Cardiac G Protein-Coupled Receptor Pharmacology

Dr Lauren T. May
National Heart Foundation Future Leader Fellow
Co-Lab Head
Email: Lauren.May@monash.edu
Project areas | Key publications | Collaborations | Lab members | Funding

Project areas

Research focus

Adenosine A3 receptors (green) bound by a fluorescent antagonist (red).

Adenosine receptor stimulation represents a powerful mechanism to maintain homeostasis, resolve inflammation and promote tissue protection/repair during conditions such as inflammation and ischaemia-reperfusion injury. Unfortunately the transition of adenosine receptor ligands into the clinic has been  severely  hindered  due to high doses causing adverse effects such as bradycardia and hypotension.

New paradigms of adenosine receptor pharmacology including allosterism, dimerization and biased agonism have considerable clinical potential as they present the opportunity to develop therapeutics that promote desired, but minimize unwanted, on-target signal transduction.

The Cardiac GPCR Pharmacology laboratory aims to understand the molecular mechanisms underlying new paradigms of adenosine receptor pharmacology and investigate how these approaches can be exploited for the development of novel therapeutics. Techniques employed include fluorescent/radioligand binding, measurement  of  second  messenger formation, high-end fluorescence microscopy and ex vivo/in vivo cardiac ischaemia-reperfusion.

Adenosine Receptor Biased Agonism to Treat Ischaemic Heart Disease


In contrast to prototypical A1AR agonists, the biased agonist, VCP746, mediates cytoprotection in the absence of bradycardia.

Adenosine receptor signalling within cardiomyocytes, either during or subsequent to ischaemia-reperfusion injury, reduces infarct size and improves post-ischemic heart function. However, the transition of AR agonists into the clinic has been severely hindered due to on-target side effects like bradycardia, atrioventricular block and hypotension.

Preliminary studies of the recently identified adenosine receptor biased agonist, VCP746, suggest this compound confers potent cardioprotective and anti-remodelling effects with minimal impact on heart rate or blood pressure; enabling the separation of desired effects from adverse effects. This project will provide a mechanistic insight into VCP746 in acute and long-term models of ischaemia-reperfusion injury, cardiac remodelling and heart failure.

Studies being conducted in our laboratory will enhance the development of adenosine receptor agonists as potent cardioprotective and anti-remodelling therapeutics with an acceptable side effect profile.

Adenosine Receptor-Mediated Attenuation of Organ Transplant Rejection


Classical signalling pathways stimulated by adenosine receptors.

Allograft rejection and ischemia-reperfusion injury remains a major cause of morbidity and mortality in organ transplant recipients. Adenosine accumulates under conditions of cellular stress, including ischemia-reperfusion injury and inflammation, and mediates intracellular signal transduction through four adenosine receptors (ARs), A1AR, A2AAR, A2BAR and A3AR.

The A1AR and A2BAR typically confer cell protection through direct effects on the tissue, whereas A2AAR stimulation mediates potent anti-inflammatory effects. The aim of this study is to characterise the cytoprotective signal transduction mediated by prototypical and biased AR agonists. Studies will be performed within model systems and relevant primary cells under both control and disease conditions. Key findings will be translated into animal models of organ transplantation.

Investigating the Modulation of Adenosine A1 Receptor Mediated Cardioprotection by Adenosine A2 Receptors


The molecular mechanism underlying the modulation of A1AR-mediated cardioprotection by A2ARs may involve interactions across dimers or synergistic signal transduction.

Adenosine receptor (AR) activation represents the most powerful and well-studied cardioprotective mechanism. We have recently identified a novel A1AR signalling paradigm involved in cardioprotection. That is, an absolute requirement of coincident A2AR activation for cardioprotection mediated by prototypical A1AR selective agonists.

Although the molecular mechanisms underlying this phenomenon are currently unknown, they may involve synergistic interactions either between compartmentalized AR signalling partners or across A1AR/A2AR dimers. The current project involves investigating at a subcellular level, the influence of A2AR activation on the kinetics of A1AR ligand binding and signal transduction. A1AR-mediated signal transduction will be investigated in the absence and presence of A2AR agonists in single isolated cardiomyocytes.

Cooperative interactions between AR orthosteric binding sites will be quantified in live cells using a number of high-end fluorescence techniques. These studies will establish, for the first time, the molecular basis of A2AR modulation of A1AR-mediated cardioprotection.

