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Professor Arthur Christopoulos

Professor Arthur Christopoulos

CURRENT POSITIONS

Professor of Pharmacology
NHMRC Senior Research Fellow
Head, Drug Discovery Biology Laboratory

ADDRESS

Drug Discovery Biology Laboratory
Department of Pharmacology
Monash University
Clayton, Victoria, 3800
Australia
Ph: +613 9905 1146
Fax: +613 9905 9500
Email: arthur.christopoulos@med.monash.edu.au


Overview


EDUCATION

1990Bachelor of Pharmacy (Victorian College of Pharmacy, Monash University)
19971997 Doctor of Philosophy (Victorian College of Pharmacy, Monash University); Thesis title: “Allosteric Interactions at Muscarinic Acetylcholine Receptors”


RESEARCH FOCUS

The principal direction of our laboratory is towards understanding novel modes of regulation of GPCRs in an effort to identify novel targets or approaches for drug discovery. Our work encompasses investigation across virtually all levels of GPCR structure/function, including analysis of the functional significance of single nucleotide polymorphisms, RNA-editing and alternate mRNA splicing; signaling via G proteins and downstream messenger systems; interaction of receptors with regulatory accessory proteins; novel allosteric GPCR binding sites, and mathematical and molecular modeling of GPCR-ligand interactions

Drug Discovery Biology


IN THE NEWS

2003 Invitrogen Award winner: Dr. Arthur Christopoulos (COMBIO 2003)

2002 Victorian Young Tall Poppy Award (Australian Institute of Political Science)

Faculty of 1000 Biology | Faculty member: Arthur Christopoulos

Pharmacologist named 2007 visitor to British Pharmacological Society

Professor Christopoulos: Bright Sparks Award Winner


AWARDS

1991 Cyril Tonkin Postgraduate Research Scholarship (Victorian College of Pharmacy, Monash University, Australia)
1999 Johnson & Johnson New Investigator Award (Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists; ASCEPT)
2000 C.R. Roper Research Fellowship, Faculty of Medicine, Dentistry and Health Sciences, University of Melbourne, Australia
2002 Victorian Young Tall Poppy Award (Australian Institute of Political Science)
2002 International Union of Pharmacology (IUPHAR) Young Investigator Award (2nd Place), awarded at the 14th World Congress of Pharmacology, San Francisco, July, 2002
2003 National Health and Medical Research Council of Australia Senior Research Fellowship (Level A)
2003 Invitrogen Life Science Award, awarded at ComBio 2003, the annual meeting of the Australian Society of Biochemistry and Molecular Biology, Melbourne.
2005 National Health and Medical Research Council of Australia Senior Research Fellowship (Level B)
2007 ASCEPT Visitor to the British Pharmacological Society (Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists)
2007 Cosmos Magazine Bright Sparks Award


CURRENTLY HELD GRANTS

2009 - 2013: P.M. Sexton, A. Christopoulos, and R.J. Summers, "Understanding G protein coupled receptors: Accelerating discovery from concept to clinic", National Health and Medical Research Council of Australia Program Grant ID No 519461.
2008 - 2012: A. Christopoulos, National Health and Medical Research Council of Australia Senior Research Fellowship (Level B) ID No 491112.
2008 - 2010: P.J. Scammells, A. Christopoulos and B. Flynn, "Allosteric modulators as novel probes of G protein-coupled receptor function" Australian Research Council Discovery Grant ID No DP0877497.
2007 - 2009: P.M. Sexton, A. Christopoulos and A. Tobin, “Understanding selective drug signalling at G protein-coupled receptors” National Health and Medical Research Council of Australia Project Grant ID No 436779.
2007 - 2009: P.M. Sexton, A. Christopoulos and J. Simms, “Molecular characterisation of receptor activity modifying proteins (RAMPs)”, National Health and Medical Research Council of Australia Project Grant ID No 436781.
2006 - 2008: A. Christopoulos, P.M. Sexton, A. Tobin and R. Abagyan, “Allosteric regulation of G protein-coupled receptors”, National Health and Medical Research Council of Australia Project Grant ID No 400134.
2006 - 2008: A. Christopoulos and P.M. Sexton, “Novel modes of regulating serotonin 5HT2C receptors”, National Health and Medical Research Council of Australia Project Grant ID No 400133.
2005 - 2008: A. Christopoulos, P.M. Sexton and M.F. Crouch, Australian Research Council Linkage Grant, “Novel modes of signalling of serotonin 5HT2 receptors”, ID No. LP0562257.


