364:
Liang, Y.L., Khoshouei, M., Radjainia, M., Zhang, Y., Glukhova, A., Tarrasch, J., Thal, D.M., Furness, S.G.B., Christopoulos, G., Coudrat, T., Danev, R., Baumeister, W., Miller, LJ., Christopoulos, A., Kobilka, B.K., Wootten, D., Skiniotis, G. and P.M. Sexton (2017) Phase-plate cryo-EM structure of a
508:
Kruse, A.C., Ring, A.M., Manglik, A., Hu, J., Hu, K., Eitel, K., Hübner, H., Pardon, E., Valant, C., Sexton, P.M., Christopoulos, A., Felder, C.C., Gmeiner, P., Steyert, J., Weiss, W.I., Garcia, K.C., Wess, J. and B.K. Kobilka (2013) Activation and allosteric modulation of a muscarinic acetylcholine
402:
Qin, R.C.X., May, L.T., Li, R., Cao, N., Rosli, S., Deo, M., Alexander, A.E., Horlock, D., Bourke, J.E., Yang, Y.H., Stewart, A.G., Kaye, D.M., Du, X.-J., Sexton, P.M., Christopoulos, A., Gao X.-M. and R. H. Ritchie (2017) Small-molecule biased formyl peptide receptor agonist
Compound-17b protects
340:
Korczynska, M., Clark, M.J., Valant, C., Moo, E.V., Abold, S., Weiss, D.R., Torosyan, H., Huang, W., Kruse, A.C., May, L.T., Baltos, J., Sexton, P.M., Kobilka, B.K., Christopoulos, A., Shoichet, B.K., and R.K. Sunahara (2018) Structure-based discovery of selective positive allosteric modulators of
207:
Vuckovic, Z., Wang, J., Pham, V., Mobbs, J., Belousoff, M.T., Bhattarai, A., Nawaratne, V., Leach, K., Burger, W.A.C., van der
Westhuizen, E.T., Khajehali, E., Thompson, G., Yeasmin, M., Liang, Y.L., Glukhova, A., Wootten, D., Lindsley, C.W., Tobin, A.B., Sexton, P.M., Danev, R., Valant, C., Miao,
477:
Christopoulos, A., Changeux, J.P., Catterall, W.A., Fabbro, D., Burris, T.P., Cidlowski, J.A., Olsen, R.W., Peters, J.A., Neubig, R.R., Pin, J.P., Sexton, P.M., Kenakin, T.P., Ehlert, F.J., Spedding M. and C.J. Langmead (2014) International Union of Basic and
Clinical Pharmacology. XC. Multi-site
426:
Wootten, D., Reynolds, C.A., Smith, K.J., Mobarec, J.C., Koole, C., Savage, E., Pabreja, K., Simms, J., Sridhar, R., Furness, S.G.B., Liu, M., Thompson, P.E., Miller, L.J., Christopoulos, A. and P.M. Sexton (2016) The GLP-1 receptor extracellular surface is a molecular trigger for biased agonism.
352:
Liang, Y.-L., Khosouei, M., Glukhova, A., Furness, S.G.B., Clydesdale, L., Koole, C., Troung, T.T., Thal, D.M., Lei, S., Radjainia, M., Danev, R., Baumeister, W., Wang, M.-W., Christopoulos, A., Sexton, P.M. and D. Wootten (2018) Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1
247:
Zhao, P., Liang, Y.L., Belousoff, M.J., Deganutti, G., Fletcher, M.M., Willard, F.S., Sloop, K.W., Inoue, A., Truong, T.T., Clydesdale, L., Furness, S.G.B., Christopoulos, A., Wang, M.W., Miller, L.J., Reynolds, C.A., Danev, R., Sexton, P.M. and D. Wootten (2020) Activation of GLP-1 receptor by a
383:
Bradley, S.J., Bourgognon, J.-M., Sanger, H.E., Verity, N., Mogg, A., White, D.J., Butcher, A.J., Moreno, J.A., Molloy, C., Macedo-Hatch, T., Edwards, J.E., Wess, J., Pawlak, R., Read, D.J., Sexton, P.M., Broad, L.M., Steinert, J.R., Mallucci, G.R., Christopoulos, A., Felder, C.C. and A.B. Tobin
235:
Bradley, S.J., Molloy, C., Valuskova, P., Dwomoh, L., Scarpa, M., Rossi, M., Finlayson, L., Svensson, K.A., Chernet, E., Barth, V.N., Gherbi, K., Sykes, D.A., Wilson, C., Mistry, R., Sexton, P.M., Christopoulos, A., Mogg, A.J., Rosethorne, E.M., Sakata, S., Challiss, R.A.J., M. Broad L. and A.B.