Structure-function analysis of adenosine A1 receptor allosteric binding sites


A1AR homology model based on the A2AAR crystal structure. Predicted binding regions for adenosine and allosteric ligands are shown in pink and blue, respectively.

The adenosine A1 receptor (A1AR) is known to possess at least one allosteric site that can be selectively targeted by novel small molecule modulators. However, the allosteric effects of these compounds are relatively modest, highlighting the requirement for new approaches to facilitate the design of more potent, selective and efficacious A1AR modulators.

One key question in this regard is the location of the allosteric binding site on the A1AR. Structural knowledge of this binding domain can be utilized to rationally design new allosteric modulators and to inform ongoing structure-activity studies.

The current project will utilize state of the art molecular biology, molecular modelling and pharmacological techniques to probe the A1AR orthosteric and allosteric binding pockets and thus delineate the structure-function relationship underlying the modulation of this drug target by small molecules. Key findings will assist in the design of better therapeutics for the treatment of ischaemia-reperfusion and neuropathic pain.

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Key publications

Dr Lauren T. May

Research Papers

Sengmany K, Hellyer SD, Albold S, Wang T, Conn PJ, May LT, Christopoulos A, Leach K, Gregory KJ (2019) Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology. Neuropharmacology 149: 83-96

Deora GS, Qin CX, Vecchio EA, Debono AJ, Priebbenow DL, Brady RM, Beveridge J, Teguh SC, Deo M, May LT, Krippner G, Ritchie RH, Baell JB (2019) Substituted Pyridazin-3(2 H)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists. J Med Chem 62(10): 5242-5248

Sato M, Evans BA, Sandstrom 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 (2018) α1A-Adrenoceptors activate mTOR signalling and glucose uptake in cardiomyocytes. Biochem Pharmacol 148: 27-40

Miao Y, Bhattarai A, Nguyen ATN, Christopoulos A, May LT (2018) Structural Basis for Binding of Allosteric Drug Leads in the Adenosine A1 Receptor. Sci Rep 8(1): 16836

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 (2018) Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor. Proc Natl Acad Sci U S A 115(10): E2419-E2428

Hellyer SD, Albold S, Wang T, Chen ANY, May LT, Leach K, Gregory KJ (2018) "Selective" Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu5 Allosteric Ligands. Mol Pharmacol 93(5): 504-514

Goulding J, May LT, Hill SJ (2018) Characterisation of endogenous A2A and A2B receptor-mediated cyclic AMP responses in HEK 293 cells using the GloSensor biosensor: Evidence for an allosteric mechanism of action for the A2B-selective antagonist PSB 603. Biochem Pharmacol 147: 55-66

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 (2018) Structure of the adenosine-bound human adenosine A1 receptor-Gi complex. 558(7711): 559-563

Aurelio L, Baltos JA, Ford L, Nguyen ATN, Jorg M, Devine SM, Valant C, White PJ, Christopoulos A, May LT, Scammells PJ (2018) A Structure-Activity Relationship Study of Bitopic N(6)-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists. J Med Chem 61(5): 2087-2103

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 (2017) Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice. Nat Commun 8: 14232

Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jorg M, Scammells PJ, May LT, Sexton PM, Christopoulos A (2017) Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity. Cell 168(5): 867-877 e813

Baltos JA, Vecchio EA, Harris MA, Qin CX, Ritchie RH, Christopoulos A, White PJ, May LT (2017) Capadenoson, a clinically trialed partial adenosine A1 receptor agonist, can stimulate adenosine A2B receptor biased agonism. Biochem Pharmacol 135: 79-89

Vecchio EA, Tan CY, Gregory KJ, Christopoulos A, White PJ, May LT (2016) Ligand-Independent Adenosine A2B Receptor Constitutive Activity as a Promoter of Prostate Cancer Cell Proliferation. J Pharmacol Exp Ther 357(1): 36-44

Vecchio EA, Chuo CH, Baltos JA, Ford L, Scammells PJ, Wang BH, Christopoulos A, White PJ, May LT (2016) The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. Biochem Pharmacol 117: 46-56

Nguyen AT, Vecchio EA, Thomas T, Nguyen TD, Aurelio L, Scammells PJ, White PJ, Sexton PM, Gregory KJ, May LT, Christopoulos A (2016) Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity. Mol Pharmacol 90(6): 715-725

Nguyen AT, Baltos JA, Thomas T, Nguyen TD, Munoz LL, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT (2016) Extracellular Loop 2 of the Adenosine A1 Receptor Has a Key Role in Orthosteric Ligand Affinity and Agonist Efficacy. Mol Pharmacol 90(6): 703-714