CURRENTLY HELD CONTRACT RESEARCH AGREEMENTS

2008: A. Christopoulos and P.M. Sexton, "Investigating the mechanism of action of GPCR allosteric modulators/agonists and assay development", contract with GlaxoSmithKline Australia Pty Ltd.


CURRENT COLLABORATORS

Prof. Patrick Sexton Dept. of Pharmacology, Monash University, Melbourne, Australia
Prof. Roger Summers
Dept. of Pharmacology, Monash University, Melbourne, Australia
Prof. Peter J. Scammells Dept. of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, Melbourne, Australia
Prof. Andrew Tobin University of Leicester, UK
Prof. Ruben Abagyan Scripps Research Institute, USA
Dr Harvey J. Motulsky GraphPad Software, San Diego, CA, USA
Dr. Martyn Wood GlaxoSmithKline, Harlow, United Kingdom
Dr Christian Felder Eli Lilly, Indianapolis, USA


CURRENT PROFESSIONAL AFFILIATIONS

2003 – Present:Member of the National Association of Research Fellows
2002 – Present:Member of the Serotonin Club
2000 – Present:Member of the Australian Society for Medical Research
1999 – Present:Member of the American Society of Pharmacology and Experimental Therapeutics
1996 – Present:Member of the Society For Neuroscience
1996 – Present:Member of the International Brain Research Organization
1995 – 2004:Member of the New York Academy of Sciences
1990 – Present:Member of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists
1990 – Present:Member of the Pharmaceutical Society of Australia


PROFESSIONAL ACTIVITIES

Company Director:

2005 - 2006: DKR Pharma, Pty. Ltd., (ACN/ABN 117 650 405)

Consultancies:

1998 - Present: GraphPad Software (PRISM, InStat, StatMate), San Diego, CA, USA.
1999 - 2002: AMRAD Australia, Pty, Ltd, Pharmaceutical R &D Company
2001 - 2004: “Today/Tonight”, Australian current affairs/news television program
2005 - 2006: Consultant & Scientific Advisory Board Member, Novasite Pharmaceuticals, USA
2005 - Present: Consultant & Scientific Advisory Board Member, Addex Pharmaceuticals, Switzerland
2007: Consultant & Scientific Advisory Board Member, Caden Biosciences, USA
2007 - Present: Consultant & Scientific Advisory Board Member, Alchemia Ltd., Australia
2006 - Present: AMGEN Inc., USA
2006 - Present: Bristol Myers Squibb, USA

Editorial Boards:

2006 - Present: Board Member of the international journal, “Molecular Pharmacology”
2006 - Present: Board Member of the international journal, “Pharmacology & Therapeutics”
2005 - Present: Board Member of the international journal, “Journal of Receptors and Signal Transduction”
2004 - Present: Board Member of the international journal, “Clinical and Experimental Pharmacology and Physiology”
2001 - 2004: Board Member of the international journal, “Receptors and Channels”

Guest Editorial Positions:

2001 - 2004: Guest Editor of Special Issues of “Receptors and Channels”
2002 - 2004: Guest Editor of Special Issues of the international journal, “Mini-reviews in Medicinal Chemistry”
2003 - 2005: Executive Guest Editor of the international journal “Current Pharmaceutical Design”

Other Editorial Positions:

2006 - Present: Faculty of 1000 Biology. Faculty member of Pharmacology and Drug Discovery (Molecular Pharmacology Section)

Committee Memberships:

