Research Outputs

Relevant publications and other resources created by researchers affiliated with the Centre

2021

Burger WAC, Gentry PR, Berizzi AE, Vuckovic Z, van der Westhuizen ET, Thompson G, Yeasmin M, Lindsley CW, Sexton PM, Langmead CJ, Tobin AB, Christopoulos A, Valant C, Thal DM. Identification of a novel allosteric site at the M5 muscarinic acetylcholine receptor.  ACS Chem. Neurosci. (2021), 12(16):3112-3123. doi: 10.1021/acschemneuro.1c00383.

Darke H, Sundram S, Cropper SJ, Carter O. Dynamic face processing impairments are associated with cognitive and positive psychotic symptoms across psychiatric disorders.  N.P.J. Schizophr. (2021), 7(1):36. doi: 10.1038/s41537-021-00166-z.

Davey, CG.  Out of the night-time and into the day: Ketamine and MDMA as therapies for mental disorders.  Aust. N Z J Psychiatry (2021), 55(8):741-743,  doi: 10.1177/00048674211032112.

Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A.  Positive allosteric mechanisms of adenosine A(1) receptor-mediated analgesia.  Nature (2021), 597(7877):571-576. doi: 10.1038/s41586-021-03897-2.

Nair PC, Miners JO, McKinnon RA, Langmead CJ, Gregory KJ, Copolov D, Chan SKW, Bastiampillai T.  Binding of SEP-363856 within TAAR1 and the 5HT1A receptor: implications for the design of novel antipsychotic drugs.  Mol. Psychiatry (2021) Aug 10. doi: 10.1038/s41380-021-01250-7.

Pantelis C, Jayaram M, Hannan AJ, Wesselingh R, Nithianantharajah J, Wannan CM, Syeda WT, Choy KC, Zantomio D, Christopoulos A, Velakoulis D, O'Brien TJ. Neurological, neuropsychiatric and neurodevelopmental complications of COVID-19. Aust. N.Z.J. Psychiatry (2021), 55(8):750-762. doi: 10.1177/0004867420961472.

Payne JE, Chambers R, Liknaitzky P. Combining psychedelic and mindfulness interventions: Synergies to inform clinical practice.  ACS Pharmacol. Transl. Sci. (2021), 4(2):416-423. doi: 10.1021/acsptsci.1c00034.

Perkins D, Sarris J, Rossell S, Bonomo Y, Forbes D, Davey C, Hoyer D, Loo C, Murray G, Hood S, Schubert V, Galvão-Coelho NL, O'Donnell M, Carter O, Liknaitzky P, Williams M, Siskind D, Penington D, Berk M, Castle D.  Medicinal psychedelics for mental health and addiction: Advancing research of an emerging paradigm.  Aust. N.Z.J. Psychiatry (2021) Mar 21:4867421998785. doi: 10.1177/0004867421998785.

Walker LC, Huckstep KL, Chen NA, Hand LJ, Lindsley CW, Langmead CJ, Lawrence AJ.  Muscarinic M4 and M5 receptors in the ventral subiculum differentially modulate alcohol seeking versus consumption in male alcohol-preferring rats.  Br. J. Pharmacol. (2021), 178(18):3730-3746. doi: 10.1111/bph.15513.

2020

Bradley SJ, Molloy C, Valuskova P, Dwomoh L, Scarpa M, Rossi M, Finlayson L, Svensson KA, Chernet E, Barth VN, Gherbi K, Sykes DA, Wilson CA, Mistry R, Sexton PM, Christopoulos A, Mogg AJ, Rosethorne EM, Sakata S, John Challiss RA, Broad LM, Tobin AB.  Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs.  Nat. Chem. Biol. (2020), 16(3):240-249. doi: 10.1038/s41589-019-0453-9.

Gibbons A, Sundram S, Dean B.  Changes in non-coding RNA in depression and bipolar disorder: Can they be used as diagnostic or theranostic biomarkers? Noncoding RNA (2020), 6(3):33. doi: 10.3390/ncrna6030033.

Hatzipantelis CJ, Langiu M, Vandekolk TH, Pierce TL, Nithianantharajah J, Stewart GD, Langmead CJ. Translation-focused approaches to GPCR drug discovery for cognitive impairments associated with schizophrenia.  ACS Pharmacol. Transl. Sci. (2020), 3(6):1042-1062. doi: 10.1021/acsptsci.0c00117.

Hatzipantelis CJ, Lu Y, Spark DL, Langmead CJ, Stewart GD.  β-Arrestin-2-dependent mechanism of GPR52 signaling in frontal cortical neurons.  ACS Chem. Neurosci. (2020), 11(14):2077-2084. doi: 10.1021/acschemneuro.0c00199.