223:
Draper-Joyce, C.J., Bhola, R., Wang, J., Bhattarai, A., Nguyen, A.T.N., Cowie-Kent, I., O’Sullivan, K., Chia, L.Y., Venugopal, H., Valant, C., Thal, D.M., Wootten, D., Panel, N., Carlsson, J., Christie, M.J., White, P.J., Scammells, P., May, L.T., Sexton, P.M., Danev, R., Miao, Y., Glukhova, A.,
263:
Hollingsworth, S.A., Kelly, B., Valant, C., Michaelis, J.A., Mastromihalis, O., Thompson, G., Venkatakrishnan, A.J., Hertig, S., Scammells, P.J., Sexton, P.M., Felder, C.C., Christopoulos, A. and R. O. Dror (2019) Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic
239:
Liang, Y.-L., Belousoff, M.J., Fletcher, M., Zhang, X., Khoshouei, M., Deganutti, G., Koole, C., Furness, S.B.G., Miller, L.J., Hay, D.L., Christopoulos, A., Reynolds, C.A., Wootten, D., and P.M. Sexton (2020) Structure and dynamics of the adrenomedullin (AM) receptors, AM1 and AM2, reveals key
203:
Burger, W.A.C., Pham, V., Vuckovic, Z., Powers, A.S., Mobbs, J.I., Laloudakis, Y., Glukhova, A., Wootten, D., Tobin, A.B., Sexton, P.M., Paul, S.M., Felder, C.C., Danev, R., Dror, R.O., Christopoulos, A., Valant, C. and D.M. Thal (2023) Xanomeline displays concomitant orthosteric and allosteric
255:
Vuckovic, Z., Gentry, P.R., Berizzi, A. E., Hirata, K., Varghese, S., Thompson, G., van der
Westhuizen, E.T., Burger, W.A.C., Rahmani, R., Valant, C., Langmead, C., Lindsley, C., Baell, J., Tobin, A.B., Sexton, P.M., Christopoulos A. and D.M. Thal (2019) Crystal structure of the M5 muscarinic
271:
Draper-Joyce, C.J., Khosouei, M., Thal. D.M., Liang, Y.L., Nguyen, A.T.N., Gurness, S.G.B., Venugopal, H., Baltos, J., Plitzko, J.P., Danev, R., Baumeisterm W., May, L.T., Wootten, D., Sexton, P.M., Glukhova, A. and A. Christopoulos (2018) Structure of the adenosine-bound human A1
500:
Dror, R.O., Green, H.F., Valant, C., Borhani, D.W., Valcourt, J.R., Pan, A.C., Arlow, D.H., Canals, M., Lane, J.R., Rahmani, R., Baell, J.B., Sexton, P.M., Christopoulos, A. and D.E. Shaw (2013) Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs.
442:
Klein
Herenbrink, C., Sykes, D.A., Donthamsetti, P., Canals, M., Coudrat, T., Shonberg, J., Scammells, P.J., Capuano, B., Sexton, P.M., Charlton, S.J., Javitch, J.A., Christopoulos, A. and J.R. Lane (2016) The role of kinetic context in apparent biased agonism at GPCRs.
469:
Lane, J.R., Donthamsetti, P., Shonberg, J., Draper-Joyce, C.J., Dentry, S., Michino, M., Shi, L., López, L., Scammells, P.J., Capuano, B., Sexton, P.M., Javitch, J.A. and A. Christopoulos (2014) A new mechanism of allostery in a G protein-coupled receptor dimer.