2008: Member of NHMRC Grant Review Panel (GRP) 6b
2007: Corresponding Member of the Nomenclature Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR).
2007: Councillor (Rest of the World), Serotonin Club
2007: Member of the Monash School of Biomedical Sciences Executive Research Consultative Group
2005 - 2006: Chair of the NHMRC Scholarships (Training Awards) Biomed Panel 2
2004: Member of the NHMRC Biomedical Postgraduate Research Scholarships (Training Awards) Panel
2004 - 2005: Chair of the National Scientific Advisory Committee for the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists (ASCEPT)
2002 - 2003: Member of the National Scientific Advisory Committee for the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists (ASCEPT)
2003 - 2004: Councillor of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists (ASCEPT), “Education and Training” portfolio
2003 Member of the Executive Committee of the Department of Pharmacology, University of Melbourne

Pharmacy Practice:

1995 - 2003: Pharmacist Continuing Education Lecturer, Pharmaceutical Society of Australia


CURRENT TEACHING RESPONSIBILITIES

2007 – Present: Unit Co-ordinator, 3rd Year Science (Monash University) PHAR 3042 “Modern drug development”.
2006 - Present: 4th Year Science (Monash University) Pharmacology Honours Course - 1 Lecture “Receptor Agonism”.
2006 - Present: 4th Year Science (Monash University) Pharmacology Honours Course - 1 Lecture “Receptor Antagonism”.
2006 - Present:

3rd Year Science (Monash University) Pharmacology PHA3042 Drug Discovery and Development - 1 Lecture “Drug Targets”.
3rd Year Science (Monash University) Pharmacology PHA3042 Drug Discovery and Development - 1 Lecture “Allosteric Drugs”.


GRADUATE AND POSTGRADUATE SUPERVISION

B. Sci. Hons, University of Melbourne

2000 Yvonne Lin, “Regulation of muscarinic receptor trafficking by allosteric modulators” (awarded H2A).
2001 Olivia M. Ryan, “Analysis of functional cross talk between prejunctional receptors in the guinea pig myenteric plexus” (awarded H1; Dux of year).
2002 Nicola Smith, “Regulation of the serotonin 5HT2C receptor by agonists and antagonists” (awarded H1).
2002 Lauren May “Effects of allosteric modulators on M2 muscarinic acetylcholine receptor trafficking” (awarded H1).
2004 Karen Gregory “Signaling of RNA-Edited 5HT2C receptors” (awarded H1; Dux of year).

B. Sci. Hons, Monash University

2007 Oshadhi Nawartne “Pharmacology of DREADDs”. (awarded H1; Dux of year)
2008 Anna Davey “Structure-function studies of M4 muscarinic receptors”.
2008 David George “Cellular and behavioural effects of a novel class of antipsychotic”.

Higher Degrees, University of Melbourne

1999 - 2003 Mark G. Devlin “Regulation of cannabinoid CB1 and serotonin 5-HT2 receptors”.
2000 - 2003 Alfred A. Lanzafame “Neuromodulation of muscarinic acetylcholine receptors”.
2002 - 2006 Vimesh Avlani “Molecular mechanisms of M2 muscarinic acetylcholine receptor modulators”.
2003 - 2007 Lauren May “Allosteric modulation of G protein-coupled receptors”.

Higher Degrees, Monash University

2005 - Karen Gregory “Allosteric modulation of GPCRs” (PhD in Progress).
2006 - Gregory Stewart “Novel modes of regulation serotonin 5HT2C receptors” (PhD in Progress).


NATIONAL AND INTERNATIONAL PRESENTATIONS SINCE 2005

International

Invited Plenary Presentations

1. “New tricks for old dogs: Allosteric modulation of G protein-coupled receptors”, invitation to speak at the Life Sciences 2007 Meeting, July 8th-12th, 2007, Glasgow, United Kingdom.

Invited Keynote Presentations

1. “The potential of allosteric modulation for GPCR drug discovery”, invitation to deliver keynote address at the 20th International Symposium on Medicinal Chemistry (EFMC-ISMC 2008) Vienna, Austria, August 31st - Sept 4th, 2008.

