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"Selective" Class C G protein-coupled receptor modulators are neutral or biased mGlu5 allosteric ligands.

Hellyer SD, Albold S, Wang T, Chen AN, May LT, Leach K, Gregory KJ.

Mol Pharmacol. 2018 Mar 7. pii: mol.117.111518. doi: 10.1124/mol.117.111518. [Epub ahead of print]


Regulation of early growth response 2 expression by secreted frizzled related protein 1.

Gregory KJ, Morin SM, Schneider SS.

BMC Cancer. 2017 Jul 7;17(1):473. doi: 10.1186/s12885-017-3426-y.


Molecular insights into allosteric modulation of Class C G protein-coupled receptors.

Leach K, Gregory KJ.

Pharmacol Res. 2017 Feb;116:105-118. doi: 10.1016/j.phrs.2016.12.006. Epub 2016 Dec 11. Review.


Neurobiological insights and novel therapeutic opportunities for CNS disorders from mGlu receptor allosteric and biased modulation.

Hellyer S, Leach K, Gregory KJ.

Curr Opin Pharmacol. 2017 Feb;32:49-55. doi: 10.1016/j.coph.2016.10.007. Epub 2016 Nov 11. Review.


Extracellular Loop 2 of the Adenosine A1 Receptor Has a Key Role in Orthosteric Ligand Affinity and Agonist Efficacy.

Nguyen AT, Baltos JA, Thomas T, Nguyen TD, Muñoz LL, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT.

Mol Pharmacol. 2016 Dec;90(6):703-714. Epub 2016 Sep 28.


Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

Nguyen AT, Vecchio EA, Thomas T, Nguyen TD, Aurelio L, Scammells PJ, White PJ, Sexton PM, Gregory KJ, May LT, Christopoulos A.

Mol Pharmacol. 2016 Dec;90(6):715-725. Epub 2016 Sep 28.


Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery.

Sengmany K, Singh J, Stewart GD, Conn PJ, Christopoulos A, Gregory KJ.

Neuropharmacology. 2017 Mar 15;115:60-72. doi: 10.1016/j.neuropharm.2016.07.001. Epub 2016 Jul 5.


Structure-Activity Analysis of Biased Agonism at the Human Adenosine A3 Receptor.

Baltos JA, Paoletta S, Nguyen AT, Gregory KJ, Tosh DK, Christopoulos A, Jacobson KA, May LT.

Mol Pharmacol. 2016 Jul;90(1):12-22. doi: 10.1124/mol.116.103283. Epub 2016 May 2.


Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators.

Gregory KJ, Velagaleti R, Thal DM, Brady RM, Christopoulos A, Conn PJ, Lapinsky DJ.

ACS Chem Biol. 2016 Jul 15;11(7):1870-9. doi: 10.1021/acschembio.6b00026. Epub 2016 May 4.


Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor.

Leach K, Gregory KJ, Kufareva I, Khajehali E, Cook AE, Abagyan R, Conigrave AD, Sexton PM, Christopoulos A.

Cell Res. 2016 May;26(5):574-92. doi: 10.1038/cr.2016.36. Epub 2016 Mar 22.


Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

Lindsley CW, Emmitte KA, Hopkins CR, Bridges TM, Gregory KJ, Niswender CM, Conn PJ.

Chem Rev. 2016 Jun 8;116(11):6707-41. doi: 10.1021/acs.chemrev.5b00656. Epub 2016 Feb 16. Review.


Ligand-Independent Adenosine A2B Receptor Constitutive Activity as a Promoter of Prostate Cancer Cell Proliferation.

Vecchio EA, Tan CY, Gregory KJ, Christopoulos A, White PJ, May LT.

J Pharmacol Exp Ther. 2016 Apr;357(1):36-44. doi: 10.1124/jpet.115.230003. Epub 2016 Jan 20.


Quantification of adenosine A(1) receptor biased agonism: Implications for drug discovery.

Baltos JA, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT.

Biochem Pharmacol. 2016 Jan 1;99:101-12. doi: 10.1016/j.bcp.2015.11.013. Epub 2015 Nov 12.


VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy.

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.

J Pharmacol Exp Ther. 2016 Jan;356(1):123-36. doi: 10.1124/jpet.115.226597. Epub 2015 Oct 26.


Metabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus bias.

Sengmany K, Gregory KJ.

Br J Pharmacol. 2016 Oct;173(20):3001-17. doi: 10.1111/bph.13281. Epub 2015 Nov 11. Review.


Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents.

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, Bartolomé-Nebreda JM, Macdonald GJ, Talpos JC, Steckler T, Jones CK, Lindsley CW, Conn PJ.

Neuron. 2015 May 20;86(4):1029-1040. doi: 10.1016/j.neuron.2015.03.063. Epub 2015 Apr 30.


Identification of a high affinity MPEP-site silent allosteric modulator (SAM) for the metabotropic glutamate subtype 5 receptor (mGlu5).

Gregory KJ, Malosh C, Turlington M, Morrison R, Vinson P, Daniels JS, Jones C, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Apr 15 [updated 2015 Feb 11].


