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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.


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.


"Selective" Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu5 Allosteric Ligands.

Hellyer SD, Albold S, Wang T, Chen ANY, May LT, Leach K, Gregory KJ.

Mol Pharmacol. 2018 May;93(5):504-514. doi: 10.1124/mol.117.111518. Epub 2018 Mar 7.


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.


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.


α1A-Adrenoceptors activate mTOR signalling and glucose uptake in cardiomyocytes.

Sato M, Evans BA, Sandström AL, Chia LY, Mukaida S, Thai BS, Nguyen A, Lim L, Tan CYR, Baltos JA, White PJ, May LT, Hutchinson DS, Summers RJ, Bengtsson T.

Biochem Pharmacol. 2018 Feb;148:27-40. doi: 10.1016/j.bcp.2017.11.016. Epub 2017 Nov 24.


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.


Targeting Adenosine Receptors for the Treatment of Cardiac Fibrosis.

Vecchio EA, White PJ, May LT.

Front Pharmacol. 2017 May 5;8:243. doi: 10.3389/fphar.2017.00243. eCollection 2017. Review.


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.


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.


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.


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.


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.


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.


The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling.

Vecchio EA, Chuo CH, Baltos JA, Ford L, Scammells PJ, Wang BH, Christopoulos A, White PJ, May LT.

Biochem Pharmacol. 2016 Oct 1;117:46-56. doi: 10.1016/j.bcp.2016.08.007. Epub 2016 Aug 9.


Sarcolemmal dependence of cardiac protection and stress-resistance: roles in aged or diseased hearts.

See Hoe LE, May LT, Headrick JP, Peart JN.

Br J Pharmacol. 2016 Oct;173(20):2966-91. doi: 10.1111/bph.13552. Epub 2016 Sep 9. Review.


VCP746, a novel A1 adenosine receptor biased agonist, reduces hypertrophy in a rat neonatal cardiac myocyte model.

Chuo CH, Devine SM, Scammells PJ, Krum H, Christopoulos A, May LT, White PJ, Wang BH.

Clin Exp Pharmacol Physiol. 2016 Oct;43(10):976-82. doi: 10.1111/1440-1681.12616.


Structure-Activity Analysis of Biased Agonism at the Human Adenosine A3 Receptor.

Baltos JA, Paoletta S, Nguyen AT, Gregory KJ, Tosh DK, Christopoulos A, Jacobson KA, May LT.

Mol Pharmacol. 2016 Jul;90(1):12-22. doi: 10.1124/mol.116.103283. Epub 2016 May 2.


Ligand-Independent Adenosine A2B Receptor Constitutive Activity as a Promoter of Prostate Cancer Cell Proliferation.

Vecchio EA, Tan CY, Gregory KJ, Christopoulos A, White PJ, May LT.

J Pharmacol Exp Ther. 2016 Apr;357(1):36-44. doi: 10.1124/jpet.115.230003. Epub 2016 Jan 20.


Quantification of adenosine A(1) receptor biased agonism: Implications for drug discovery.

Baltos JA, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT.

Biochem Pharmacol. 2016 Jan 1;99:101-12. doi: 10.1016/j.bcp.2015.11.013. Epub 2015 Nov 12.


A Positive Allosteric Modulator of the Adenosine A1 Receptor Selectively Inhibits Primary Afferent Synaptic Transmission in a Neuropathic Pain Model.

Imlach WL, Bhola RF, May LT, Christopoulos A, Christie MJ.

Mol Pharmacol. 2015 Sep;88(3):460-8. doi: 10.1124/mol.115.099499. Epub 2015 Jun 23.


An Atypical Presentation of Vaginal Agenesis.

Huguelet PS, May LT, Scott SM.

J Pediatr Adolesc Gynecol. 2015 Oct;28(5):e123-6. doi: 10.1016/j.jpag.2014.10.005. Epub 2014 Oct 24.


Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation.

Gherbi K, May LT, Baker JG, Briddon SJ, Hill SJ.

FASEB J. 2015 Jul;29(7):2859-71. doi: 10.1096/fj.14-265199. Epub 2015 Apr 2.


Synthesis and pharmacological evaluation of dual acting ligands targeting the adenosine A2A and dopamine D2 receptors for the potential treatment of Parkinson's disease.

Jörg M, May LT, Mak FS, Lee KC, Miller ND, Scammells PJ, Capuano B.

J Med Chem. 2015 Jan 22;58(2):718-38. doi: 10.1021/jm501254d. Epub 2014 Dec 24.


Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist.

Valant C, May LT, Aurelio L, Chuo CH, White PJ, Baltos JA, Sexton PM, Scammells PJ, Christopoulos A.

Proc Natl Acad Sci U S A. 2014 Mar 25;111(12):4614-9. doi: 10.1073/pnas.1320962111. Epub 2014 Mar 11.


Allosteric interactions at adenosine A(1) and A(3) receptors: new insights into the role of small molecules and receptor dimerization.