Khajehali E, Bradley S, van der Westhuizen ET, Molloy C, Valant C, Finlayson L, Lindsley CW, Sexton PM, Tobin AB, Christopoulos A. Restoring agonist function at a chemogenetically modified M(1) muscarinic acetylcholine receptor.  ACS Chem. Neurosci. (2020), 11(24):4270-4279. doi: 10.1021/acschemneuro.0c00540.

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.  Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists.  Neuropharmacology (2019), 144:244-255. doi: 10.1016/j.neuropharm.2018.10.028.

Spark DL, Mao M, Ma S, Sarwar M, Nowell CJ, Shackleford DM, Sexton PM, Nithianantharajah J, Stewart GD, Langmead CJ.  In the loop: Extrastriatal regulation of spiny projection neurons by GPR52.  ACS Chem. Neurosci. (2020), 11(14):2066-2076. doi: 10.1021/acschemneuro.0c00197.

Walker LC, Berizzi AE, Chen NA, Rueda P, Perreau VM, Huckstep K, Srisontiyakul J, Govitrapong P, Xiaojian J, Lindsley CW, Jones CK, Riddy DM, Christopoulos A, Langmead CJ, Lawrence AJ.  Acetylcholine muscarinic M4 receptors as a therapeutic target for alcohol use disorder: Converging evidence from humans and rodents.  Biol. Psychiatry (2020), 88(12):898-909. doi: 10.1016/j.biopsych.2020.02.019.

Wells R, Jacomb I, Swaminathan V, Sundram S, Weinberg D, Bruggemann J, Cropley V, Lenroot RK, Pereira AM, Zalesky A, Bousman C, Pantelis C, Weickert CS, Weickert TW.  The impact of childhood adversity on cognitive development in schizophrenia.  Schizophr. Bull. (2020), 46(1):140-153. doi: 10.1093/schbul/sbz033.

2019

Esménio S, Soares JM, Oliveira-Silva P, Zeidman P, Razi A, Gonçalves ÓF, Friston K, Coutinho J.  Using resting-state DMN effective connectivity to characterize the neurofunctional architecture of empathy.  Sci. Rep. (2019), 9(1):2603. doi: 10.1038/s41598-019-38801-6.

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.  Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs.  Nat. Commun. (2019), 10(1):3289. doi: 10.1038/s41467-019-11062-7.

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.  Molecular determinants of the intrinsic efficacy of the antipsychotic aripiprazole.  ACS Chem. Biol. (2019), 14(8):1780-1792. doi: 10.1021/acschembio.9b00342.

Parkes L, Tiego J, Aquino K, Braganza L, Chamberlain SR, Fontenelle LF, Harrison BJ, Lorenzetti V, Paton B, Razi A, Fornito A, Yücel M.  Transdiagnostic variations in impulsivity and compulsivity in obsessive-compulsive disorder and gambling disorder correlate with effective connectivity in cortical-striatal-thalamic-cortical circuits.  Neuroimage (2019), 202:116070. doi: 10.1016/j.neuroimage.2019.116070.

Preller KH, Razi A, Zeidman P, Stämpfli P, Friston KJ, Vollenweider FX.  Effective connectivity changes in LSD-induced altered states of consciousness in humans.  Proc. Natl. Acad. Sci. USA. (2019), 116(7):2743-2748. doi: 10.1073/pnas.1815129116.

Vuckovic Z, Gentry PR, Berizzi AE, Hirata K, Varghese S, Thompson G, van der Westhuizen ET, Burger WAC, Rahmani R, Valant C, Langmead CJ, Lindsley CW, Baell JB, Tobin AB, Sexton PM, Christopoulos A, Thal DM. Crystal structure of the M5 muscarinic acetylcholine receptor. Proc. Natl. Acad. Sci. U.S.A. (2019), 116(51):26001-26007. doi: 10.1073/pnas.1914446116 .

2018

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.  Discovery and optimization of potent and CNS penetrant M5-preferring positive allosteric modulators derived from a novel, chiral N-(Indanyl)piperidine amide scaffold.  ACS Chem. Neurosci. (2018), 9(7):1572-1581. doi: 10.1021/acschemneuro.8b00126.

Berk M, Loo C, Davey CG, Harvey BH.  Ketamine and rapidly acting antidepressants: Breaking the speed of sound or light?  Aust. N.Z.J. Psychiatry (2018), 52(11):1026-1029. doi: 10.1177/0004867418783567.

Berizzi AE, Bender AM, Lindsley CW, Conn PJ, Sexton PM, Langmead CJ, Christopoulos A. Structure-activity relationships of Pan-Gαq/11-coupled muscarinic acetylcholine receptor positive allosteric modulators.  ACS Chem. Neurosci. (2018), 9(7):1818-1828. doi: 10.1021/acschemneuro.8b00136.

Berizzi AE, Perry CJ, Shackleford DM, Lindsley CW, Jones CK, Chen NA, Sexton PM, Christopoulos A, Langmead CJ, Lawrence AJ.  Muscarinic M5 receptorsmodulate ethanol seeking in rats.  Neuropsychopharmacology (2018), 43(7):1510-1517. doi: 10.1038/s41386-017-0007-3.

