM.

Nature. 2018 Sep;561(7724):492-497. doi: 10.1038/s41586-018-0535-y. Epub 2018 Sep 12.

11.

Glucagon-like peptide-1 receptor internalisation controls spatiotemporal signalling mediated by biased agonists.

Fletcher MM, Halls ML, Zhao P, Clydesdale L, Christopoulos A, Sexton PM, Wootten D.

Biochem Pharmacol. 2018 Oct;156:406-419. doi: 10.1016/j.bcp.2018.09.003. Epub 2018 Sep 7.

PMID:
30195733
12.

Toward an understanding of the structural basis of allostery in muscarinic acetylcholine receptors.

Burger WAC, Sexton PM, Christopoulos A, Thal DM.

J Gen Physiol. 2018 Oct 1;150(10):1360-1372. doi: 10.1085/jgp.201711979. Epub 2018 Sep 6. Review.

13.

Differential engagement of polar networks in the glucagon-like peptide 1 receptor by endogenous variants of the glucagon-like peptide 1.

Furness SGB, Christopoulos A, Sexton PM, Wootten D.

Biochem Pharmacol. 2018 Oct;156:223-240. doi: 10.1016/j.bcp.2018.08.033. Epub 2018 Aug 25.

PMID:
30149018
14.

Mechanisms of signalling and biased agonism in G protein-coupled receptors.

Wootten D, Christopoulos A, Marti-Solano M, Babu MM, Sexton PM.

Nat Rev Mol Cell Biol. 2018 Oct;19(10):638-653. doi: 10.1038/s41580-018-0049-3. Review.

PMID:
30104700
15.

Structural insights into G-protein-coupled receptor allostery.

Thal DM, Glukhova A, Sexton PM, Christopoulos A.

Nature. 2018 Jul;559(7712):45-53. doi: 10.1038/s41586-018-0259-z. Epub 2018 Jul 4. Review.

PMID:
29973731
16.

Structure of the adenosine-bound human adenosine A1 receptor-Gi complex.

Draper-Joyce CJ, Khoshouei M, Thal DM, Liang YL, Nguyen ATN, Furness SGB, Venugopal H, Baltos JA, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, Christopoulos A.

Nature. 2018 Jun;558(7711):559-563. doi: 10.1038/s41586-018-0236-6. Epub 2018 Jun 20.

PMID:
29925945
17.

Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor.

Khajehali E, Valant C, Jörg M, Tobin AB, Conn PJ, Lindsley CW, Sexton PM, Scammells PJ, Christopoulos A.

Biochem Pharmacol. 2018 Aug;154:243-254. doi: 10.1016/j.bcp.2018.05.009. Epub 2018 May 17.

18.

Comparative genotypic and phenotypic analysis of human peripheral blood monocytes and surrogate monocyte-like cell lines commonly used in metabolic disease research.

Riddy DM, Goy E, Delerive P, Summers RJ, Sexton PM, Langmead CJ.

PLoS One. 2018 May 10;13(5):e0197177. doi: 10.1371/journal.pone.0197177. eCollection 2018.

19.

Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism.

Lei S, Clydesdale L, Dai A, Cai X, Feng Y, Yang D, Liang YL, Koole C, Zhao P, Coudrat T, Christopoulos A, Wang MW, Wootten D, Sexton PM.

J Biol Chem. 2018 Jun 15;293(24):9370-9387. doi: 10.1074/jbc.RA118.003278. Epub 2018 May 1.

20.

Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity.

Diepenhorst NA, Leach K, Keller AN, Rueda P, Cook AE, Pierce TL, Nowell C, Pastoureau P, Sabatini M, Summers RJ, Charman WN, Sexton PM, Christopoulos A, Langmead CJ.

Br J Pharmacol. 2018 Nov;175(21):4095-4108. doi: 10.1111/bph.14344. Epub 2018 Jun 3.

PMID:
29714810
21.

Bitopic Binding Mode of an M1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes.

Bradley SJ, Molloy C, Bundgaard C, Mogg AJ, Thompson KJ, Dwomoh L, Sanger HE, Crabtree MD, Brooke SM, Sexton PM, Felder CC, Christopoulos A, Broad LM, Tobin AB, Langmead CJ.

Mol Pharmacol. 2018 Jun;93(6):645-656. doi: 10.1124/mol.118.111872. Epub 2018 Apr 25.

22.

Assessment of the Molecular Mechanisms of Action of Novel 4-Phenylpyridine-2-One and 6-Phenylpyrimidin-4-One Allosteric Modulators at the M1 Muscarinic Acetylcholine Receptors.

van der Westhuizen ET, Spathis A, Khajehali E, Jörg M, Mistry SN, Capuano B, Tobin AB, Sexton PM, Scammells PJ, Valant C, Christopoulos A.

Mol Pharmacol. 2018 Jul;94(1):770-783. doi: 10.1124/mol.118.111633. Epub 2018 Apr 24.

PMID:
29691279
23.

Structure-Activity Relationships of Pan-Gαq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators.

Berizzi AE, Bender AM, Lindsley CW, Conn PJ, Sexton PM, Langmead CJ, Christopoulos A.

ACS Chem Neurosci. 2018 Jul 18;9(7):1818-1828. doi: 10.1021/acschemneuro.8b00136. Epub 2018 Apr 30.

24.

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold.

