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THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Introduction and Other Protein Targets.

Alexander SP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, 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. 2019 Dec;176 Suppl 1:S1-S20. doi: 10.1111/bph.14747.


THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors.

Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators.

Br J Pharmacol. 2019 Dec;176 Suppl 1:S21-S141. doi: 10.1111/bph.14748.


Evaluation of operational models of agonism and allosterism at receptors with multiple orthosteric binding sites.

Gregory KJ, Giraldo J, Daio J, Christopoulos A, Leach K.

Mol Pharmacol. 2019 Nov 8. pii: mol.119.118091. doi: 10.1124/mol.119.118091. [Epub ahead of print]


Rapid head and neck tissue identification in thyroid and parathyroid surgery using optical coherence tomography.

Yang N, Boudoux C, De Montigny E, Maniakas A, Gologan O, Madore WJ, Khullar S, Guertin L, Christopoulos A, Bissada E, Ayad T.

Head Neck. 2019 Oct 1. doi: 10.1002/hed.25972. [Epub ahead of print]


Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole.

Klein Herenbrink C, Verma R, Lim HD, Kopinathan A, Keen A, Shonberg J, Draper-Joyce CJ, Scammells PJ, Christopoulos A, Javitch JA, Capuano B, Shi L, Lane JR.

ACS Chem Biol. 2019 Aug 16;14(8):1780-1792. doi: 10.1021/acschembio.9b00342. Epub 2019 Aug 5.


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.


Cystic masses of the lateral neck: Diagnostic value comparison between fine-needle aspiration, core-needle biopsy, and frozen section.

Tabet P, Saydy N, Letourneau-Guillon L, Gologan O, Bissada É, Ayad T, Tabet JC, Guertin L, Nguyen-Tan PF, Christopoulos A.

Head Neck. 2019 Aug;41(8):2696-2703. doi: 10.1002/hed.25755. Epub 2019 Apr 4.


Unusual presentation for small lymphocytic lymphoma: Case report of a man with bilateral ear involvement and review of the literature.

Tram Do B, Charpentier AM, Bourré-Tessier J, Maietta A, Doucet S, Ayad T, Christopoulos A.

Eur Ann Otorhinolaryngol Head Neck Dis. 2019 Jun;136(3S):S45-S47. doi: 10.1016/j.anorl.2018.10.017. Epub 2019 Mar 15.


Free versus pedicled flaps for reconstruction of head and neck cancer defects: a systematic review.

Gabrysz-Forget F, Tabet P, Rahal A, Bissada E, Christopoulos A, Ayad T.

J Otolaryngol Head Neck Surg. 2019 Mar 14;48(1):13. doi: 10.1186/s40463-019-0334-y. Review.


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.


Parry-Romberg syndrome treatment with fat transfer and a new bleaching formula.

Liapakis IE, Tzouganakis AC, Paschalis EI, Englander M, Christopoulos A, Gloustianou G, Kontoes P.

J Cosmet Dermatol. 2019 Feb 15. doi: 10.1111/jocd.12819. [Epub ahead of print]


Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology.

Sengmany K, Hellyer SD, Albold S, Wang T, Conn PJ, May LT, Christopoulos A, Leach K, Gregory KJ.

Neuropharmacology. 2019 May 1;149:83-96. doi: 10.1016/j.neuropharm.2019.02.005. Epub 2019 Feb 11.


Phase I/II trial of Durvalumab plus Tremelimumab and stereotactic body radiotherapy for metastatic head and neck carcinoma.

Bahig H, Aubin F, Stagg J, Gologan O, Ballivy O, Bissada E, Nguyen-Tan FP, Soulières D, Guertin L, Filion E, Christopoulos A, Lambert L, Tehfe M, Ayad T, Charpentier D, Jamal R, Wong P.

BMC Cancer. 2019 Jan 14;19(1):68. doi: 10.1186/s12885-019-5266-4.


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.


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.


Structural Basis for Binding of Allosteric Drug Leads in the Adenosine A1 Receptor.

Miao Y, Bhattarai A, Nguyen ATN, Christopoulos A, May LT.

Sci Rep. 2018 Nov 15;8(1):16836. doi: 10.1038/s41598-018-35266-x.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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/ Epub 2018 Mar 13. Review.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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