The Janus face of G Protein-Coupled Receptors: Implications for Disease Mechanisms and Opportunities for Drug Discovery

Sexton, Patrick (Primary Chief Investigator (PCI))
Bunnett, Nigel (Chief Investigator (CI))
Christopoulos, Arthur (Chief Investigator (CI))
Summers, Roger (Chief Investigator (CI))

Drug Discovery Biology

Project: Research

Status	Finished
Effective start/end date	1/01/14 → 31/12/18

Funding

National Health and Medical Research Council (NHMRC) (Australia): A$3,797,920.00
National Health and Medical Research Council (NHMRC) (Australia): A$3,797,920.00

74 Article
6 Review Article

Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics
Vuckovic, Z., Wang, J., Pham, V., Mobbs, J. I., Belousoff, M. J., Bhattarai, A., Burger, W. A. C., Thompson, G., Yeasmin, M., Nawaratne, V., Leach, K., van der Westhuizen, E. T., Khajehali, E., Liang, Y. L., Glukhova, A., Wootten, D., Lindsley, C. W., Tobin, A., Sexton, P., Danev, R., & 4 othersValant, C., Miao, Y., Christopoulos, A. & Thal, D. M., 30 May 2023, In: eLife. 12, 52 p., e83477.
Research output: Contribution to journal › Article › Research › peer-review

Open Access

13 Citations (Scopus)
Structure–activity relationship of pyrazol-4-yl-pyridine derivatives and identification of a radiofluorinated probe for imaging the muscarinic acetylcholine receptor M₄
Haider, A., Deng, X., Mastromihalis, O., Pfister, S. K., Jeppesen, T. E., Xiao, Z., Pham, V., Sun, S., Rong, J., Zhao, C., Chen, J., Li, Y., Connors, T. R., Davenport, A. T., Daunais, J. B., Hosseini, V., Ran, W., Christopoulos, A., Wang, L., Valant, C., & 1 othersLiang, S. H., Jan 2023, In: Acta Pharmaceutica Sinica B. 13, 1, p. 213-226 14 p.
Research output: Contribution to journal › Article › Research › peer-review

Open Access

6 Citations (Scopus)
Xanomeline displays concomitant orthosteric and allosteric binding modes at the M₄ mAChR
Burger, W. A. C., Pham, V., Vuckovic, Z., Powers, A. S., Mobbs, J. I., Laloudakis, Y., Glukhova, A., Wootten, D., Tobin, A. B., Sexton, P. M., Paul, S. M., Felder, C. C., Danev, R., Dror, R. O., Christopoulos, A., Valant, C. & Thal, D. M., Dec 2023, In: Nature Communications. 14, 1, 11 p., 5440.
Research output: Contribution to journal › Article › Research › peer-review

Open Access

10 Citations (Scopus)

The Janus face of G Protein-Coupled Receptors: Implications for Disease Mechanisms and Opportunities for Drug Discovery

Project Details

Funding

Research output

Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics

Structure–activity relationship of pyrazol-4-yl-pyridine derivatives and identification of a radiofluorinated probe for imaging the muscarinic acetylcholine receptor M4

Xanomeline displays concomitant orthosteric and allosteric binding modes at the M4 mAChR

Structure–activity relationship of pyrazol-4-yl-pyridine derivatives and identification of a radiofluorinated probe for imaging the muscarinic acetylcholine receptor M₄

Xanomeline displays concomitant orthosteric and allosteric binding modes at the M₄ mAChR