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Items: 1 to 50 of 317

1.

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.

PMID:
30002805
2.

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
3.

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
4.
5.

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
6.

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 May 17;154:243-254. doi: 10.1016/j.bcp.2018.05.009. [Epub ahead of print]

7.

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
8.

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 May 1. doi: 10.1111/bph.14344. [Epub ahead of print]

PMID:
29714810
9.

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.

10.

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
11.

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 Apr 30. doi: 10.1021/acschemneuro.8b00136. [Epub ahead of print]

PMID:
29683647
12.

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 Apr 21. doi: 10.1111/bph.14337. [Epub ahead of print] Review.

PMID:
29679502
13.

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 Apr 26. doi: 10.1021/acschemneuro.8b00126. [Epub ahead of print]

PMID:
29678111
14.

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
15.

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 Mar 13;51:28-34. doi: 10.1016/j.sbi.2018.03.002. [Epub ahead of print] Review.

PMID:
29547818
16.

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
17.

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.

18.

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 Feb 26. doi: 10.1002/lary.27150. [Epub ahead of print]

PMID:
29481692
19.

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
20.

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.

21.

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.

22.

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
23.

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
24.

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.

25.

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.

26.

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
27.

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
28.

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
29.

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
30.

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.

31.

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
32.

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
33.

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.

34.

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.

35.

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
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.

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
38.

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
39.

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.

40.

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.

41.

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
42.

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.

43.

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.

44.

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.

45.

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
46.

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
47.

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.

48.

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.

49.

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.

50.

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

Furness SGB, 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.

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