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Items: 1 to 50 of 324

1.

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. 2018 Oct 22;144:244-255. doi: 10.1016/j.neuropharm.2018.10.028. [Epub ahead of print]

PMID:
30359639
2.

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.

Von Moo E, 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
3.

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.

PMID:
30209400
4.

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
5.

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.

PMID:
30190312
6.

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
7.

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
8.

Successful use of adipose-derived mesenchymal stem cells to correct a male breast affected by Poland Syndrome: a case report.

Christopoulos A, Ligoudistianou C, Bethanis P, Gazouli M.

J Surg Case Rep. 2018 Jul 9;2018(7):rjy151. doi: 10.1093/jscr/rjy151. eCollection 2018 Jul.

9.

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.

PMID:
29973731
10.

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
11.
12.

Strength in numbers-an arrestin interaction code.

Draper-Joyce CJ, Christopoulos A.

Nat Struct Mol Biol. 2018 Jun;25(6):437-439. doi: 10.1038/s41594-018-0077-x. No abstract available.

PMID:
29872226
13.

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.

14.

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.

PMID:
29717000
15.

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
16.

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.

17.

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
18.

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.

PMID:
29683647
19.

New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism.

Vecchio EA, Baltos JA, Nguyen ATN, Christopoulos A, White PJ, May LT.

Br J Pharmacol. 2018 Nov;175(21):4036-4046. doi: 10.1111/bph.14337. Epub 2018 Jun 21. Review.

PMID:
29679502
20.

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.

PMID:
29678111
21.

Identification of Global and Ligand-Specific Calcium Sensing Receptor Activation Mechanisms.

Keller AN, Kufareva I, Josephs TM, Diao J, Mai VT, Conigrave AD, Christopoulos A, Gregory KJ, Leach K.

Mol Pharmacol. 2018 Jun;93(6):619-630. doi: 10.1124/mol.118.112086. Epub 2018 Apr 10.

PMID:
29636377
22.

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
23.

Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles.

Dallagnol JCC, Khajehali E, van der Westhuizen ET, Jörg M, Valant C, Gonçalves AG, Capuano B, Christopoulos A, Scammells PJ.

J Med Chem. 2018 Apr 12;61(7):2875-2894. doi: 10.1021/acs.jmedchem.7b01812. Epub 2018 Mar 23.

PMID:
29544056
24.

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.

25.

Decreasing Revision Surgery in FAMM Flap Reconstruction of the Oral Cavity: Traditional Versus Modified Harvesting Technique.

Ibrahim B, Rahal A, Bissada E, Christopoulos A, Moubayed SP, Guertin L, Tabet JC, Olivier MJ, Ayad T.

Laryngoscope. 2018 Aug;128(8):1802-1805. doi: 10.1002/lary.27150. Epub 2018 Feb 26.

PMID:
29481692
26.

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
27.

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.

28.

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.

29.

A Structure-Activity Relationship Study of Bitopic N6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists.

Aurelio L, Baltos JA, Ford L, Nguyen ATN, Jörg M, Devine SM, Valant C, White PJ, Christopoulos A, May LT, Scammells PJ.

J Med Chem. 2018 Mar 8;61(5):2087-2103. doi: 10.1021/acs.jmedchem.8b00047. Epub 2018 Feb 23.

PMID:
29446948
30.

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.

PMID:
29425482
31.

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.

32.

The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions.

Draper-Joyce CJ, Verma RK, Michino M, Shonberg J, Kopinathan A, Klein Herenbrink C, Scammells PJ, Capuano B, Abramyan AM, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR.

Sci Rep. 2018 Jan 19;8(1):1208. doi: 10.1038/s41598-018-19642-1.

33.

The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor.

Draper-Joyce CJ, Michino M, Verma RK, Klein Herenbrink C, Shonberg J, Kopinathan A, Scammells PJ, Capuano B, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR.

Biochem Pharmacol. 2018 Feb;148:315-328. doi: 10.1016/j.bcp.2018.01.002. Epub 2018 Jan 9.

PMID:
29325769
34.

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
35.