Jorg M, Glukhova A, Abdul-Ridha A, Vecchio EA, Nguyen AT, Sexton PM, White PJ, May LT, Christopoulos A, Scammells PJ (2016) Novel Irreversible Agonists Acting at the A1 Adenosine Receptor. J Med Chem 59(24): 11182-11194

Chuo CH, Devine SM, Scammells PJ, Krum H, Christopoulos A, May LT, White PJ, Wang BH (2016) VCP746, a novel A1 adenosine receptor biased agonist, reduces hypertrophy in a rat neonatal cardiac myocyte model. Clin Exp Pharmacol Physiol 43(10): 976-982

Baltos JA, Paoletta S, Nguyen AT, Gregory KJ, Tosh DK, Christopoulos A, Jacobson KA, May LT (2016) Structure-Activity Analysis of Biased Agonism at the Human Adenosine A3 Receptor. Mol Pharmacol 90(1): 12-22

Baltos JA, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT (2016) Quantification of adenosine A(1) receptor biased agonism: Implications for drug discovery. Biochem Pharmacol 99: 101-112

Jorg M, May LT, Mak FS, Lee KC, Miller ND, Scammells PJ, Capuano B (2015) Synthesis and pharmacological evaluation of dual acting ligands targeting the adenosine A2A and dopamine D2 receptors for the potential treatment of Parkinson's disease. J Med Chem 58(2): 718-738

Imlach WL, Bhola RF, May LT, Christopoulos A, Christie MJ (2015) A Positive Allosteric Modulator of the Adenosine A1 Receptor Selectively Inhibits Primary Afferent Synaptic Transmission in a Neuropathic Pain Model. Mol Pharmacol 88(3): 460-468

Gherbi K, May LT, Baker JG, Briddon SJ, Hill SJ (2015) Negative cooperativity across beta1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 beta1-adrenoceptor binding conformation. FASEB J 29(7): 2859-2871

Valant C, May LT*, Aurelio L, Chuo CH, White PJ, Baltos JA, Sexton PM, Scammells PJ, Christopoulos A (2014) Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Proc Natl Acad Sci U S A 111(12): 4614-4619. *Co-First Author

Hill SJ, May LT, Kellam B, Woolard J (2014) Allosteric interactions at adenosine A(1) and A(3) receptors: new insights into the role of small molecules and receptor dimerization. Br J Pharmacol 171(5): 1102-1113

Siddiquee K, Hampton J, McAnally D, May LT, Smith LH (2013) The apelin receptor inhibits the angiotensin II type 1 receptor via allosteric trans-inhibition. Br J Pharmacol 168:1104-17

Wootten D, Savage EE, Valant C, May LT, Sloop KW, Ficorilli J, Showalter AD, Willard FS, Christopoulos A, Sexton P (2012) Allosteric modulation of endogenous metabolites as an avenue for drug discovery. Mol Pharmacol 82:281-90

May LT, Bridge LJ, Stoddart LA, Briddon SJ, Hill SJ (2011) Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding kinetics. FASEB J 25:3465-76

May LT, Self TJ, Briddon SJ, Hill SJ (2010) The effect of allosteric modulators on the kinetics of agonist-G protein-coupled receptor interactions in single living cells. Mol Pharmacol 78:511-23

May LT, Briddon SJ, Hill SJ (2010) Antagonist selective modulation of adenosine –A1 and –A3 receptor pharmacology by Brilliant Black BN: Evidence for allosteric interactions. Mol Pharmacol 77:678-86

May LT, Avlani VA, Langmead CJ, Herdon HJ, Wood MJ, Sexton PM and Chistopoulos A (2007) Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors. Mol Pharmacol 72:463-76

Bisson WH and Cheltsov AV, Bruey-Sedano N, Lin B, Chen J, Goldberger N, May  LT, Christopoulos A, Dalton JT, Sexton PM, Zhang XK, Abagyan R. (2007) Discovery of Antiandrogen Activity of Non-steroidal Scaffolds of Marketed Drugs. Proc Natl Acad Sci U.S.A. 104:11927-32

May LT, Sexton PM and Christopoulos A (2005) Effects of urea pretreatment on the binding properties of adenosine A1 receptors. British Journal of Pharmacology 146:1119-29.

May LT, Lin Y, Sexton PM and Christopoulos A (2005) Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators. J Pharmacol Exp Ther 312:382-90.

