20052020

Research output per year

If you made any changes in Pure these will be visible here soon.

Research Output

Detailed In Vitro Pharmacological Characterization of Clinically Tested Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5

Arsova, A., Møller, T. C., Vedel, L., Hansen, J. L., Foster, S. R., Gregory, K. J. & Bräuner-Osborne, H., 1 Jul 2020, In : Molecular Pharmacology. 98, 1, p. 49-60 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Differential contribution of metabotropic glutamate receptor 5 common allosteric binding site residues to biased allosteric agonism

Sengmany, K., Hellyer, S. D., Christopoulos, A., Lapinsky, D. J., Leach, K. & Gregory, K. J., 5 May 2020, (Accepted/In press) In : Biochemical Pharmacology. 15 p., 114011.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Evaluation of Operational Models of Agonism and Allosterism at Receptors with Multiple Orthosteric Binding Sites

Gregory, K., Giraldo, J., Diao, J., Christopoulos, A. & Leach, K., 2020, In : Molecular Pharmacology. 97, 1, p. 35-45 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
2 Citations (Scopus)

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., Jun 2020, In : Basic & Clinical Pharmacology & Toxicology. 126, S6, p. 104-115 12 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Negative allosteric modulators of the human calcium-sensing receptor bind to overlapping and distinct sites within the 7-transmembrane domain

Josephs, T. M., Keller, A. N., Khajehali, E., DeBono, A., Langmead, C. J., Conigrave, A. D., Capuano, B., Kufareva, I., Gregory, K. J. & Leach, K., Apr 2020, In : British Journal of Pharmacology. 177, 8, p. 1917-1930 14 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)
2019

How an activation signal is transmitted through an excitatory receptor

Gregory, K. J., 7 Feb 2019, In : Nature. 566, 7742, p. 42-43 2 p.

Research output: Contribution to journalArticleOtherpeer-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

5 Citations (Scopus)

Metabotropic glutamate receptor 5 (mGlu5)-positive allosteric modulators differentially induce or potentiate desensitization of mGlu5 signaling in recombinant cells and neurons

Hellyer, S. D., Albold, S., Sengmany, K., Singh, J., Leach, K. & Gregory, K. J., 1 Jan 2019, In : Journal of Neurochemistry. 151, 3, p. 301-315 15 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

The concise guide to Pharmacology 2019/20: G protein-coupled receptors

Alexander, S. P. H., Christopoulos, A., Davenport, A. P., Kelly, E., Mathie, A., Peters, J. A., Veale, E. L., Armstrong, J. F., Faccenda, E., Harding, S. D., Pawson, A. J., Sharman, J. L., Southan, C., Davies, J. A. & CGTP Collaborators, 1 Dec 2019, In : British Journal of Pharmacology. 176, S1, p. S21-S141 120 p.

Research output: Contribution to journalArticleOtherpeer-review

Open Access
File
91 Citations (Scopus)
2018

Biased agonism and allosteric modulation of metabotropic glutamate receptor 5

Trinh, P. N. H., May, L. T., Leach, K. & Gregory, K. J., 15 Nov 2018, In : Clinical Science. 132, 21, p. 2323-2338 16 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
File
5 Citations (Scopus)

Drugs to tune up glutamatergic systems: Modulators of glutamate metabotropic receptors

Sengmany, K. & Gregory, K. J., 1 Jan 2018, Biochemical Approaches for Glutamatergic Neurotransmission. Parrot, S. & Denoroy, L. (eds.). 1 ed. New York NY USA: Humana Press, p. 227-261 35 p. (Neuromethods; vol. 130).

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

Dual Action Calcium-Sensing Receptor Modulator Unmasks Novel Mode-Switching Mechanism

Gregory, K., Kufareva, I., Keller, A. N., Khajehali, E., Mun, H., Goolam, M. A., Mason, R. S., Capuano, B., Conigrave, A., Christopoulos, A. & Leach, K., 12 Sep 2018, In : ACS Pharmacology & Translational Science. 1, 2, p. 96-109 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

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

5 Citations (Scopus)

“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

7 Citations (Scopus)
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

23 Citations (Scopus)

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

Leach, K. & Gregory, K. J., 1 Feb 2017, In : Pharmacological Research. 116, p. 105-118 14 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

25 Citations (Scopus)
7 Citations (Scopus)

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
File
155 Citations (Scopus)
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

15 Citations (Scopus)

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

31 Citations (Scopus)

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

33 Citations (Scopus)

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

22 Citations (Scopus)

Practical strategies and concepts in GPCR allosteric modulator discovery: recent advances with metabotropic glutamate receptors

Lindsley, C. W., Emmitte, K. A., Hopkins, C. R., Bridges, T. M., Gregory, K. J., Niswender, C. M. & Conn, P. J., 8 Jun 2016, In : Chemical Reviews. 116, 11, p. 6707-6741 35 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

92 Citations (Scopus)

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

29 Citations (Scopus)

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

25 Citations (Scopus)

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

24 Citations (Scopus)

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

39 Citations (Scopus)

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

Open Access
File
24 Citations (Scopus)
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
File
44 Citations (Scopus)

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 others, Mackie, 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

72 Citations (Scopus)

Molecular insights into metabotropic glutamate receptor allosteric modulations

Gregory, K. J. & Conn, P. J., 1 Jul 2015, In : Molecular Pharmacology. 88, 1, p. 188-202 15 p.

Research output: Contribution to journalShort SurveyResearchpeer-review

29 Citations (Scopus)
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 others, Xiang, 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

33 Citations (Scopus)

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

32 Citations (Scopus)

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

65 Citations (Scopus)

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

330 Citations (Scopus)
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

60 Citations (Scopus)

Correction to: 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., Oct 2013, In : Molecular Pharmacology. 84, 4, p. 654 1 p.

Research output: Contribution to journalComment / DebateOtherpeer-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

24 Citations (Scopus)

Glutamate Receptors, Metabotropic

Gregory, K. J. & Conn, P. J., 15 Feb 2013, Encyclopedia of Biological Chemistry: Second Edition. Academic Press, p. 395-398 4 p.

Research output: Chapter in Book/Report/Conference proceedingEncyclopaedia / Dictionary EntryOtherpeer-review

1 Citation (Scopus)

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 others, Daigle, 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

34 Citations (Scopus)

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

Gregory, K. J., Noetzel, M. J. & Niswender, C. M., 2013, Progress in Molecular Biology and Translational Science. Kenakin, T. (ed.). Oxford UK: Elsevier, p. 61 - 121 61 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

30 Citations (Scopus)

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

60 Citations (Scopus)

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

76 Citations (Scopus)
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

30 Citations (Scopus)

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

61 Citations (Scopus)

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 others, Stauffer, S. R., 2012, In : Bioorganic and Medicinal Chemistry Letters. 22, 20, p. 6481 - 6485 5 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

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 : The Journal of Biological Chemistry. 287, 44, p. 37066 - 37077 12 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)
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

44 Citations (Scopus)

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

88 Citations (Scopus)