Skip to Content


ACS Chem Neurosci Burger et al 2021 BJP Walker et al 2021 Johnson et al 2021      
Mol CellACS Chem Neurosc 2020 11(14) ACS Pharm Transl Sci ACS Pharmacology Translational Sci PNAS 117(30) 2020 Biological Psychiatry 88(12) 2020   
BJP Nature Nanotech 14(12) 2019 PNAS Neuropharm 144 (2019) Pharmacol Reviews ACS Chem Neurosci 9(7) 2018   

Research Papers

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 (2021) Identification of a novel allosteric site at the M5 muscarinic acetylcholine receptor.  ACS Chem. Neurosci. 12(16):3112-3123. doi: 10.1021/acschemneuro.1c00383.

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

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

Johnson RM, Zhang X, Piper SJ, Nettleton TJ, Vandekolk THLangmead CJ, Danev R, Sexton PM, Wootten D (2021) Cryo-EM structure of the dual incretin receptor agonist, peptide-19, in complex with the glucagon-like peptide-1 receptor.   Biochem. Biophys. Res. Commun. 578:84-90. doi: 10.1016/j.bbrc.2021.09.016.

Giuffrida L, Sek K, Henderson MA, Lai J, Chen AXY, Meyran D, Todd KL, Petley EV, Mardiana S, Mølck C, Stewart GD, Solomon BJ, Parish IA, Neeson PJ, Harrison SJ, Kats LM, House IG, Darcy PK, Beavis PA.  (2021) CRISPR/Cas9 mediated deletion of the adenosine A2A receptor enhances CAR T cell efficacy.  Nat. Comm. 12,  Article number:3236

Rueda P, Merlin J, Chimenti S, Feletou M, Paysant J, White PJ, Christopoulos A, Sexton PM, Summers RJ, Charman WN, May LT, Langmead CL (2021) Pharmacological insights into safety and efficacy determinants for the development of adenosine receptor biased agonists in the treatment of heart failure. Front. Pharmacol. 12: 628060

Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Šenel P, Stewart GD, Liang Y-L, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D (2020)  Differential GLP-1R binding and activation by peptide and non-peptide agonists. Mol. Cell 80(3):485-500. e7. doi: 10.1016/j.molcel.2020.09.020

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

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

Hellmann J, Drabek M, Yin J, Gunera J, Pröll T, Frank Kraus F, Langmead CJ, Hübner H, Weikert D, Kolb P, Rosenbaum DM, Gmeiner P. (2020) Structure-based development of a subtype-selective orexin 1 receptor antagonist. PNAS 117(30): 18059-18067

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

Josephs TM, Keller AN, Khajehali E, DeBono A, Langmead CJ, Conigrave AD, Capuano B, Kufareva I, Gregory KJ, Leach K.  (2020) Negative allosteric modulators of the human calcium-sensing receptor bind to overlapping and distinct sites within 7-transmembrane domain.  Br. J. Pharmacol. 177(8):1917-1930. doi: 10.1111/bph.14961

Ramírez-García PD, Retamal JS, Shenoy P, Imlach W, Sykes M, Truong N, Constandil L, Pelissier T, Nowell CJ, Khor SY, Layani LM, Lumb C, Poole DP, Lieu T, Stewart GD, Mai QN, Jensen DD, Latorre R, Scheff NN, Schmidt BL, Quinn JF, Whittaker MR, Veldhuis NA, Davis TP, Bunnett NW. (2019)  A pH-responsive nanoparticle targets the neurokinin 1 receptor in endosomes to prebvent chronic pain.  Nat. Nanotechnol. 14(12):1150-1159. doi: 10.1038/s41565-019-0568-x

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. (2019) Crystal structure of the M5 muscarinic acetylcholine receptor.  Proc. Natl. Acad. Sci. U S A. 116(51):26001-26007. doi: 10.1073/pnas.1914446116

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

Riddy DM, Goy E, Delerive P, Summers RJ, Sexton PM, Langmead CJ.  (2018) Comparative genotypic and phenotypic analysis of human peripheral blood monocytes and surrogate monocyte-like cell lines commonly used in metabolic disease research.  PLoS One. 13(5):e0197177. doi: 10.1371/journal.pone.0197177

Stewart GD,  Comps-Agrar L, Nørskov-Lauritsen LB,  Pin J-P, Kniazeff J. (2018) Allosteric interactions between GABA B1 subunits control orthosteric binding sites occupancy within GABA B oligomers.  Neuropharmacology. 136(Pt A):92-101. doi: 10.1016/j.neuropharm.2017.12.042

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

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

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

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. (2018) 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. 9(7):1572-1581. doi: 10.1021/acschemneuro.8b00126

Diepenhorst NA, Leach K, Keller AN, Rueda P, Cook AE, Pierce TL, Nowell C, Pastoureau P, Sabatini M, Summers RJ, Charman WN, Sexton PM, Christopoulos A, Langmead CJ. (2018) Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity.  Br. J. Pharmacol. 175(21):4095-4108. doi: 10.1111/bph.14344

Sengmany K, Singh J, Stewart GD, Conn PJ, Christopoulos A, Gregory KJ. (2017) Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery.  Neuropharmacology. 115:60-72. doi: 10.1016/j.neuropharm.2016.07.001