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.  Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes.  Mol. Pharmacol. (2018), 93(6):645-656. doi: 10.1124/mol.118.111872.

Burger WAC, Sexton PM, Christopoulos A, Thal DM. Toward an understanding of the structural basis of allostery in muscarinic acetylcholine receptors.  J. Gen. Physiol. (2018), 150(10):1360-1372. doi: 10.1085/jgp.201711979.

Dallagnol JCC, Khajehali E, van der Westhuizen ET, Jörg M, Valant C, Gonçalves AG, Capuano B, Christopoulos A, Scammells PJ.  Synthesis and pharmacological evaluation of heterocyclic carboxamides: Positive allosteric modulators of the M1 muscarinic acetylcholine receptor with weak agonist activity and diverse modulatory profiles.  J. Med. Chem. (2018), 61(7):2875-2894. doi: 10.1021/acs.jmedchem.7b01812.

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. Structure of the adenosine-bound human adenosine A(1) receptor-G(i) complex. Nature (2018), 558(7711):559-563. doi: 10.1038/s41586-018-0236-6.

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.  The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D(2) receptor.  Biochem. Pharmacol. (2018), 148:315-328. doi: 10.1016/j.bcp.2018.01.002.

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.  The action of a negative allosteric modulator at the dopamine D(2) receptor is dependent upon sodium ions.  Sci. Rep. (2018), 8(1):1208. doi: 10.1038/s41598-018-19642-1.

Khajehali E, Valant C, Jörg M, Tobin AB, Conn PJ, Lindsley CW, Sexton PM, Scammells PJ, Christopoulos A.  Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor.  Biochem. Pharmacol. (2018), 154:243-254. doi: 10.1016/j.bcp.2018.05.009.

Thal DM, Glukhova A, Sexton PM and Christopoulos A. Structural insights into G-protein-coupled receptor allostery. Nature (2018) 559: 45–53. doi: 10.1038/s41586-018-0259-z.

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.  DREADD agonist 21 is an effective agonist for muscarinic-based DREADDs in vitro and in vivo.  ACS Pharmacol. Transl. Sci. (2018), 1(1):61-72. doi: 10.1021/acsptsci.8b00012.

Van Rheenen TE, Cropley V, Zalesky A, Bousman C, Wells R, Bruggemann J, Sundram S, Weinberg D, Lenroot RK, Pereira A, Shannon Weickert C, Weickert TW, Pantelis C.  Widespread volumetric reductions in schizophrenia and schizoaffective patients displaying compromised cognitive abilities.  Schizophr. Bull. (2018), 44(3):560-574. doi: 10.1093/schbul/sbx109.

2017

Bradley SJ, Bourgognon J-M, Sanger HE, Verity N, Mogg A, White DJ, Butcher AJ, Moreno JA, Molloy C, Macedo-Hatch T, Edwards JE, Wess J, Pawlak R, Read DJ, Sexton PM, Broad LM, Steinert JR, Mallucci GR, Christopoulos A, Felder CC and Tobin AB. M1-muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss. J. Clin. Invest. (2017), 127: 487–499. doi: 10.1172/JCI87526.

Cropley VL, Klauser P, Lenroot RK, Bruggemann J, Sundram S, Bousman C, Pereira A, Di Biase MA, Weickert TW, Weickert CS, Pantelis C, Zalesky A.   Accelerated gray and white matter deterioration with age in schizophrenia.  Am. J. Psychiatry (2017), 174(3):286-295. doi: 10.1176/appi.ajp.2016.16050610.

Mostaid MS, Lee TT, Chana G, Sundram S, Shannon Weickert C, Pantelis C, Everall I, Bousman C.  Elevated peripheral expression of neuregulin-1 (NRG1) mRNA isoforms in clozapine-treated schizophrenia patients.  Transl. Psychiatry (2017), 7(12):1280. doi: 10.1038/s41398-017-0041-2.

2016

Choy KHC, Shackelford DM, Malone DT, Mistry SN, Patil RT, Scammels PJ, Langmead CJ, Pantelis C, Sexton PM, Lane JR, Christopoulos A.  Positive allosteric modulation of the muscarinic M1 receptor improves efficacy of antipsychotics in mouse glutaminergic deficit models of behavior. J. Pharmacol. Exp. Ther. (2016), 359(2):354-365. doi: 10.1124/jpet.116.235788 .

Thal, DM, Sun, B, Feng, D, Nawaratne, V, Leach, K, Felder, CC, Bures, MG, Evans, DA, Weis, WI, Bachhawat, P, Kobilka, TS, Sexton, PM, Kobilka, BM and Christopoulos A. Crystal structures of the M1 and M4 muscarinic acetylcholine receptors and insights into their allosteric modulation. Nature. (2016), 531: 335–340. doi: 10.1038/nature17188.