Review Papers

Vecchio EA, White PJ, May LT (2019) The adenosine A2B G protein-coupled receptor: Recent advances and therapeutic implications. Pharmacol Ther 198: 20-33

Vecchio EA, Baltos JA, Nguyen ATN, Christopoulos A, White PJ, May LT (2018) New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism. Br J Pharmacol 175(21): 4036-4046

Trinh PNH, May LT, Leach K, Gregory KJ (2018) Biased agonism and allosteric modulation of metabotropic glutamate receptor 5. Clin Sci (Lond) 132(21): 2323-2338

Vecchio EA, White PJ, May LT (2017) Targeting Adenosine Receptors for the Treatment of Cardiac Fibrosis. Front Pharmacol 8: 243

Lane JR, May LT, Parton RG, Sexton PM, Christopoulos A (2017) A kinetic view of GPCR allostery and biased agonism. Nat Chem Biol 13(9): 929-937

See Hoe LE, May LT, Headrick JP, Peart JN (2016) Sarcolemmal dependence of cardiac protection and stress-resistance: roles in aged or diseased hearts. Br J Pharmacol 173(20): 2966-2991

Hill SJ, May LT, Kellam B, Woolard J (2014) Allosteric interactions at adenosine A1 and A3 receptors: New insights into the role of small molecules and receptor dimerization. British Journal of Pharmacology 171:1102-1113

Hill SJ, Williams C, May LT (2010) Insights into GPCR pharmacology from the measurement of changes in intracellular cyclic AMP; Advantages and pitfalls of differing methodologies. British Journal of Pharmacology 161:1266-75

May LT, Holliday ND, Hill, SJ (2010) The Evolving Pharmacology of GPCRs. GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms in G Protein Coupled Receptors. Chapter 2:27-60

May LT, Hill SJ (2008) ERK phosphorylation: Spatial and temporal regulation by G protein-coupled receptors. Int J Biochem Cell Biol 40:2013-7

May LT, Leach K, Sexton PM and Christopoulos A (2007) Allosteric Modulation of G Protein-Coupled Receptors. Annu Rev Pharmacol Toxicol. 47:1-51

Associate Professor Paul J. White

Research Papers

Sato M, Evans BA, Sandstrom 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 (2018) α1A-Adrenoceptors activate mTOR signalling and glucose uptake in cardiomyocytes. Biochem Pharmacol 148: 27-40

Aurelio L, Baltos JA, Ford L, Nguyen ATN, Jorg M, Devine SM, Valant C, White PJ, Christopoulos A, May LT, Scammells PJ (2018) A Structure-Activity Relationship Study of Bitopic N(6)-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists. J Med Chem 61(5): 2087-2103

Baltos JA, Vecchio EA, Harris MA, Qin CX, Ritchie RH, Christopoulos A, White PJ, May LT (2017) Capadenoson, a clinically trialed partial adenosine A1 receptor agonist, can stimulate adenosine A2B receptor biased agonism. Biochem Pharmacol 135: 79-89

Vecchio EA, Tan CY, Gregory KJ, Christopoulos A, White PJ, May LT (2016) Ligand-Independent Adenosine A2B Receptor Constitutive Activity as a Promoter of Prostate Cancer Cell Proliferation. J Pharmacol Exp Ther 357(1): 36-44

Vecchio EA, Chuo CH, Baltos JA, Ford L, Scammells PJ, Wang BH, Christopoulos A, White PJ, May LT (2016) The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. Biochem Pharmacol 117: 46-56

Nguyen AT, Vecchio EA, Thomas T, Nguyen TD, Aurelio L, Scammells PJ, White PJ, Sexton PM, Gregory KJ, May LT, Christopoulos A (2016) Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity. Mol Pharmacol 90(6): 715-725

Nguyen AT, Baltos JA, Thomas T, Nguyen TD, Munoz LL, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT (2016) Extracellular Loop 2 of the Adenosine A1 Receptor Has a Key Role in Orthosteric Ligand Affinity and Agonist Efficacy. Mol Pharmacol 90(6): 703-714

Jorg M, Glukhova A, Abdul-Ridha A, Vecchio EA, Nguyen AT, Sexton PM, White PJ, May LT, Christopoulos A, Scammells PJ (2016) Novel Irreversible Agonists Acting at the A1 Adenosine Receptor. J Med Chem 59(24): 11182-11194

