A complete publication list can be found here.

Key research papers

Dinh LV, DeBono A, Keller AN, Josephs TM, Gregory KJ, Leach K, Capuano B (2021) “Development of AC265347-Inspired Calcium-Sensing Receptor Ago-Positive Allosteric Modulators” ChemMedChem 16, 22, 3451-3462.

Arsova A, Møller TC, Hellyer SD, Vedel L, Foster SR, Hansen JL, Bräuner-Osborne H & Gregory KJ, (2021) “Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 as Tool Compounds to Study Signaling Bias” Molecular Pharmacology. 99, 5, 328-341

Hellyer SD, Aggarwal S, Chen ANY, Leach K, Lapinsky DJ & Gregory KJ, (2020), “Development of Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 2 Based on Two Positive Allosteric Modulator Chemotypes” ACS Chemical Neuroscience. 11, 11, 1597-1609

Sengmany K, Hellyer SD, Christopoulos A, Lapinsky DJ, Leach K & Gregory KJ (2020) “Differential contribution of metabotropic glutamate receptor 5 common allosteric binding site residues to biased allosteric agonism” Biochemical Pharmacology. 177, 114011

Chen ANY, Hellyer SD, Trinh PNH, Leach K & Gregory KJ (2020) “Identification of monellin as the first naturally derived proteinaceous allosteric agonist of metabotropic glutamate receptor 5” Basic & Clinical Pharmacology & Toxicology. 126, S6, 104-115

Hellyer SD, Sengmany K, Keller AN, Christopoulos A, Leach K & Gregory KJ, (2020) “Probe dependence and biased potentiation of metabotropic glutamate receptor 5 is mediated by differential ligand interactions in the common allosteric binding site” Biochemical Pharmacology. 177, 114013

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

Mun HC, Leach K, Conigrave AD (2019) “L-Amino Acids Promote Calcitonin Release via a Calcium-Sensing Receptor: Gq/11-Mediated Pathway in Human C-Cells” Endocrinology 160(7): 1590-1599

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

Keller AN, Kufareva I, Josephs TM, Diao J, Mai VT, Conigrave AD, Christopoulos A, Gregory KJ, Leach K (2018) “Identification of Global and Ligand-Specific Calcium Sensing Receptor Activation Mechanisms” Mol Pharmacol 93(6): 619-630

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

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, 15:115:60-72

Nickols HH, Yuh JP, Gregory KJ, Morrison RD, Bates BS, Stauffer SR, Emmitte KA, Bubser M, Peng W, Nedelcovych MT, Thompson A, Lv X, Xiang Z, Daniels JS, Niswender CM, Lindsley CW, Jones CK, Conn PJ (2016) “VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy” J Pharmacol Exp Ther 356(1): 123-136

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

Gregory KJ, Velagaleti R, Thal DM, Brady RM, Christopoulos A, Conn PJ, Lapinsky DJ (2016) “Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators” ACS Chem Biol., 11(7):1870-9

Leach K, Gregory KJ, Kufareva I, Khajehali E, Cook, AE, Abagyan, Conigrave AD, Sexton PM and Christopoulos A (2016) “Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor Cell Research, 26(5):574-92

Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans D, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK & Christopoulos A (2016) “Crystal structures of the M1 and M4 muscarinic acetylcholine receptors and insights into their allosteric modulation” Nature, 531:335-40.

Nickols HH, Yuh JP, Gregory KJ, Morrison RD, Bates BS, Stauffer SR, Emmitte KA, Bubser M, Peng W, Nedelcovych MT, Thompson A, Lv X, Xiang Z, Daniels JS, Niswender CM, Lindsley CW, Jones CK, Conn PJ (2016) “VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy” J Pharmacol Exp Ther., 356(1):123-36

Khajehali E, Malone DT, Glass M, Sexton PM, Christopoulos A & Leach K (2015) “Biased agonism and biased modulation at the CB1 cannabinoid receptor” Mol. Pharmacol. 88(2):368-379

Rook JM, Xiang Z, Lv X, Ghoshal A, Dickerson JW, Bridges TM, Johnson KA, Foster DJ, Gregory KJ, Vinson PN, Thompson AD, Byun N, Collier RL, Bubser M, Nedelcovych MT, Gould RW, Stauffer SR, Daniels JS, Niswender CM, Lavreysen H, Mackie C, Conde-Ceide S, Alcazar J, Bartolome-Nebreda JM, Macdonald GJ, Talpos JC, Steckler T, Jones CK, Lindsley CW & Conn PJ (2015) “Biased mGlu5-positive allosteric modulators provide in vivo efficacy without potentiating mGlu5 modulation of NMDAR currents” Neuron 86(4):1029-1040