576:
Valant, C., Gregory, K.J., Hall, N.E., Scammells, P.J., Lew, M.J., Sexton, P.M. and A. Christopoulos (2008) A novel mechanism of G protein-coupled receptor functional selectivity: muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand,
227:
Josephs, T.M., Belousoff, M.J., Liang, Y.L., Piper, S.J., Cao, J., Garama, D.J., Leach, K., Gregory, K.J., Christopoulos, A., Hay, D.L., Danev, R., Wootten, D. and P.M. Sexton (2021) Structure and dynamics of the CGRP receptor in apo and peptide-bound forms.
186:
has annually regularly named him a Highly Cited
Researcher in Pharmacology and Toxicology. In 2021, Arthur was named a Highly Cited Researcher in both Pharmacology and Toxicology and Biology and Biochemistry categories. In 2017 he was elected a Fellow of the
527:
Leach, K., Wen, A., Cook, A.E., Sexton, P.M., Conigrave, A.D, and A. Christopoulos (2013) Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium sensing receptor by positive and negative allosteric modulators.
300:
Liang, Y.L., Khoshouei, M., Deganuti, G., Glukhova, A., Koole, C., Peat, T.S., Radjainia, M., Plitzko, J.M., Baumeister, W., Miller, L.M., Hay, D.L., Christopoulos, A., Reynolds, C.A., Wootten, D. and P M. Sexton (2018) Cryo-EM structure of the active,
485:
Valant, C., May, L.T., Aurelio, L., Chuo, C.H., White, P.J., Baltos, J., Sexton, P.M., Scammells, P.J. and A. Christopoulos (2014) Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist.
434:
Leach, K., Gregory, K.J., Kufareva, I., Khajehali, E., Cook, A.E., Abagyan, R., Conigrave, A.D., Sexton P.M. and A. Christopoulos (2016) Towards a structural understanding of allosteric drugs at the human calcium sensing receptor
418:
Miao, Y., Goldfeld, D., Moo, E.V., Sexton, P.M., Christopoulos, A., McCammon, A.J. and C. Valant (2016) Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor.
410:
Furness, S.G.B., Liang, Y.-L., Nowell, C.J., Halls, M.L., Wookey, P.J., Dal Maso, E., Inoue, A., Christopoulos, A., Wootten, D. and P.M. Sexton (2016) Ligand-dependent modulation of G protein conformation alters drug efficacy.
1101:
561:
Valant, C., Felder, C.C., Sexton, P.M. and A. Christopoulos (2012) Probe-dependence in the allosteric modulation of a G protein-coupled receptor: Implications for detection and validation of allosteric ligand effects.
549:
Wootten D., Savage E.E., Valant C., May L.T., Sloop K.W., Ficorilli J., Showalter A.D., Willard F.S., Christopoulos A. and P.M. Sexton. Allosteric modulation of endogenous metabolites as an avenue for drug discovery.
215:
Cao, J., Belousoff, M.J., Liang, Y.L., Johnson, R.M., Josephs, T.M., Fletcher, M.M., Christopoulos, A., Hay, D.L., Danev, R., Wootten, D. and P.M. Sexton (2022) A structural basis for amylin receptor phenotype.
161:
454:
D., Nawaratne, V., Leach, K., Felder, C.C., Bures, M.G., Evans, D.A., Weis, W.I., Bachhawat, P., Kobilka, T.S., Sexton, P.M., Kobilka, B.M. and A. Christopoulos (2015) Crystal structures of the M
569:
Canals, M., Lane, J.R., Wen, A., Scammells, P.J., Sexton, P.M. and A. Christopoulos (2012) A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation.
1030:
516:
Mistry, S., Valant, C., Sexton, P., Capuano, B., Christopoulos, A. and P.J. Scammells (2013) Synthesis and pharmacological profiling of analogues of BQCA as allosteric modulators of the M
164:, the Rand Medal from the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists, the 2014 IUPHAR Analytical Pharmacology Lecturer, a 2015 Doctor of Laws (
535:
Gregory, K.J., Sexton, P.M., Tobin, A.B. and A. Christopoulos (2012) Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor.
31:
1106:
493:
Kruse, A.C., Kobilka, B.K., Gautam, D., Sexton, P.M., Christopoulos, A. and J., Wess (2014) Insights into muscarinic acetylcholine receptor biology, pharmacology, and structure.