Invited Presentations at Symposia: (of 17 total)

1. “Allosterism and drug discovery”, invitation to speak at EPHAR 2008, July 13-17th, 2008, Manchester, United Kingdom.
2. “Topography in drug discovery:  The challenge of allosteric modulators”, Experimental Biology 2008, April 9th, 2008, San Diego, United States.
3. “Structure-function meets ligand-directed modeling: Towards novel muscarinic receptor chemotypes”, international Experimental Biology satellite meeting, "Recent Advances in Muscarinic Receptor Pharmacology and Therapeutics", San Diego, CA, April 5th, 2008.
4. “The many faces of allosteric modulation of GPCRs”, invitation to speak at the IBRO World Congress, July 12-17th, 2007, Melbourne, Australia.
5. “Allosteric modulation of GPCRs: Expanding the pharmacological toolbox”, Invitation to speak at the British Pharmacological Society Cell Signalling Meeting, April 16th - 17th, 2007, Leicester, United Kingdom.
6. “Allosteric GPCR modulators: Expanding the pharmacological toolbox”, International Symposium of the University of Bonn Graduate College, September 26th, 2006, Bonn, Germany.
7. “GPCR allosterism: A novel approach to drug selectivity”. Symposium: “Frontiers in G Protein-Coupled Receptor Research” at the 15th World Congress of Pharmacology (IUPHAR 2006), July 3rd, 2006, Beijing, China.
8. “Non-classical modes of signaling by serotonin 5HT2C receptors”. Annual meeting of the Serotonin Club, Sapporo, Japan, June 30, 2006.
9. “Screening for Allosteric Modulators of GPCRs”. Symposium “Novel approaches to GPCR targets” at the BIO 2006 Meeting, April 12th, 2006, Chicago, McCormick Place Convention Center.
10. “The Pros and Cons of allosteric modulators of GPCRs”. Symposium “Allosteric Modulators of GPCRs: From small molecules to accessory proteins” at the Experimental Biology 2006 (FASEB) Meeting, April 5th, 2006, San Francisco, Moscone Convention Center.
11. “Message in a model: Receptor theory as a tool for studying functional selectivity” Invitation to speak at the Symposium ”The Ten Commandments of Pharmacology: Does Functional Selectivity/Agonist Trafficking Make Nothing Sacred?” at the Experimental Biology 2005 (FASEB) Meeting, April 5th, 2005, San Diego Convention Center.

Session Chairs:

1. “Allosteric Modulators of GPCRs: From small molecules to accessory proteins” at the Experimental Biology 2006 (FASEB) Meeting, April 5th, 2006, San Francisco, Moscone Convention Center.

Invited Seminars (of 26 total):

1. “The challenge of understanding allosteric sites on G protein-coupled receptors”, Bristol Myers Squibb, Princeton, New Jersey, April 19th, 2008.
2. “The challenge of understanding allosteric sites on G protein-coupled receptors”, Eli Lilly Research Laboratories, Indianapolis, Indiana, April 18th, 2008.
3. “The role of topography in drug discovery: Exploiting allosteric sites on G protein-coupled receptors”, invited seminar in the Department of Pharmacology, Vanderbilt University, Tennessee, April 15th, 2008.
4. “Topography in drug discovery: Exploiting allosteric sites on G protein-coupled receptors”, Department of Pharmacology, University of Minnesota, Minneapolis, March 28th, 2008.
5. “Allosterically engendering novel GPCR phenotypes”, invited seminar at the University of Reading School of Pharmacy, June 29th, 2007.
6. “Allosterically engendering novel GPCR phenotypes”, invited seminar at the University of Aberdeen Institute of Medical Sciences, July 5th, 2007.
7. “Allosteric modulation of GPCRs”, invited seminar at the Institute for Functional Genomics, Montpellier, France, April 10th, 2007.
8. “Analytical pharmacology in the new millennium”, invited presentation to the Nomencalture Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), Paris, France, April 14th, 2007.
9. “Recent advances in the study of GPCR allosterism”, invited seminar at GlaxoSmithKline, Harlow, UK, April 18th, 2007.
10. “GPCR allosteric modulators and drug discovery”, invited seminar at Pfizer, Sandwich, UK, April 20th, 2007.
11. “'Complex' pharmacology: Allosterically engendering novel GPCR phenotypes”, invited seminar at National Institute for Medical Research, Mill Hill, London, UK, April 23rd, 2007.
12. Seeing the forest for the trees: GPCR allosterism and drug discovery, Merck & Co, Rawhay, New Jersey, April 10th, 2006.
13. Seeing the forest for the trees: GPCR allosterism and drug discovery, Eli Lilly Research Laboratories, Indianapolis, Indiana, April 7th, 2006.
14. GPCR allosterism and drug discovery, AMGEN, San Francisco, California, April 4th, 2006.
15. Allosteric or Orthosteric? Targeting drugs to G protein-coupled receptors, Bristol Myers Squibb, Princeton, New Jersey, September 23rd, 2005.
16. Allosteric Modulation and Targeting drugs to G protein-coupled receptors, GlaxoSmithKline, Research Triangle Park, North Carolina, September 21st, 2005.
17. Screening for allosteric modulators of GPCRs, Invitation to speak at the Merck GPCR Colloquium, Merck, West Point, Pennsylvania, April 7th, 2005.

