Karen Gregory

Dr

20052021
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Research Output 2005 2019

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2019

Identification of monellin as the first naturally derived proteinaceous allosteric agonist of metabotropic glutamate receptor 5

Chen, A. N. Y., Hellyer, S. D., Trinh, P. N. H., Leach, K. & Gregory, K. J., 14 Apr 2019, (Accepted/In press) In : Basic and Clinical Pharmacology and Toxicology. 22 p.

Research output: Contribution to journalArticleResearchpeer-review

Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology

Sengmany, K., Hellyer, S. D., Albold, S., Wang, T., Conn, P. J., May, L. T., Christopoulos, A., Leach, K. & Gregory, K. J., 1 May 2019, In : Neuropharmacology. 149, p. 83-96 14 p.

Research output: Contribution to journalArticleResearchpeer-review

2018

Identification of global and ligand-specific calcium sensing receptor activation mechanisms S

Keller, A., Kufareva, I., Josephs, T. M., Diao, J., Mai, V. T-V., Conigrave, A. D., Christopoulos, A., Gregory, K. J. & Leach, K., 1 Jun 2018, In : Molecular Pharmacology. 93, 6, p. 619-630 12 p.

Research output: Contribution to journalArticleResearchpeer-review

“Selective” class C G protein-coupled receptor modulators are neutral or biased mGlu5 allosteric ligands

Hellyer, S. D., Albold, S., Wang, T., Chen, A. N. Y., May, L. T., Leach, K. & Gregory, K. J., 1 May 2018, In : Molecular Pharmacology. 93, 5, p. 504-514 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2017

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

Sengmany, K., Singh, J., Stewart, G. D., Conn, P. J., Christopoulos, A. & Gregory, K. J., 15 Mar 2017, In : Neuropharmacology. 115, p. 60-72 13 p.

Research output: Contribution to journalArticleResearchpeer-review

THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview

Alexander, S. P. H., Kelly, E., Marrion, N. V., Peters, J. A., Faccenda, E., Harding, S. D., Pawson, A. J., Sharman, J. L., Southan, C., Buneman, O. P., Cidlowski, J. A., Christopoulos, A., Davenport, A. P., Fabbro, D., Spedding, M., Striessnig, J., Davies, J. A. & CGTP Collaborators, 1 Dec 2017, In : British Journal of Pharmacology. 174, S1, p. S1-S16 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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2016

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

Gregory, K., Velagaleti, R., Thal, D. M., Brady, R. M., Christopoulos, A., Conn, P. J. & Lapinsky, D. J., 15 Jul 2016, In : ACS Chemical Biology. 11, 7, p. 1870-1879 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Extracellular loop 2 of the adenosine A1 receptor has a key role in orthosteric ligand affinity and agonist efficacy

Nguyen, A. T. N., Baltos, J-A., Thomas, T., Nguyen, T. D., Lopez Munoz, L., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A. & May, L. T., 1 Dec 2016, In : Molecular Pharmacology. 90, 6, p. 703-714 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Ligand-independent adenosine A2B receptor constitutive activity as a promoter of prostate cancer cell proliferation

Vecchio, E. A., Tan, C. Y. R., Gregory, K., Christopoulos, A., White, P. J. & May, L. T., 1 Apr 2016, In : Journal of Pharmacology and Experimental Therapeutics. 357, 1, p. 36-44 9 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Sengmany, K. & Gregory, K. J., 1 Oct 2016, In : British Journal of Pharmacology. 173, 20, p. 3001-3017 17 p.

Research output: Contribution to journalArticleResearchpeer-review

Quantification of adenosine A1 receptor biased agonism: Implications for drug discovery

Baltos, J-A., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A. & May, L. T., 1 Jan 2016, In : Biochemical Pharmacology. 99, p. 101-112 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling, and cooperativity

Nguyen, A. T. N., Vecchio, E. A., Thomas, T., Nguyen, T. D., Aurelio, L., Scammells, P. J., White, P. J., Sexton, P. M., Gregory, K. J., May, L. T. & Christopoulos, A., 1 Dec 2016, In : Molecular Pharmacology. 90, 6, p. 715-725 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Structure-activity analysis of biased agonism at the human adenosine A3 receptor

Baltos, J-A., Paoletta, S., Nguyen, A. T. N., Gregory, K. J., Tosh, D. K., Christopoulos, A., Jacobson, K. A. & May, L. T., 1 Jul 2016, In : Molecular Pharmacology. 90, 1, p. 12-22 11 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Leach, K., Gregory, K., Kufareva, I., Khajehali, E., Cook, A. E., Abagyan, R., Conigrave, A. D., Sexton, P. M. & Christopoulos, A., 1 May 2016, In : Cell Research. 26, 5, p. 574-592 19 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Nickols, H. H., Yuh, J. P., Gregory, K. J., Morrison, R. D., Bates, B. S., Stauffer, S. R., Emmitte, K. A., Bubser, M., Peng, W., Nedelcovych, M. T., Thompson, A. D., Lv, X., Xiang, Z., Daniels, J. S., Niswender, C. M., Lindsley, C. W., Jones, C. K. & Conn, P. J., 1 Jan 2016, In : Journal of Pharmacology and Experimental Therapeutics. 356, 1, p. 123-136 14 p.