Estrogen-mediated signaling is differentially affected by the expression levels of Sfrp1 in mammary epithelial cells.

Gregory KJ, Schneider SS.

Cell Biol Int. 2015 Jul;39(7):873-9. doi: 10.1002/cbin.10468. Epub 2015 May 5.


Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation.

Gregory KJ, Conn PJ.

Mol Pharmacol. 2015 Jul;88(1):188-202. doi: 10.1124/mol.114.097220. Epub 2015 Mar 25.


Measurement uncertainty analysis of low-dose-rate prostate seed brachytherapy: post-implant dosimetry.

Gregory KJ, Pattison JE, Bibbo G.

Australas Phys Eng Sci Med. 2015 Mar;38(1):71-81. doi: 10.1007/s13246-014-0325-2. Epub 2015 Jan 3.


Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7.

Jalan-Sakrikar N, Field JR, Klar R, Mattmann ME, Gregory KJ, Zamorano R, Engers DW, Bollinger SR, Weaver CD, Days EL, Lewis LM, Utley TJ, Hurtado M, Rigault D, Acher F, Walker AG, Melancon BJ, Wood MR, Lindsley CW, Conn PJ, Xiang Z, Hopkins CR, Niswender CM.

ACS Chem Neurosci. 2014 Dec 17;5(12):1221-37. doi: 10.1021/cn500153z. Epub 2014 Oct 9.


Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics.

Cook AE, Mistry SN, Gregory KJ, Furness SG, Sexton PM, Scammells PJ, Conigrave AD, Christopoulos A, Leach K.

Br J Pharmacol. 2015 Jan;172(1):185-200. doi: 10.1111/bph.12937. Epub 2014 Dec 1.


Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator.

Wu H, Wang C, Gregory KJ, Han GW, Cho HP, Xia Y, Niswender CM, Katritch V, Meiler J, Cherezov V, Conn PJ, Stevens RC.

Science. 2014 Apr 4;344(6179):58-64. doi: 10.1126/science.1249489. Epub 2014 Mar 6.


Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site.

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.

ACS Chem Neurosci. 2014 Apr 16;5(4):282-95. doi: 10.1021/cn400225x. Epub 2014 Feb 26.


Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS.

Yin S, Noetzel MJ, Johnson KA, Zamorano R, Jalan-Sakrikar N, Gregory KJ, Conn PJ, Niswender CM.

J Neurosci. 2014 Jan 1;34(1):79-94. doi: 10.1523/JNEUROSCI.1129-13.2014.


Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).

Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, Meiler J, Conn PJ, Lindsley CW, Stauffer SR.

J Med Chem. 2013 Oct 24;56(20):7976-96. doi: 10.1021/jm401028t. Epub 2013 Oct 9.


Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5.

Rodriguez AL, Tarr JC, Zhou Y, Williams R, Gregory KJ, Bridges TM, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 17 [updated 2013 Mar 22].


N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.

Gregory KJ, Herman EJ, Ramsey AJ, Hammond AS, Byun NE, Stauffer SR, Manka JT, Jadhav S, Bridges TM, Weaver CD, Niswender CM, Steckler T, Drinkenburg WH, Ahnaou A, Lavreysen H, Macdonald GJ, Bartolomé JM, Mackie C, Hrupka BJ, Caron MG, Daigle TL, Lindsley CW, Conn PJ, Jones CK.

J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. doi: 10.1124/jpet.113.206623. Epub 2013 Aug 21.


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.

Gregory KJ, Nguyen ED, Reiff SD, Squire EF, Stauffer SR, Lindsley CW, Meiler J, Conn PJ.

Mol Pharmacol. 2013 May;83(5):991-1006. doi: 10.1124/mol.112.083949. Epub 2013 Feb 26.


Pharmacology of metabotropic glutamate receptor allosteric modulators: structural basis and therapeutic potential for CNS disorders.

Gregory KJ, Noetzel MJ, Niswender CM.

Prog Mol Biol Transl Sci. 2013;115:61-121. doi: 10.1016/B978-0-12-394587-7.00002-6. Review.


A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling.

Noetzel MJ, Gregory KJ, Vinson PN, Manka JT, Stauffer SR, Lindsley CW, Niswender CM, Xiang Z, Conn PJ.

Mol Pharmacol. 2013 Apr;83(4):835-47. doi: 10.1124/mol.112.082891. Epub 2013 Jan 24. Erratum in: Mol Pharmacol. 2013 Oct;84(4):654.


Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.

Rook JM, Noetzel MJ, Pouliot WA, Bridges TM, Vinson PN, Cho HP, Zhou Y, Gogliotti RD, Manka JT, Gregory KJ, Stauffer SR, Dudek FE, Xiang Z, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ.

Biol Psychiatry. 2013 Mar 15;73(6):501-9. doi: 10.1016/j.biopsych.2012.09.012. Epub 2012 Nov 7.


Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.