National

Invited Keynote Presentations

1. “Structure-function studies of an allosteric binding site on M2 muscarinic acetylcholine receptors: A critical role for a dynamic E2 loop”, Drug Design Amongst the Vines, Royal Australian Chemical Institute, Hunter Valley, New South Wales, December 5th, 2006.

Invited Presentations at Symposia (of 10 total):

1. “The many shades of GPCR allosterism”, invitation to speak at ComBio, annual scientific meeting of the Australian Society of Biochemistry and Molecular Biology, Sydney, September 22nd-26th, 2007.
2. “Allosteric modulation of neurotransmitter responses”, 3rd Australian Health and Medical Research Congress, Melbourne, November 28th, 2006.
3. “Allosteric modulators of G protein-coupled receptors: Novel drugs for the CNS”, Joint CINP/ASPR Scientific Meeting, December 8th, 2005.
4. “Allosteric modulators of G protein-coupled receptors”, Annual Scientific Meeting of the Institute for Biomedical Research, University of Sydney, July 8th, 2005.

Session Chairs (of 11 total):

1. Chairperson, “From structure to function: The role of receptor dynamics”, 3rd Annual Australian Health and Medical Research Congress, Nov 26th-Dec 1st, Melbourne, 2006.
2. Chairperson, “Regulation of Cell Signalling”, Annual Scientific Meeting of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists, Hilton on the Park, Melbourne, December 6th, 2005.
3. Chairperson, “Allosteric Regulation of GPCRs” “Molecular Pharmacology of G Protein-Coupled Receptors”, Melbourne, 3rd December, 2005.

Invited Seminars (of 17 total):

1. “Allosteric regulation of G protein-coupled receptors”, Institute for Molecular Bioscience, University of Queensland, June 17th, 2005.


PUBLICATIONS SINCE 2002

Refereed Journal Articles (from a total of 53)