134:
701:
149:
and ACS Pharmacology and
Translational Sciences. Prior to taking up his current position as Dean, Professor Christopoulos held a Senior Principal Research Fellowship of the
188:
542:
Kenakin, T., Watson, C., Muniz-Medina, V. and A. Christopoulos (with
Appendix by S. Watson) (2012) A simple method to quantify functional selectivity and agonist bias.
751:
726:
372:
Glukhova, A., Thal, D.T., Nguyen, A.T.N., Vecchio, E.A., Jörg, M., Scammells, P.J., May, L.T., Sexton, P.M. and A. Christopoulos (2017) Structure of the adenosine A
171:
319:
Berizzi, A., Perry, C., Shackleford, D., Lindsley, C., Jones, C., Chen, N., Sexton, P.M., Christopoulos, A., Langmead, C.J. and A.J. Lawrence (2018) Muscarinic M
801:
191:, in 2018 he was elected as a Fellow of the British Pharmacological Society and in 2023 he was elected as a Fellow of the Pharmaceutical Society of Australia.
1096:
150:
208:
Y., Christopoulos, A and D.M. Thal (2023) Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics.
1091:
333:
Wootten, D., Christopoulos, A., Solano, M.M., Babu, M.M., and P.M. Sexton (2018) Mechanisms of signalling and bias in G-protein coupled receptors.
41:
and from 2021 to 2023 he served as the inaugural
Director of Monash University's Neuromedicines Discovery Centre. He was elected a Fellow of the
584:
Motulsky, H. and
Christopoulos, A. Fitting Models to Biological Data Using Linear and Nonlinear Regression: A practical guide to curve fitting
651:
224:
Imlach, W.L. and A. Christopoulos (2021) Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia. Nature 597: 571-576.
1076:
62:
38:
1086:
1081:
596:
295:
395:
Lane, J.R., May, L.T., Parton, R.G., Sexton, P.M and A. Christopoulos (2017) A kinetic view of GPCR allostery and biased agonism.
236:
Tobin (2020) Biased M1-muscarinic receptor-mutant mice inform the design of next generation drugs. Nature Chem. Biol. 16: 240–249.
312:
Thal, D.M., Glukhova, A., Sexton P.M. and A. Christopoulos (2018) Structural insights into G-protein-coupled receptor allostery.
179:
146:
42:
1071:
876:
1031:"Monash researchers founding scientists of new GPCR biotechnology company launched with AUD$ 140 million in financing"
702:"Twenty-two Australians recognised among our nation's most distinguished scientists | Australian Academy of Science"
110:
982:
828:
142:
129:, and animal models of behaviour. He has served on the Editorial Board of several scientific journals, including
608:
Christopoulos, A. (2002) Allosteric binding sites on cell-surface receptors: Novel targets for drug discovery.
588:
287:
285:
Fitting Models to Biological Data Using Linear and Nonlinear Regression: A practical guide to curve fitting.
138:
86:
74:
1066:
130:
901:
98:
194:
In 2022, Prof. Christopoulos was an academic co-founder of the GPCR biotech. startup, Septerna Inc.
58:
54:
478:
Pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands.
183:
122:
157:
118:
601:
Christopoulos, A. and T. Kenakin (2002) G protein-coupled receptor allosterism and complexing,
592:
291:
69:, and subsequently pursued postdoctoral studies in the Department of Neuroscience Research in
66:
35:
27:
126:
1004:
1047:
388:-muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss.
1051:
106:
156:
He is the recipient of numerous national and international awards, including the 2013
1060:
166:
114:
82:
462:
muscarinic acetylcholine receptors and insights into their allosteric modulation.
931:
631:"Governance | IUPHAR - International Union of Basic & Clinical Pharmacology"
102:
802:"WCP 2014: 17th World Congress of Basic and Clinical Pharmacology in Cape Town"
853:
70:
78:
23:
113:(GPCRs) – the largest class of drug targets - and incorporates molecular
630:
776:
676:
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902:"Highly Cited Researchers - The Most Influential Scientific Minds"
1102:
Fellows of the Australian Academy of Health and Medical Sciences
956:
829:"Prof. Christopoulos receives honorary doctorate | Neos Kosmos"
162:
American Society for Pharmacology and Experimental Therapeutics
909:
855:
Gaddum Memorial Lecture 2016: Professor Arthur Christopoulos
182:
and the 2016 GSK Award for Research Excellence. Since 2014,
240:
mechanisms in the control of receptor phenotypes by RAMPs.