Chuo CH, Devine SM, Scammells PJ, Krum H, Christopoulos A, May LT, White PJ, Wang BH (2016) VCP746, a novel A1 adenosine receptor biased agonist, reduces hypertrophy in a rat neonatal cardiac myocyte model. Clin Exp Pharmacol Physiol 43(10): 976-982

Baltos JA, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT (2016) Quantification of adenosine A(1) receptor biased agonism: Implications for drug discovery. Biochem Pharmacol 99: 101-112

Jin L, Boyd BJ, White PJ, Pennington MW, Norton RS, Nicolazzo JA (2015) Buccal mucosal delivery of a potent peptide leads to therapeutically-relevant plasma concentrations for the treatment of autoimmune diseases. J Control Release 199:37-44.

Valant C, May LT*, Aurelio L, Chuo C, White PJ, Baltos J, Sexton PM, Scammells PJ, Christopoulos A (2014) Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Proc Natl Acad Sci U S A 111(12): 4614-4619 *Co-First Author

Lau S, Graham B, Cao N, Boyd BJ, Pouton CW, White PJ (2012) Enhanced extravasation, stability and in vivo cardiac gene silencing via in situ siRNA-albumin conjugation. Mol Pharmaceutics 9(1):71-80

Hausler NE, Devine SM, McRobb FM, Warfe L, Pouton CW, Haynes JM, White PJ, Scammells PJ* (2012) Synthesis and pharmacological evaluation of dual acting antioxidant A(2A) adenosine receptor agonists. J Med Chem 55(7):3521-34.

Valant C, Aurelio L, Urmaliya VB, White PJ, Scammells PJ, Sexton PM, et al. (2010) Delineating the mode of action of adenosine A1 receptor allosteric modulators. Mol Pharmacol 78(3):444-55

Urmaliya VB, Pouton CW, Ledent C, Short JL, White PJ (2010) Cooperative cardioprotection through adenosine A1 and A2A receptor agonism in ischemia-reperfused isolated mouse heart. J Cardiovascular Pharmacol 56(4):379-88

Urmaliya VB, Pouton CW, Devine SM, Haynes JM, Warfe L, Scammells PJ, White PJ. (2010) A novel highly selective adenosine A1 receptor agonist VCP28 reduces ischemia injury in a cardiac cell line and ischemia-reperfusion injury in isolated rat hearts at concentrations that do not affect heart rate. J Cardiovascular Pharmacol 56(3):282-292

Urmaliya VB, Church JE, Coupar IM, Rose'Meyer RB, Pouton CW, White PJ. (2009) Cardioprotection induced by adenosine A1 receptor agonists in a cardiac cell ischemia model involves cooperative activation of adenosine A2A and A2B receptors by endogenous adenosine. J Cardiovascular Pharmacol 53(5):424-33

White PJ, Anastasopoulos F, Church JE, Kuo CY, Boyd BJ, Hickey PL, et al. (2008) Generic construction of single component particles that elicit humoural and cellular immune responses without the need for adjuvants. Vaccine 26(52):6824-31

Nguyen TT, Cao N, Short JL, White PJ. (2006) Intravenous insulin-like growth factor-I receptor antisense treatment reduces angiotensin receptor expression and function in spontaneously hypertensive rats. J Pharmacol Exp Ther 318(3):1171-7

Wraight CJ, White PJ, McKean SC, Fogarty RD, Venables DJ, Liepe IJ, et al. (2000) Reversal of epidermal hyperproliferation in psoriasis by insulin-like growth factor I receptor antisense oligonucleotides. Nat Biotechnol. 18(5):521-6

Review Papers

Vecchio EA, White PJ, May LT (2019) The adenosine A2B G protein-coupled receptor: Recent advances and therapeutic implications. Pharmacol Ther 198: 20-33

Vecchio EA, Baltos JA, Nguyen ATN, Christopoulos A, White PJ, May LT (2018) New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism. Br J Pharmacol 175(21): 4036-4046

Vecchio EA, White PJ, May LT (2017) Targeting Adenosine Receptors for the Treatment of Cardiac Fibrosis. Front Pharmacol 8: 243

White PJ, Anastasopoulos F, Pouton CW, Boyd BJ. (2009) Overcoming biological barriers to in vivo efficacy of antisense oligonucleotides. Exp Rev Mol Med 11:e10

White PJ. Barriers to successful delivery of short interfering RNA after systemic administration. (2008) Clin Exper Pharmacol Physiol 35(11):1371-6