Hill SJ, May LT, Kellam B, Woolard J.

Br J Pharmacol. 2014 Mar;171(5):1102-13. doi: 10.1111/bph.12345. Review.


The apelin receptor inhibits the angiotensin II type 1 receptor via allosteric trans-inhibition.

Siddiquee K, Hampton J, McAnally D, May L, Smith L.

Br J Pharmacol. 2013 Mar;168(5):1104-17. doi: 10.1111/j.1476-5381.2012.02192.x.


Allosteric modulation of endogenous metabolites as an avenue for drug discovery.

Wootten D, Savage EE, Valant C, May LT, Sloop KW, Ficorilli J, Showalter AD, Willard FS, Christopoulos A, Sexton PM.

Mol Pharmacol. 2012 Aug;82(2):281-90. doi: 10.1124/mol.112.079319. Epub 2012 May 10.


Undifferentiated sarcoma of the liver: a single institution experience using a uniform treatment approach.

May LT, Wang M, Albano E, Garrington T, Dishop M, Macy ME.

J Pediatr Hematol Oncol. 2012 Apr;34(3):e114-6. doi: 10.1097/MPH.0b013e3182331fbe.


Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding kinetics.

May LT, Bridge LJ, Stoddart LA, Briddon SJ, Hill SJ.

FASEB J. 2011 Oct;25(10):3465-76. doi: 10.1096/fj.11-186296. Epub 2011 Jun 29.


The effect of allosteric modulators on the kinetics of agonist-G protein-coupled receptor interactions in single living cells.

May LT, Self TJ, Briddon SJ, Hill SJ.

Mol Pharmacol. 2010 Sep;78(3):511-23. doi: 10.1124/mol.110.064493. Epub 2010 Jun 22.


Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A1 receptor ligands.

Baker JG, Middleton R, Adams L, May LT, Briddon SJ, Kellam B, Hill SJ.

Br J Pharmacol. 2010 Feb;159(4):772-86. doi: 10.1111/j.1476-5381.2009.00488.x. Epub 2010 Jan 26.


Antagonist selective modulation of adenosine A1 and A3 receptor pharmacology by the food dye Brilliant Black BN: evidence for allosteric interactions.

May LT, Briddon SJ, Hill SJ.

Mol Pharmacol. 2010 Apr;77(4):678-86. doi: 10.1124/mol.109.063065. Epub 2010 Jan 19.


ERK phosphorylation: spatial and temporal regulation by G protein-coupled receptors.

May LT, Hill SJ.

Int J Biochem Cell Biol. 2008;40(10):2013-7. doi: 10.1016/j.biocel.2008.04.001. Epub 2008 Apr 6. Review.


Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.

Bisson WH, Cheltsov AV, Bruey-Sedano N, Lin B, Chen J, Goldberger N, May LT, Christopoulos A, Dalton JT, Sexton PM, Zhang XK, Abagyan R.

Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):11927-32. Epub 2007 Jul 2.


Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors.

May LT, Avlani VA, Langmead CJ, Herdon HJ, Wood MD, Sexton PM, Christopoulos A.

Mol Pharmacol. 2007 Aug;72(2):463-76. Epub 2007 May 24.


Allosteric modulation of G protein-coupled receptors.

May LT, Leach K, Sexton PM, Christopoulos A.

Annu Rev Pharmacol Toxicol. 2007;47:1-51. Review.


Effects of urea pretreatment on the binding properties of adenosine A1 receptors.

May LT, Sexton PM, Christopoulos A.

Br J Pharmacol. 2005 Dec;146(8):1119-29.


G-protein-coupled receptor allosterism: the promise and the problem(s).

Christopoulos A, May LT, Avlani VA, Sexton PM.

Biochem Soc Trans. 2004 Nov;32(Pt 5):873-7. Review.


Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators.

May LT, Lin Y, Sexton PM, Christopoulos A.

J Pharmacol Exp Ther. 2005 Jan;312(1):382-90. Epub 2004 Aug 27.


Allosteric modulation of G protein-coupled receptors.

May LT, Avlani VA, Sexton PM, Christopoulos A.

Curr Pharm Des. 2004;10(17):2003-13. Review.


Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors.

Avlani V, May LT, Sexton PM, Christopoulos A.

J Pharmacol Exp Ther. 2004 Mar;308(3):1062-72. Epub 2004 Jan 7.


Allosteric modulators of G-protein-coupled receptors.

May LT, Christopoulos A.

Curr Opin Pharmacol. 2003 Oct;3(5):551-6. Review.


Distinct classes of chaperoned IL-6 in human blood: differential immunological and biological availability.

Ndubuisi MI, Patel K, Rayanade RJ, Mittelman A, May LT, Sehgal PB.

J Immunol. 1998 Jan 1;160(1):494-501.


Interleukin-6 chaperones in blood.

May LT, Ndubuisi MI, Patel K, García D.

Ann N Y Acad Sci. 1995 Jul 21;762:120-8.


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