178:, the 2016 recipient of the Gaddum Memorial Award from the
961:
AAHMS - Australian Academy of Health and Medical Sciences
403:
against myocardial ischemia-reperfusion injury in mice.
32:
International Union of Basic and Clinical Pharmacology
204:
binding modes at the M4 mAChR. Nature Comm. 14: 5440.
135:
Journal of Pharmacology and Experimental Therapeutics
81:
to establish his laboratory within the Department of
376:
receptor reveals the basis for subtype selectivity.
34:
from 2018 to 2022. In 2019 he was appointed Dean of
189:Australian Academy of Health and Medical Sciences
656:Faculty of Pharmacy and Pharmaceutical Sciences
652:"Professor Arthur Christopoulos named new Dean"
160:and the 2024 Goodman and Gilman Award from the
39:Faculty of Pharmacy and Pharmaceutical Sciences
8:
1107:Fellows of the Australian Academy of Science
323:receptors modulate ethanol seeking in rats.
151:National Health and Medical Research Council
97:Arthur Christopoulos’ research focuses on
89:. In 2006, he moved to Monash University.
16:Australian pharmacologist and toxicologist
305:-protein complexed, human CGRP receptor.
622:
283:Harvey Motulsky, Arthur Christopoulos.
1029:Monash University (1 February 2022).
7:
172:National and Kapodistrian University
1097:Academic staff of Monash University
1009:Pharmaceutical Society of Australia
345:muscarinic acetylcholine receptor.
877:"Previous Winners | GSK Australia"
827:Thomaidou, Zoe (28 October 2015).
14:
1005:"New Fellows recognised at PSA23"
677:"Neuromedicines Discovery Centre"
981:BPS, London (19 December 2018).
365:class B GPCR-G protein complex.
1092:University of Minnesota faculty
681:Neuromedicines Discovery Centre
180:British Pharmacological Society
147:British Journal of Pharmacology
26:of Analytical Pharmacology at
1:
232:. 372: eabf7258.
63:Victorian College of Pharmacy
43:Australian Academy of Science
30:. He was a Councillor of the
983:"2018 Fellowships announced"
488:Proc. Natl. Acad. Sci. (USA)
421:Proc. Natl. Acad. Sci. (USA)
347:Proc. Natl. Acad. Sci. (USA)
1003:wpclarkeg (4 August 2023).
495:Nature Rev. Drug Discovery,
111:G protein-coupled receptors
1123:
1077:Australian pharmacologists
932:"Highly Cited Researchers"
610:Nature Rev. Drug Discovery
450:Thal, D.M., Sun, B., Feng
335:Nat. Rev. Mol. Cell Biol.
256:acetylcholine receptor.
143:ACS Chemical Neuroscience
53:Christopoulos obtained a
1087:Monash University alumni
1082:Australian toxicologists
1050:publications indexed by
806:guidetopharmacology blog
77:, prior to returning to
589:Oxford University Press
288:Oxford University Press
260:(USA) 116: 26001–26007.
139:Pharmacological Reviews
87:University of Melbourne
75:University of Minnesota
258:Proc. Natl. Acad. Sci.
131:Molecular Pharmacology
520:muscarinic receptor.
341:antagonists for the M
325:Neuropsychopharmacol.
248:non-peptide agonist.
119:mathematical modeling
1048:Arthur Christopoulos
752:"2024 Award Winners"
727:"2013 Award Winners"
117:, computational and
55:Bachelor of Pharmacy
20:Arthur Christopoulos
1072:20th-century births
912:on 20 February 2019
544:ACS Chem. Neurosci.
423:. 113: E5675-E5684.
184:Clarivate Analytics
123:medicinal chemistry
105:and signal-pathway
36:Monash University's
706:www.science.org.au
472:Nature Chem. Biol.
397:Nature Chem. Biol.
158:John J. Abel Award
858:, 7 February 2017
581:283: 29312–29321.
539:287: 37066–37077.
431:. 165: 1632–1643.
349:115: E2419-E2428.
125:, structural and
67:Monash University
28:Monash University
22:is an Australian
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107:biased agonism
101:mechanisms of
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