Manka JT, Vinson PN, Gregory KJ, Zhou Y, Williams R, Gogi K, Days E, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2012 Oct 15;22(20):6481-5. doi: 10.1016/j.bmcl.2012.08.043. Epub 2012 Aug 24.


Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor.

Gregory KJ, Sexton PM, Tobin AB, Christopoulos A.

J Biol Chem. 2012 Oct 26;287(44):37066-77. doi: 10.1074/jbc.M112.408534. Epub 2012 Sep 10.


Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.

Gregory KJ, Noetzel MJ, Rook JM, Vinson PN, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM, Conn PJ.

Mol Pharmacol. 2012 Nov;82(5):860-75. doi: 10.1124/mol.112.080531. Epub 2012 Aug 3.


Rapid and direct microRNA quantification by an enzymatic luminescence assay.

Sun Y, Gregory KJ, Chen NG, Golovlev V.

Anal Biochem. 2012 Oct 1;429(1):11-7. doi: 10.1016/j.ab.2012.06.021. Epub 2012 Jul 1.


Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.

Mueller R, Dawson ES, Meiler J, Rodriguez AL, Chauder BA, Bates BS, Felts AS, Lamb JP, Menon UN, Jadhav SB, Kane AS, Jones CK, Gregory KJ, Niswender CM, Conn PJ, Olsen CM, Winder DG, Emmitte KA, Lindsley CW.

ChemMedChem. 2012 Mar 5;7(3):406-14. doi: 10.1002/cmdc.201100510. Epub 2012 Jan 20. No abstract available.


Overview of receptor allosterism.

Gregory KJ, Sexton PM, Christopoulos A.

Curr Protoc Pharmacol. 2010 Dec;Chapter 1:Unit 1.21. doi: 10.1002/0471141755.ph0121s51.


Allosteric modulation of metabotropic glutamate receptors.

Sheffler DJ, Gregory KJ, Rook JM, Conn PJ.

Adv Pharmacol. 2011;62:37-77. doi: 10.1016/B978-0-12-385952-5.00010-5. Review.


Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.

Hammond AS, Rodriguez AL, Townsend SD, Niswender CM, Gregory KJ, Lindsley CW, Conn PJ.

ACS Chem Neurosci. 2010 Oct 20;1(10):702-716. Epub 2010 Aug 19.


Vitamin D binding protein-macrophage activating factor directly inhibits proliferation, migration, and uPAR expression of prostate cancer cells.

Gregory KJ, Zhao B, Bielenberg DR, Dridi S, Wu J, Jiang W, Huang B, Pirie-Shepherd S, Fannon M.

PLoS One. 2010 Oct 18;5(10):e13428. doi: 10.1371/journal.pone.0013428.


Real-time bioluminescent assay for inhibitors of RNA and DNA polymerases and other ATP-dependent enzymes.

Gregory KJ, Sun Y, Chen NG, Golovlev V.

Anal Biochem. 2011 Jan 15;408(2):226-34. doi: 10.1016/j.ab.2010.08.016. Epub 2010 Aug 18.


Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential.

Gregory KJ, Dong EN, Meiler J, Conn PJ.

Neuropharmacology. 2011 Jan;60(1):66-81. doi: 10.1016/j.neuropharm.2010.07.007. Epub 2010 Jul 14. Review.


Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias.

Gregory KJ, Hall NE, Tobin AB, Sexton PM, Christopoulos A.

J Biol Chem. 2010 Mar 5;285(10):7459-74. doi: 10.1074/jbc.M109.094011. Epub 2010 Jan 5.


Uncertainties in effective dose estimates of adult CT head scans: the effect of head size.

Gregory KJ, Bibbo G, Pattison JE.

Med Phys. 2009 Sep;36(9):4121-5.


Reduction of sample evaporation in small volume microplate luminescence assays.

Gregory KJ, Sun Y.

Anal Biochem. 2009 Apr 15;387(2):321-3. doi: 10.1016/j.ab.2009.01.034. Epub 2009 Feb 3.


Efficiency and specificity of microRNA-primed nucleotide analog incorporation by various DNA polymerases.

Sun Y, Gregory KJ, Golovlev V.

Anal Biochem. 2009 Aug 15;391(2):85-90. doi: 10.1016/j.ab.2009.05.010. Epub 2009 May 12.


Adaptive memory: fitness relevance and the hunter-gatherer mind.

Nairne JS, Pandeirada JN, Gregory KJ, Van Arsdall JE.

Psychol Sci. 2009 Jun;20(6):740-6. doi: 10.1111/j.1467-9280.2009.02356.x. Epub 2009 May 5.


On the uncertainties in effective dose estimates of adult CT head scans.

Gregory KJ, Bibbo G, Pattison JE.

Med Phys. 2008 Aug;35(8):3501-10.


A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand.

Valant C, Gregory KJ, Hall NE, Scammells PJ, Lew MJ, Sexton PM, Christopoulos A.

J Biol Chem. 2008 Oct 24;283(43):29312-21. doi: 10.1074/jbc.M803801200. Epub 2008 Aug 22.

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