White PJ, Atley LM, Wraight CJ. (2004) Antisense oligonucleotide treatments for psoriasis. Exp Opinion Biol Therapy 4(1):75-81

Wraight CJ, White PJ (2001) Antisense oligonucleotides in cutaneous therapy. Pharmacol Ther 90(1):89-104

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Collaborations

Adenosine Receptor Biased Agonism to Treat Ischaemic Heart Disease (LTM & PJW)

  • Prof  Peter Scammells, Medicinal Chemistry and Drug Action, MIPS, Monash University
  • Prof  Arthur Christopoulos, Drug Discovery Biology, MIPS, Monash University
  • Prof  Patrick Sexton, Drug Discovery Biology, MIPS, Monash University
  • Prof Henry Krum, Department of Epidemiology & Preventive Medicine, Monash University
  • Dr Bing Wang, Department of Epidemiology & Preventive Medicine, Monash University
  • Dr Andrew Kompa, Department of Epidemiology & Preventive Medicine, Monash University

Structure-function analysis of allosteric binding sites on adenosine A1 receptors (LTM)

  • Prof  Arthur Christopoulos, Drug Discovery Biology, MIPS, Monash University
  • Dr Laura Lopez, Drug Discovery Biology, MIPS, Monash University

VCP746, a novel adenosinergic therapeutic, promotes beta-cell regeneration (LTM)

  • Dr Karen Dwyer, St. Vincent's Hospital, Immunology Research Centre

Novel GPCR mechanisms to treat neural hyper-excitation in chronic pain (LTM)

  • Professor Macdonald Christie, Pharmacology, School of Medical Sciences, The University of Sydney
  • Prof  Arthur Christopoulos, Drug Discovery Biology, MIPS, Monash University

GPCR regulation, trafficking and compartmentalisation in breast cancer metastasis (LTM)

Formyl peptide receptor signal transduction (LTM)

  • A/Prof Rebecca Ritchie, Heart Failure Pharmacology, Baker IDI Heart & Diabetes Institute
  • Chengxue Helena Qin, Heart Failure Pharmacology, Baker IDI Heart & Diabetes Institute
  • Prof  Arthur Christopoulos, Drug Discovery Biology, MIPS, Monash University
  • Prof  Patrick Sexton, Drug Discovery Biology, MIPS, Monash University
  • Adenosine Receptor-Mediated Attenuation of Organ Transplant Rejection (LTM)
  • Professor Robert Jones, Liver Transplant Unit Director, Austin Hospital

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Lab members

Dr Anh T. Nguyen
Research Fellow

Dr Jo-Anne Baltos
Research Fellow

Dr Ling Yeong Chia
Research Fellow

Sam McNeill
PhD Candidate

Bui San Thai
PhD Candidate

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Funding

Dr Lauren T. May

  • National Heart Foundation Future Leader Fellowship (2018 – 2024) "G Protein-Coupled Receptor Context-Specific Biased Agonism to Treat Ischaemic Heart Disease"
  • CI, NHMRC Project Grant (2018 – 2020) "Adenosine Receptor Context-Specific Biased Agonism to Treat Ischaemic Heart Disease"
  • CI, NHMRC Project Grant (2018 – 2022) "Adenosine A1 receptor modulation: Structure, dynamics & novel pharmacological interventions"
  • CI, NHMRC Project Grant (2017 – 2019) "Investigating the impact of coincident modulation of adenosine and glutamate receptors on neuronal activity - implications for CNS drug discovery"
  • CI, NHMRC Project Grant (2015 – 2017) "Adenosine Receptor Biased Agonism to Treat Ischaemic Heart Disease"
  • CI, NHMRC Project Grant (2015 – 2017) "Understanding mechanisms of allostery and biased agonism at the adenosine A1 receptor"
  • ARC DECRA Fellowship (2013 – 2016) "Allosteric Fingerprinting of G Protein-Coupled Receptor Monomers and Oligomers"
  • Co-PI, JDRF Project Grant (2013 – 2014) "VCP746, a novel adenosinergic therapeutic, promotes beta-cell regeneration"

Associate Professor Paul J White

  • CI, NHMRC Project Grant (2018 – 2020) "Adenosine Receptor Context-Specific Biased Agonism to Treat Ischaemic Heart Disease"
  • CI, NHMRC Project Grant (2015 – 2017) "Adenosine Receptor Biased Agonism to Treat Ischaemic Heart Disease"

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