1. Chan W.Y., McKinzie D., Bose S., Mitchell S., Witkin J., Thompson R.C., Christopoulos, A., Lazareno S., Birdsall  N.J.M., Bymaster F.P. and C.C. Felder (2008) Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia. Proc. Natl. Acad. Sci. (USA), In Press.
2. Avlani, V.A., McLoughlin, D.J., Sexton, P.M. and A. Christopoulos (2008) The impact of orthosteric radioligand depletion on the quantification of allosteric modulator interactions. J. Pharmacol. Exp. Ther. 36: 21637-1640.
3. Sexton, P.M., Christopoulos, G., Christopoulos, A., Nylen, E.S., Snider Jr., R.H. and K.L. Becker (2008) Procalcitonin has bioactivity at calcitonin receptor family complexes: Potential mediator in sepsis. Crit. Care. Med. 325: 927-934.
4. Udawela, M., Christopoulos, G., Morfis, M., Tilakaratne, N., Christopoulos, A. and P. M. Sexton (2008) The effects of C-terminal truncation of receptor activity modifying proteins on the induction of amylin receptor phenotype from human CTb receptors. Reg. Pep., 145: 65-71.
5. Avlani, V.A., Gregory, K.J., Morton, C.J., Parker, M.W., Sexton, P.M. and A. Christopoulos (2007) Critical role for the second extracellular loop in the binding of orthosteric and allosteric G protein-coupled receptor ligands.  J. Biol. Chem., 282: 25677-25686.
6. Bisson, W.H., Cheltsov, A.V., Bruey-Sedano, N., Chen, J., Goldberger, N., May, L.T., Christopoulos, A., Dalton, J.T., Sexton, P.M., X.-K. Zhang and R. Abagyan (2007), Discovery of antiandrogen activity of non-steroidal scaffolds of marketed drugs,  Proc. Natl. Acad. Sci. (USA), 104: 11927-11932.
7. May, L.T., Avlani, V.A., Langmead, C.J., Herdon, H.J., Wood, M. D., Sexton, P.M. and A. Christopoulos (2007) Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors.  Mol. Pharmacol., 72: 463-476.
8. Espallergues, J., Lapalud, P., Christopoulos, A., Avlani, V.A., Sexton, P.M., Vamvakides, A. and T. Maurice (2007) Involvement of the sigma1 (σ1) receptor in the anti-amnesic, but not antidepressant-like, effects of the aminotetrahydrofuran derivative ANAVEX1-41. Brit. J. Pharmacol.,  152: 267-279.
9. Moloney, G. P., Angus, J. A., Robertson, A. D., Stoermer, M. J., Robinson, M., Wright, C., McRae, K. and A. Christopoulos (2008) Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: Novel agonists for the CB1 receptor. Eur. J. Med. Chem., 43: 513-539.
10. Hay, D.L., Christopoulos, G., Christopoulos, A. and P.M. Sexton (2006) Determinants of 1 - Piperidinecarboxamide, N - [2 - [[5 – Amino – l - [[4 - (4 - pyridinyl) – l -piperazinyl]carbonyl]pentyl]amino] – 1 - [(3,5 – dibromo – 4 - hydroxyphenyl)methyl] -2-oxoethyl]-4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl) (BIBN4096BS) affinity for calcitonin gene-related peptide and amylin receptors:  The role of receptor activity modifying protein 1. Mol. Pharmacol., 70: 1984-1991.
11. Udawela, M., Christopoulos, G., Morfis, M., Christopoulos, A., Ye, S., Tilakaratne, N. and P. M. Sexton (2006) A critical role for the short intracellular C-terminus in receptor activity modifying protein function. Mol. Pharmacol., 70: 1750-1760.
12. Lanzafame, A.A., Sexton, P.M. and A. Christopoulos (2006) Interaction studies of multiple binding sites on M4 muscarinic acetylcholine receptors. Mol. Pharmacol., 70: 736-746.
13. Udawela, M. Christopoulos G., Tilakaratne, N., Christopoulos, A., Albiston, A. and P. M. Sexton (2006) Distinct receptor activity modifying protein (RAMP) domains differentially modulate interaction with calcitonin receptors. Mol. Pharmacol. 69: 1984-1989.