Riddy DM, Cook AE, Diepenhorst NA, Bosnyak S, Brady R, Mannoury la Cour C, Mocaer E, Summers RJ, Charman WN, Sexton PM, Christopoulos A, Langmead CJ. (2017)  Isoform-specific biased agonism of histamine H3 receptor agonists.  Mol. Pharmacol. 91(2):87-99. doi: 10.1124/mol.116.106153 Erratum in: Mol.  Pharmacol. 91(3):263, 2017

Diepenhorst NA, Nowell CJ, Rueda P, Henriksen K, Pierce T, Cook AE, Pastoureau P, Sabatini M, Charman WN, Christopoulos A, Summers RJ, Sexton PM, Langmead CJ.  (2017) High throughput, quantitative analysis of human osteoclast differentiation and activity.  Anal. Biochem. 2017 519:51-56. doi: 10.1016/j.ab.2016.12.010

Mølck C, Ryall J, Failla LM, Coates JL, Pascussi J-M, Heath JK, Stewart GD, Hollande F. (2016) The A 2b adenosine receptor antagonist PSB-603 promotes oxidative phosphorylation and ROS production in colorectal cancer cells via adenosine receptor-independent mechanism. Cancer Letters 383(1):135-143. doi: 10.1016/j.canlet.2016.09.018

Rueda P, Harley E, Lu Y, Stewart GD, Fabb S, Diepenhorst N, Cremers B, Rouillon MH, Wehrle I, Geant A, Lamarche G, Leach K, Charman WN, Christopoulos A, Summers RJ, Sexton PM, Langmead CJ. (2016)  Murine GPRC6A mediates cellular responses to L-amino acids, but not osteocalcin variants.  PLoS One. 11(1):e0146846. doi: 10.1371/journal.pone.0146846

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

Berizzi AE, Gentry PR, Rueda P, Den Hoedt S, Sexton PM, Langmead CJ, Christopoulos A. (2016)  Molecular mechanisms of action of M5 muscarinic acetylcholine receptor allosteric modulators.  Mol. Pharmacol. 90(4):427-36. doi: 10.1124/mol.116.104182

Riddy DM, Valant C, Rueda P, Charman WN, Sexton PM, Summers RJ, Christopoulos A, Langmead CJ. (2015)  Label-free kinetics: Exploiting functional hemi-equilibrium to derive rate constants for muscarinic receptor antagonists.  Mol. Pharmacol. 88(4):779-90. doi: 10.1124/mol.115.100545


Langmead CJ (ed). Advances in Pharmacology: From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors. Cambridge, MA, Elsevier. 2020 doi: 10.1016/S1054-3589(20)30037-5

Reviews & Editorials

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

Park JLangmead CJ, Riddy DM. (2020)  New advances in targeting the resolution of inflammation:  Implications for specialized pro-resolving mediator GPCR drug discovery.  ACS Pharmacol. Transl. Sci. 3(1):88-106. doi: 10.1021/acsptsci.9b00075

Gogos A, Langmead C, Sullivan JC, Lawrence, AJ. (2019) The importance of sex differences in pharmacology research. Br. J. Pharmacol. 176 (21): 4087-4089. doi: 10.1111/bph.14819

Sek K, Mølck C, Stewart GD, Kats L, Darcy PK, Beavis PA (2018) Targeting adenosine receptor signaling in cancer immunotherapy. Int. J. Mol. Sci. 19(12):3837. doi: 10.3390/ijms19123837

Langmead CJ, Summers RJ. (2018) Molecular pharmacology of GPCRs.  Br. J. Pharmacol. 175(21):4005-4008. doi: 10.1111/bph.14474

Riddy DM, Delerive P, Summers RJ, Sexton PM, Langmead CJ. (2018) G protein-coupled receptors targeting insulin resistance, obesity and type 2 diabetes mellitus.  Pharmacol. Rev. 70(1):39-67. doi: 10.1124/pr.117.014373

Diepenhorst N, Rueda P, Cook AE, Pastoureau P, Sabatini M, Langmead CJ. (2018)  G protein-coupled receptors as anabolic drug targets in osteoporosis.  Pharmacol. Ther. 184:1-12. doi: 10.1016/j.pharmthera.2017.10.015

Christopoulos A, Changeux JP, Catterall WA, Fabbro D, Burris TP, Cidlowski JA, Olsen RW, Peters JA, Neubig RR, Pin JP, Sexton PM, Kenakin TP, Ehlert FJ, Spedding M, Langmead CJ. (2014)  International Union of Basic and Clinical Pharmacology.XC. multisite pharmacology:  recommendations for the nomenclature of receptor allosterism and allosteric ligands.  Pharmacol. Rev. 66(4):918-47. doi: 10.1124/pr.114.008862

Langmead CJ, Christopoulos A. (2014)  Functional and structural perspectives on allosteric modulation of GPCRs.  Curr. Opin. Cell Biol. 27:94-101. doi: 10.1016/

Langmead CJ, Christopoulos A. (2013) Supra-physiological efficacy at GPCRs: superstition or super agonists?  Br. J. Pharmacol. 169(2):353-6. doi: 10.1111/bph.12142