Bender AM, Cho HP, Nance KD, Lingenfelter KS, Luscombe VB, Gentry PR, Voigtritter K, Berizzi AE, Sexton PM, Langmead CJ, Christopoulos A, Locuson CW, Bridges TM, Chang S, O'Neill JC, Zhan X, Niswender CM, Jones CK, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2018 Jul 18;9(7):1572-1581. doi: 10.1021/acschemneuro.8b00126. Epub 2018 Apr 26.

25.

Vascular and molecular pharmacology of the metabolically stable CGRP analogue, SAX.

Sheykhzade M, Abdolalizadeh B, Koole C, Pickering DS, Dreisig K, Johansson SE, Abboud BK, Dreier R, Berg JO, Jeppesen JL, Sexton PM, Edvinsson L, Wootten D, Sams A.

Eur J Pharmacol. 2018 Jun 15;829:85-92. doi: 10.1016/j.ejphar.2018.04.007. Epub 2018 Apr 10.

PMID:
29653090
26.

Recent advances in the determination of G protein-coupled receptor structures.

Thal DM, Vuckovic Z, Draper-Joyce CJ, Liang YL, Glukhova A, Christopoulos A, Sexton PM.

Curr Opin Struct Biol. 2018 Aug;51:28-34. doi: 10.1016/j.sbi.2018.03.002. Epub 2018 Mar 13. Review.

PMID:
29547818
27.

Muscarinic M5 receptors modulate ethanol seeking in rats.

Berizzi AE, Perry CJ, Shackleford DM, Lindsley CW, Jones CK, Chen NA, Sexton PM, Christopoulos A, Langmead CJ, Lawrence AJ.

Neuropsychopharmacology. 2018 Jun;43(7):1510-1517. doi: 10.1038/s41386-017-0007-3. Epub 2018 Feb 5.

28.

Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex.

Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D.

Nature. 2018 Mar 1;555(7694):121-125. doi: 10.1038/nature25773. Epub 2018 Feb 21.

PMID:
29466332
29.

Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy.

Dal Maso E, Zhu Y, Pham V, Reynolds CA, Deganutti G, Hick CA, Yang D, Christopoulos A, Hay DL, Wang MW, Sexton PM, Furness SGB, Wootten D.

Biochem Pharmacol. 2018 Apr;150:214-244. doi: 10.1016/j.bcp.2018.02.005. Epub 2018 Feb 16.

30.

Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor.

Korczynska M, Clark MJ, Valant C, Xu J, Moo EV, Albold S, Weiss DR, Torosyan H, Huang W, Kruse AC, Lyda BR, May LT, Baltos JA, Sexton PM, Kobilka BK, Christopoulos A, Shoichet BK, Sunahara RK.

Proc Natl Acad Sci U S A. 2018 Mar 6;115(10):E2419-E2428. doi: 10.1073/pnas.1718037115. Epub 2018 Feb 16.

31.

To Bind or Not to Bind: Unravelling GPCR Polypharmacology.

Sexton PM, Christopoulos A.

Cell. 2018 Feb 8;172(4):636-638. doi: 10.1016/j.cell.2018.01.018.

32.

Correspondence: Reply to 'Compound 17b and formyl peptide receptor biased agonism in relation to cardioprotective effects in ischaemia-reperfusion injury'.

Qin CX, May LT, Sexton PM, DeBono AJ, Baell JB, Christopoulos A, Ritchie RH.

Nat Commun. 2018 Feb 7;9(1):530. doi: 10.1038/s41467-017-02656-0. No abstract available.

33.

Characterization of signalling and regulation of common calcitonin receptor splice variants and polymorphisms.

Dal Maso E, Just R, Hick C, Christopoulos A, Sexton PM, Wootten D, Furness SGB.

Biochem Pharmacol. 2018 Feb;148:111-129. doi: 10.1016/j.bcp.2017.12.016. Epub 2017 Dec 23.

PMID:
29277692
34.

G Protein-Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus.

Riddy DM, Delerive P, Summers RJ, Sexton PM, Langmead CJ.

Pharmacol Rev. 2018 Jan;70(1):39-67. doi: 10.1124/pr.117.014373. Review.

PMID:
29233848
35.

Improving virtual screening of G protein-coupled receptors via ligand-directed modeling.

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

PLoS Comput Biol. 2017 Nov 13;13(11):e1005819. doi: 10.1371/journal.pcbi.1005819. eCollection 2017 Nov.

36.

A kinetic view of GPCR allostery and biased agonism.

Lane JR, May LT, Parton RG, Sexton PM, Christopoulos A.

Nat Chem Biol. 2017 Aug 18;13(9):929-937. doi: 10.1038/nchembio.2431.

PMID:
28820879
37.

Coding GPCR-G protein specificity.

Furness SG, Sexton PM.

Cell Res. 2017 Oct;27(10):1193-1194. doi: 10.1038/cr.2017.92. Epub 2017 Jul 11.

38.

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 Jun 1;546(7656):118-123. doi: 10.1038/nature22327. Epub 2017 Apr 24.

39.

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.

40.

Coexpressed 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 Jun 1;158(6):1685-1700. doi: 10.1210/en.2017-00023.

PMID:
28368447
41.

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 Jul 15;136:99-108. doi: 10.1016/j.bcp.2017.03.018. Epub 2017 Mar 29.

42.

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.

43.

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.

44.

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.

45.

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.

46.

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.

47.

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
48.

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
49.

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.

50.

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

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