14. Mathiesen J.M., Christopoulos, A., Ulven T., Royer J., Campillo M., Heinemann A., Pardo L. and E. Kostenis (2006) On the mechanism of interaction of potent, surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2. Mol. Pharmacol., 69: 1441-1453.
15. Langmead, C.L., Fry V.A.H., Forbes, I.T., Branch, C.A., Christopoulos, A., Wood, M.D. and H. J. Herdon (2006) Probing the molecular mechanism of interaction between AC-42 and the muscarinic M1 receptor:  Direct pharmacological evidence that AC-42 is an allosteric agonist. Mol. Pharmacol., 69: 236-246.
16. May, L.T., Sexton, P.M. and A. Christopoulos (2005) Effects of urea pre-treatment on the binding properties of adenosine A1 receptors.  Br. J. Pharmacol., 146: 1119-1129.
17. Price, M.R., Baillie, G., Thomas, A., Stevenson, L.A., Easson, M., Goodwin, R., McLean, A., McIntosh, L., Goodwin, G., Walker, G., Westwood, P., Marrs, J., Thomson, F., Cowley, P., Christopoulos, A., Pertwee, R.G. and Ruth A. Ross (2005) Allosteric modulation of the cannabinoid CB1 receptor. Mol. Pharmacol., 67: 1484-1495.
18. Werry, T.D., Gregory, K.J., Sexton, P.M. and A. Christopoulos (2005) Characterization of serotonin 5-HT2C receptor signaling to extracellular signal-regulated kinases 1 and 2.  J. Neurochem.  93: 1603-1615.
19. Hay, D.L., Christopoulos, G., Christopoulos, A., Poyner D.R. and P.M. Sexton (2005) Pharmacological discrimination of calcitonin receptor-receptor activity modifying protein complexes. Mol. Pharmacol. 67: 1655-1665.
20. Kostenis, E., Milligan, G., Christopoulos, A., Sanchez-Ferrer, C., Heringer-Walther, S., Sexton, P.M., Gembardt, F., Kellett, E., Martini, L. Vanderheyden, P., Schultheiss, H-P. and T. Walther (2005). The G protein-coupled receptor Mas is a physiological antagonist of the angiotensin II AT1 receptor. Circulation, 111: 1806-1813.
21. Hutchinson, D.S., Sato, M., Evans, B.A., Christopoulos, A. and RJ. Summers (2005) Evidence for pleiotropic signalling at the mouse b3-adrenoceptor revealed by SR59230A. J. Pharmacol. Exp. Ther. 312: 1064-1074.
22. May, L.T., Lin, Y., Sexton, P.M. and A. Christopoulos (2005) Regulation of M2 muscarinic acetylcholine receptor expression and signalling by prolonged exposure to allosteric modulators, J. Pharmacol. Exp. Ther. 312: 382-390.
23. Lanzafame, A., Guida, E. and A. Christopoulos (2004) Effects of anandamide on the binding and signaling properties of M1 muscarinic acetylcholine receptors. Biochem. Pharmacol. 68: 2207 – 2219.
24. Devlin, M.G., Smith, N.J., Ryan, O. M., Guida, E., Sexton, P.M. and A. Christopoulos (2004) Regulation of serotonin 5-HT2C receptors by chronic ligand exposure, Eur. J. Pharmacol., 308: 59-69.
25. Lanzafame, A. and A. Christopoulos (2004), Investigation of the interaction of a putative allosteric modulator, N-(2,3-diphenyl-1,2,4-thiadiazole-5-(2H)-ylidene) methanamine hydrobromide (SCH-202676), with M1 muscarinic acetylcholine receptors, J. Pharmacol. Exp. Ther., 308: 830-837.
26. Avlani, V. May, L.T., Sexton, P.M. and A. Christopoulos (2004), Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors, J. Pharmacol. Exp. Ther., 308: 1062-1072.
27. Christopoulos, A., Christopoulos, G., Morfis M., Udawela, M., Laburthe, M., Couvineau A., Kuwasako, K., Tilakaratne, N. and P. M. Sexton (2003), Novel partners and function of receptor activity modifying proteins, J. Biol. Chem., 278: 3293-3297.
28. Devlin, M.G. and A. Christopoulos (2002), Modulation of cannabinoid agonist binding by 5-HT in the rat cerebellum, J. Neurochem. 80: 1095-1102.
29. Lyon, G., Wright, J., Christopoulos, A., Novick, R.P. and T.W. Muir (2002), Reversible and specific extracellular antagonism of receptor-histidine-kinase signaling, J. Biol. Chem. 227: 6247-6253.