Research output: Contribution to journalArticleResearchpeer-review

2015

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

Cook, A. E., Mistry, S. N., Gregory, K. J., Furness, S. G. B., Sexton, P., Scammells, P. J., Conigrave, A., Christopoulos, A. & Leach, K., 2015, In : British Journal of Pharmacology. 172, 1, p. 185 - 200 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Biased mGlu5-positive allosteric modulators provide in vivo efficacy without potentiating mGlu5 modulation of NMDAR currents

Rook, J. M., Xiang, Z., Lv, X., Ghoshal, A., Dickerson, J. W., Bridges, T. M., Johnson, K. A., Foster, D. J., Gregory, K. J., Vinson, P. N., Thompson, A. D., Byun, N., Collier, R. L., Bubser, M., Nebelcovych, M. T., Gould, R. W., Stauffer, S. R., Daniels, J. S., Niswender, C. M., Lavreysen, H. & 10 othersMackie, C., Conde-Ceide, S., Alcazar, J., Bartolome-Nebreda, J. M., Macdonald, G. J., Talpos, J. C., Steckler, T., Jones, C. K., Lindsley, C. W. & Conn, P. J., 2015, In : Neuron. 86, 4, p. 1029-1040 12 p.

Research output: Contribution to journalArticleResearchpeer-review

2014

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, J. R., Klar, R., Mattmann, M. E., Gregory, K. J., Zamorano, R., Engers, D. W., Bollinger, S. R., Weaver, C. D., Days, E., Lewis, L. M., Utley, T. J., Hurtado, M. A., Rigault, D., Acher, F. C., Walker, A. G., Melancon, B. J., Wood, M. R., Lindsley, C. W., Conn, P. J. & 3 othersXiang, Z., Hopkins, C. R. & Niswender, C. M., 2014, In : ACS Chemical Neuroscience. 5, 12, p. 1221 - 1237 17 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Gregory, K. J., Nguyen, E. D., Malosh, C. F., Mendenhall, J. L., Zic, J. Z., Bates, B. S., Noetzel, M. J., Squire, E. F., Turner, E. M., Rook, J. M., Emmitte, K. A., Stauffer, S. R., Lindsley, C. W., Meiler, J. & Conn, P. J., 2014, In : ACS Chemical Neuroscience. 5, 4, p. 282 - 295 14 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Yin, S., Noetzel, M. J., Johnson, K. A., Zamorano, R., Jalan-Sakrikar, N., Gregory, K. J., Conn, P. J. & Niswender, C. M., 2014, In : Journal of Neuroscience. 34, 1, p. 79 - 94 16 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Wu, H., Wang, C., Gregory, K. J., Han, G. W., Cho, H. P., Xia, Y., Niswender, C. M., Katritch, V., Meiler, J., Cherezov, V., Conn, P. J. & Stevens, R. C., 2014, In : Science. 344, 6179, p. 58 - 64 7 p.

Research output: Contribution to journalArticleResearchpeer-review

2013

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

Noetzel, M. J., Gregory, K. J., Vinson, P. N., Manka, J. T., Stauffer, S. R., Lindsley, C. W., Niswender, C. M., Xiang, Z. & Conn, P. J., Apr 2013, In : Molecular Pharmacology. 83, 4, p. 835-847 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs)...

Turlington, M. L., Noetzel, M. J., Chun, A. C., Zhou, Y., Gogliotti, R. D., Nguyen, E. D., Gregory, K. J., Vinson, P. N., Rook, J. M., Gogi, K., Xiang, Z., Bridges, T. M., Daniels, J. S., Jones, C. K., Niswender, C. M., Meiler, J., Conn, P. J., Lindsley, C. W. & Stauffer, S. R., 2013, In : Journal of Medicinal Chemistry. 56, 20, p. 7976 - 7996 21 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Gregory, K. J., Herman, E. J., Ramsey, A. J., Hammond, A. S., Byun, N., Stauffer, S. R., Manka, J. T., Jadhav, S. B., Bridges, T. M., Weaver, C. D., Niswender, C. M., Steckler, T., Drinkenburg, W. H., Ahnaou, A., Lavreysen, H., Macdonald, G. J., Bartolome, J., Mackie, C., Hrupka, B. J., Caron, M. G. G. & 4 othersDaigle, T. L., Lindsley, C. W., Conn, P. J. & Jones, C. K., 2013, In : Journal of Pharmacology and Experimental Therapeutics. 347, 2, p. 438 - 457 20 p.