Cook AE, Mistry SN, Gregory KJ, Furness SG, Sexton PM, Scammells PJ, Conigrave AD, Christopoulos A & Leach K (2014) “Biased allosteric modulation at the CaSR engendered by structurally diverse calcimimetics” Br. J. Pharmacol. 172(1):185-200

Wu H, Wang C, Gregory KJ, Han GW, Cho HP, Xia Y, Niswender CM, Katrich V, Meiler J, Cherezov V, Conn PJ & Stevens RC (2014) “Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator” Science 344(6179)58-64

Gregory KJ, Nguyen ED, Malosh C, Mendenhall JL, Zic JZ, Bates BS, Noetzel MJ, Squire EF, Turner EM, Rook JM, Emmitte KA, Stauffer SR, Lindsley CW, Meiler J & Conn PJ (2014) “Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site” ACS Chem. Neurosci. 5(4)282-295

Yin S, Noetzel MJ, Johnson KA, Zamorano R, Jalan-Sakrikar N, Gregory KJ, Conn PJ & Niswender CM (2014) “Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS” J. Neurosci. 34(1):79-94

Avlani V, Ma W, Mun HC, Leach K, Delbridge L, Christopoulos A & Conigrave AD (2013) “Calcium-sensing receptor-dependent activation of CREB phosphorylation in HEK293 cells and human parathyroid cells” Am. J Physiol. Endocrino.l Metab. 304(10):E1097-104

Leach K, Wen A, Cook AE, Conigrave AD, Sexton PM & Christopoulos A (2013) “Impact of clinically relevant mutations on the pharmacoregulation and signalling bias of the calcium-sensing receptor by positive and negative allosteric modulators”Endocrinology 154(3):1105-16

Gregory KJ, Nguyen ED, Reiff SD, Squire EF, Stauffer SR, Lindsley CW, Meiler J & Conn PJ (2013) “Probing the Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulator (PAM) Binding Pocket: Discovery of Point Mutations That Engender a “Molecular Switch” in PAM Pharmacology” Mol. Pharmacol. 83(5):991-1006

Leach K, Wen A, Davey AE, Conigrave AD, Sexton PM & Christopuolos A (2012) “Identification of molecular phenotypes and biased signalling induced by naturally occurring mutations of the human calcium-sensing receptor”Endocrinology 153(9)4304-16

Davey AE, Leach K, Valant C, Conigrave AD, Sexton PM & Christopoulos A (2012) “Positive and negative allosteric modulators promote biased signalling at the calcium-sensing receptor” Endocrinology 153(3):1232-41

Gregory KJ, Sexton PM, Tobin AB & Christopoulos A (2012) “Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor” J Biol Chem 287(44):37066-77

Gregory KJ, Noetzel MJ, Rook JM, Vinson PJ, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM & Conn PJ (2012) “Investigating mGlu5 allosteric modulator cooperativity, affinity and agonism: enriching structure-function studies and structure-activity relationships” Mol Pharmacol. 82(5):860-75

Review papers

Gregory KJ (2019) “How an activation signal is transmitted through an excitatory receptor” Nature 566(7742): 42-43

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

Leach K and Gregory KJ (2017) “Molecular insights into allosteric modulation of Class C G protein-coupled receptors” Pharmacol Res., 116:105-118

Hellyer S, Leach K and Gregory KJ (2017) “Neurobiological insights and novel therapeutic opportunities for CNS disorders from mGlu receptor allosteric and biased modulation” Curr Opin Pharmacol. 32:49-55.

Lindsley CW, Emmitte KA, Hopkins CR, Bridges TM, Gregory KJ, Niswender CM, Conn PJ (2016) “Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors” Chem Rev., 116(11):6707-41

Sengmany K & Gregory KJ (2016) “Metabotropic glutamate receptor 5: molecular pharmacology, allosteric modulation and stimulus-bias” Br J Pharmacol 173(20):3001-17

Leach K, Conigrave AD, Sexton PM & Christopoulos A (2015) “Towards tissue-specific pharmacology: insights from the calcium-sensing receptor as a paradigm for GPCR (patho)physiological bias” Trends Pharmacol. Sci. 36(4):215-225