Exploring metabotropic glutamate receptor 5 bias, allostery and heteromers

Research output

Research output per year 2019 2020 2021 2023

• 12 Article
• 2 Comment / Debate
• 2 Review Article

Research output per year

Research output per year

Search results

• 2023

  Calcium-Sensing Receptor Negative Allosteric Modulators Oppose Contraction of Mouse Airways

  Diao, J., Lam, M., Gregory, K. J., Leach, K. & Bourke, J. E., 1 Aug 2023, In: American Journal of Respiratory Cell and Molecular Biology. 69, 2, p. 182-196 15 p.

  Research output: Contribution to journal › Article › Research › peer-review
• 2022

  Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation

  Deganutti, G., Liang, Y. L., Zhang, X., Khoshouei, M., Clydesdale, L., Belousoff, M. J., Venugopal, H., Truong, T. T., Glukhova, A., Keller, A. N., Gregory, K. J., Leach, K., Christopoulos, A., Danev, R., Reynolds, C. A., Zhao, P., Sexton, P. M. & Wootten, D., 2022, In: Nature Communications. 13, 18 p., 92.

  Research output: Contribution to journal › Article › Research › peer-review

  Open Access
  19 Citations (Scopus)
• 2021

  Development of AC265347-Inspired Calcium-Sensing Receptor Ago-Positive Allosteric Modulators

  Dinh, L. V., DeBono, A., Keller, A. N., Josephs, T. M., Gregory, K. J., Leach, K. & Capuano, B., 19 Nov 2021, In: ChemMedChem. 16, 22, p. 3451-3462 12 p.

  Research output: Contribution to journal › Article › Research › peer-review

• Development of Covalent, Clickable Probes for Adenosine A₁and A₃Receptors

  Trinh, P. N. H., Chong, D. J. W., Leach, K., Hill, S. J., Tyndall, J. D. A., May, L. T., Vernall, A. J. & Gregory, K. J., 14 Jun 2021, In: Journal of Medicinal Chemistry. 64, 12, p. 8161–8178 18 p.

  Research output: Contribution to journal › Article › Research › peer-review
  6 Citations (Scopus)

• Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 as Tool Compounds to Study Signaling Bias

  Arsova, A., Møller, T. C., Hellyer, S. D., Vedel, L., Foster, S. R., Hansen, J. L., Bräuner-Osborne, H. & Gregory, K. J., 1 May 2021, In: Molecular Pharmacology. 99, 5, p. 328-341 14 p.

  Research output: Contribution to journal › Article › Research › peer-review
  4 Citations (Scopus)
• 2020

  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 journal › Article › Research › peer-review

  Open Access

  File
  11 Citations (Scopus)

• Development of Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 2 Based on Two Positive Allosteric Modulator Chemotypes

  Hellyer, S. D., Aggarwal, S., Chen, A. N. Y., Leach, K., Lapinsky, D. J. & Gregory, K. J., 3 Jun 2020, In: ACS Chemical Neuroscience. 11, 11, p. 1597-1609 13 p.

  Research output: Contribution to journal › Article › Research › peer-review
  5 Citations (Scopus)

• 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., Jul 2020, In: Biochemical Pharmacology. 177, 15 p., 114011.

  Research output: Contribution to journal › Article › Research › peer-review
  5 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 journal › Article › Research › peer-review
  2 Citations (Scopus)

• Probe dependence and biased potentiation of metabotropic glutamate receptor 5 is mediated by differential ligand interactions in the common allosteric binding site

  Hellyer, S. D., Sengmany, K., Keller, A. N., Christopoulos, A., Leach, K. & Gregory, K. J., Jul 2020, In: Biochemical Pharmacology. 177, 20 p., 114013.

  Research output: Contribution to journal › Article › Research › peer-review
  5 Citations (Scopus)
• 2019

  In Vitro to in Vivo Translation of Allosteric Modulator Concentration-Effect Relationships: Implications for Drug Discovery

  Gregory, K. J., Bridges, T. M., Gogliotti, R. G., Stauffer, S. R., Noetzel, M. J., Jones, C. K., Lindsley, C. W., Conn, P. J. & Niswender, C. M., 13 Dec 2019, In: ACS Pharmacology & Translational Science. 2, 6, p. 442-452 11 p.

  Research output: Contribution to journal › Article › Research › peer-review
  5 Citations (Scopus)

• 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 journal › Article › Research › peer-review
  16 Citations (Scopus)