Diffuse Idiopathic Hyperostosis Manifesting as Dysphagia and Bilateral Cord Paralysis: A Case Report and Literature Review.

Sebaaly A, Boubez G, Sunna T, Wang Z, Alam E, Christopoulos A, Shedid D.

World Neurosurg. 2018 Mar;111:79-85. doi: 10.1016/j.wneu.2017.12.063. Epub 2017 Dec 18.

PMID:
29269071
36.

Cyanotoxins as the "common suspects" for the Dalmatian pelican (Pelecanus crispus) deaths in a Mediterranean reconstructed reservoir.

Papadimitriou T, Katsiapi M, Vlachopoulos K, Christopoulos A, Laspidou C, Moustaka-Gouni M, Kormas K.

Environ Pollut. 2018 Mar;234:779-787. doi: 10.1016/j.envpol.2017.12.022. Epub 2017 Dec 21.

PMID:
29247940
37.

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.

38.

Structure-Based Design and Discovery of New M2 Receptor Agonists.

Fish I, Stößel A, Eitel K, Valant C, Albold S, Huebner H, Möller D, Clark MJ, Sunahara RK, Christopoulos A, Shoichet BK, Gmeiner P.

J Med Chem. 2017 Nov 22;60(22):9239-9250. doi: 10.1021/acs.jmedchem.7b01113. Epub 2017 Nov 13.

PMID:
29094937
39.

Work-related musculoskeletal symptoms amongst Otolaryngologists and Head and Neck surgeons in Canada.

Bolduc-Bégin J, Prince F, Christopoulos A, Ayad T.

Eur Arch Otorhinolaryngol. 2018 Jan;275(1):261-267. doi: 10.1007/s00405-017-4787-1. Epub 2017 Oct 26.

PMID:
29075981
40.

THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: G protein-coupled receptors.

Alexander SP, Christopoulos A, Davenport AP, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators.

Br J Pharmacol. 2017 Dec;174 Suppl 1:S17-S129. doi: 10.1111/bph.13878.

41.

THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview.

Alexander SP, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Buneman OP, Cidlowski JA, Christopoulos A, Davenport AP, Fabbro D, Spedding M, Striessnig J, Davies JA; CGTP Collaborators.

Br J Pharmacol. 2017 Dec;174 Suppl 1:S1-S16. doi: 10.1111/bph.13882.

42.

Allosteric modulation as a unifying mechanism for receptor function and regulation.

Changeux JP, Christopoulos A.

Diabetes Obes Metab. 2017 Sep;19 Suppl 1:4-21. doi: 10.1111/dom.12959. Review.

PMID:
28880476
43.

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
44.

Four PTEN-targeting co-expressed miRNAs and ACTN4- targeting miR-548b are independent prognostic biomarkers in human squamous cell carcinoma of the oral tongue.

Berania I, Cardin GB, Clément I, Guertin L, Ayad T, Bissada E, Nguyen-Tan PF, Filion E, Guilmette J, Gologan O, Soulieres D, Rodier F, Wong P, Christopoulos A.

Int J Cancer. 2017 Dec 1;141(11):2318-2328. doi: 10.1002/ijc.30915. Epub 2017 Aug 18.

PMID:
28779483
45.

Perioperative practices in thyroid surgery: An international survey.

Maniakas A, Christopoulos A, Bissada E, Guertin L, Olivier MJ, Malaise J, Ayad T.

Head Neck. 2017 Jul;39(7):1296-1305. doi: 10.1002/hed.24722. Epub 2017 May 11.

PMID:
28493562
46.

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.

47.

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.

48.

Capadenoson, a clinically trialed partial adenosine A1 receptor agonist, can stimulate adenosine A2B receptor biased agonism.

Baltos JA, Vecchio EA, Harris MA, Qin CX, Ritchie RH, Christopoulos A, White PJ, May LT.

Biochem Pharmacol. 2017 Jul 1;135:79-89. doi: 10.1016/j.bcp.2017.03.014. Epub 2017 Mar 23.

PMID:
28344125
49.

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.

50.

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.

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