Research output: Contribution to journalArticleResearchpeer-review

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, K. J., Nguyen, E. D., Reiff, S. D., Squire, E. F., Stauffer, S. R., Lindsley, C. W., Meiler, J. & Conn, P. J., 2013, In : Molecular Pharmacology. 83, 5, p. 991 - 1006 16 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Rook, J. M., Noetzel, M. J., Pouliot, W. A., Bridges, T. M., Vinson, P. N., Cho, H. P., Zhou, Y., Gogliotti, R. D., Manka, J. T., Gregory, K. J., Stauffer, S. R., Dudek, F. E., Xiang, Z., Niswender, C. M., Daniels, J. S., Jones, C. K., Lindsley, C. W. & Conn, P. J., 2013, In : Biological Psychiatry. 73, 6, p. 501 - 509 9 p.

Research output: Contribution to journalArticleResearchpeer-review

2012

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

Mueller, R., Dawson, E. S., Meiler, J., Rodriguez, A. L., Chauder, B. A., Bates, B. S., Felts, A. S., Lamb, J. P., Menon, U. N., Jadhav, S. B., Kane, A. S., Jones, C. K., Gregory, K. J., Niswender, C. M., Conn, P. J., Olsen, C. M., Winder, D. G., Emmitte, K. A. & Lindsley, C. W., 2012, In : ChemMedChem. 7, 3, p. 406 - 414 9 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Gregory, K. J., Noetzel, M. J., Rook, J. M., Vinson, P. N., Stauffer, S. R., Rodriguez, A. L., Emmitte, K. A., Zhou, Y., Chun, A. C., Felts, A. S., Chauder, B. A., Lindsley, C. W., Niswender, C. M. & Conn, P. J., 2012, In : Molecular Pharmacology. 82, 5, p. 860 - 875 16 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Manka, J. T., Vinson, P. N., Gregory, K. J., Zhou, Y., Williams, R. E. A., Gogi, K., Days, E., Jadhav, S., Herman, E. J., Lavreysen, H., Mackie, C., Bartolome, J., Macdonald, G. J., Steckler, T., Daniels, J. S., Weaver, C. D., Niswender, C. M., Jones, C. K., Conn, P. J., Lindsley, C. W. & 1 othersStauffer, S. R., 2012, In : Bioorganic and Medicinal Chemistry Letters. 22, 20, p. 6481 - 6485 5 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Gregory, K. J., Sexton, P. M., Tobin, A. B. & Christopoulos, A., 2012, In : Journal of Biological Chemistry. 287, 44, p. 37066 - 37077 12 p.

Research output: Contribution to journalArticleResearchpeer-review

2011

Allosteric modulation of metabotropic glutamate receptors

Sheffler, D. J., Gregory, K. J., Rook, J. M. & Conn, P. J., 2011, In : Advances in Pharmacology. 62, p. 37 - 77 41 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric modulation of metabotropic glutamate receptors: Structural insights and therapeutic potential

Gregory, K. J., Dong, E. N., Meiler, J. & Conn, P. J., 2011, In : Neuropharmacology. 60, 1, p. 66 - 81 16 p.

Research output: Contribution to journalArticleResearchpeer-review

2010

Discovery of a novel chemical class of mGlu5 allosteric ligands with distinct modes of pharmacology

Hammond, A., Rodriguez, A., Townsend, S., Niswender, C., Gregory, K., Lindsley, C. & Conn, P., 2010, In : ACS Chemical Neuroscience. 1, 10, p. 702 - 716 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Identification of orthosteric and allosteric site mutations in M 2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias

Gregory, K. J., Hall, N., Tobin, A., Sexton, P. & Christopoulos, A., 2010, In : Journal of Biological Chemistry. 285, 10, p. 7459 - 7474 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Overview of receptor allosterism

Gregory, K., Sexton, P. & Christopoulos, A., Dec 2010, In : Current Protocols in Pharmacology. Chapter 1, Supp 51, p. 1.21-1 - 1.21-34 1 p.

Research output: Contribution to journalArticleResearchpeer-review

2008
2007

Allosteric modulation of muscarinic acetylcholine receptors

Gregory, K. J., Sexton, P. & Christopoulos, A., 2007, In : Current Neuropharmacology. 5, 3, p. 157 - 167 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands

Avlani, V. A., Gregory, K. J., Morton, C. J., Parker, M. W., Sexton, P. & Christopoulos, A., 2007, In : Journal of Biological Chemistry. 282, 35, p. 25677 - 25686 10 p.

Research output: Contribution to journalArticleResearchpeer-review

2005

Characterization of serotonin 5-HT2C receptor signaling to extracellular signal-regulated kinases 1 and 2

Werry, T. D., Gregory, K. J., Sexton, P. M. & Christopoulos, A., 2005, In : Journal of Neurochemistry. 93, p. 1603 - 1615 13 p.

Research output: Contribution to journalArticleResearchpeer-review