Invited Reviews (of a total of 26)

1. 1. Werry, T.D., Loiacono, R.L., Sexton, P.M. and A. Christopoulos (2008) RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function. Pharmacol. Ther. In Press.
2. Gregory, K.J., Sexton, P.M. and A. Christopoulos (2007) Allosteric modulation of muscarinic acetylcholine receptors. Current Neuropharmacol.  5: 157-167.
3. Leach, K., Sexton, P.M. and A. Christopoulos (2007) Allosteric modulators of GPCRs: Taking advantage of permissive receptor pharmacology. Trends Pharmacol. Sci. 28: 382-389.
4. May, L.T., Leach, K., Sexton, P.M. and A. Christopoulos (2007) Allosteric modulation of G protein-coupled receptors, Ann. Rev. Pharmacol. Toxicol., 47: 1-51.
5. Urban, J.D., Clarke, W.P., von Zastrow, M., Nichols, D.E., Kobilka, B., Weinstein, H., Javitch, J.A., Roth, B.L., Christopoulos, A., Sexton, P.M., Miller, K.J., Spedding, M. and R B. Mailman (2007) Functional selectivity and classical concepts of quantitative pharmacology, J. Pharmacol. Exp. Ther., 320: 1-13.
6. Langmead, C. and A. Christopoulos (2006) Allosteric agonists of 7TM receptors: Expanding the pharmacological toolbox.Trends Pharmacol. Sci. 27: 475 - 481.
7. Sexton, P.M., Morfis, M., Tilakaratne, N., Hay, D.L., Udawela, M., Christopoulos, G. and A. Christopoulos (2006) Complexing receptor pharmacology: Modulation of Family B G protein-coupled receptor function by RAMPS, Ann. N.Y. Acad. Sci., 1070: 90-104.
8. Werry, T.D., Christopoulos, A. and P.M. Sexton (2006) Mechanisms of ERK regulation by seven transmembrane-domain receptors.  Curr. Pharm. Des., 12: 1683-702.
9. Werry, T.D., Sexton, P.M. and A. Christopoulos (2005) “Ins and Outs” of seven-transmembrane receptor signalling to ERK, Trends Endocrinol. Metab., 16: 26-33.
10. Christopoulos, A., May, T.L., Avlani, V.A. and P.M. Sexton (2004) G Protein-Coupled Receptor Allosterism:  The promise and the problem(s), Biochem. Soc. Trans. 32: 873 - 877.
11. Hay, D.L., Christopoulos, G., Christopoulos, A. and P. M. Sexton (2004) Amylin receptors: Molecular composition and pharmacology, Biochem. Soc. Trans. 32: 865 - 867.
12. Bartfai, T., Benovic, J.L., Bockaert, J., Bond, R.A., Bouvier, M., Christopoulos, A., Civelli, O., Devi, L.A., George, S., Inui, A., Kobilka, B., Leurs, R., Neubig, R. Pin, J.P., Quirion, R., Roques, B.P., Sakmar, T.P., Seifert, R., Stenkamp, R.E, and P.G. Strange (2004) The State of GPCR Research in 2004, Nature Reviews Drug Discovery, 3: 577 - 626
13. May, T.L., Avlani, V.A. Sexton, P.M. and A. Christopoulos (2004) Allosteric modulation of G Protein-Coupled Receptors, Curr. Pharm. Des. 10: 2003-2013.
14. Neubig, R.R., Spedding, M., Kenakin, T. and A. Christopoulos (2003) International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology, Pharmacol. Rev., 55: 597 - 606.
15. Morfis, M., Christopoulos, A. and P. M. Sexton (2003) RAMPs: 5 years on, where to now? Trends Pharmacol. Sci. 24:596 - 601.
16. May, L.T. and A. Christopoulos (2003) Allosteric modulators of G-protein-coupled receptors, Curr. Opin. Pharmacol., 3:551-556.
17. Lanzafame, A., Christopoulos, A. and F. Mitchelson (2003) Cellular signalling mechanisms for muscarinic acetylcholine receptors, Receptors and Channels, 9: 241-260.
18. Christopoulos, A. and T. Kenakin (2002) G protein-coupled receptor allosterism and complexing, Pharmacol. Rev. 54: 323-374.
19. Christopoulos, A. (2002) Allosteric binding sites on cell-surface receptors: Novel targets for drug discovery. Nature Rev. Drug Discovery 1: 198-210.

Books

1. Motulsky, H. J. and A. Christopoulos, Fitting models to biological data using linear and nonlinear regression (2004), Oxford University Press, NY, USA ISBN 0 19 517180 2.
2. Christopoulos, A. (Editor), Biomedical Applications of Computer Modeling (2000), CRC Press, FL, USA ISBN: 0 8493 0 100 9.

Chapters In Books (of a total of 5)

1. Karczmar, A., Lindstrom, J. and A. Christopoulos (2007) History of Research on Nicotinic and Muscarinic Cholinergic Receptors, in Exploring The Vertebrate Central Cholinergic System (A. Karczmar, Ed.), Springer, NY, USA, pp. 151-162.
2. Christopoulos, A. (2007) Muscarinic Acetylcholine Receptors in The Central Nervous System: Structure, Function and Pharmacology, in Exploring The Vertebrate Central Cholinergic System (A. Karczmar, Ed.), Springer, NY. pp. 163-208.