Molecular determinants of drug binding and selectivity at muscarinic acetylcholine receptors

Thal, David (Primary Chief Investigator (PCI))
Gooley, Paul Raymond (Chief Investigator (CI))
Dror, Ron (Chief Investigator (CI))

Drug Discovery Biology

Project: Research

Status	Finished
Effective start/end date	1/01/18 → 30/09/22

Funding

National Health and Medical Research Council (NHMRC) (Australia): A$816,866.00

9 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

3 Citations (Scopus)
Structural basis of efficacy-driven ligand selectivity at GPCRs
Powers, A. S., Pham, V., Burger, W. A. C., Thompson, G., Laloudakis, Y., Barnes, N., Sexton, P. M., Paul, S. M., Christopoulos, A., Thal, D. M., Felder, C. C., Valant, C. & Dror, R. O., 13 Feb 2023, In: Nature Chemical Biology. 19, p. 805–814 22 p.
Research output: Contribution to journal › Article › Research › peer-review

Open Access

7 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

1 Citation (Scopus)

Australian Synchrotron
Office of the Vice-Provost (Research and Research Infrastructure)
Facility/equipment: Facility
MASSIVE
Slava Kitaeff (Manager) & David Powell (Manager)
Office of the Vice-Provost (Research and Research Infrastructure)
Facility/equipment: Facility
Ramaciotti Centre for Cryo-Electron Microscopy
Georg Ramm (Manager), Simon Andrew Crawford (Operator), Hariprasad Venugopal (Operator), Joan Marea Clark (Operator) & Gediminas Gervinskas (Operator)
Faculty of Medicine Nursing and Health Sciences Research Platforms
Facility/equipment: Facility

Molecular determinants of drug binding and selectivity at muscarinic acetylcholine receptors

Project Details

Funding

Research output

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

Structural basis of efficacy-driven ligand selectivity at GPCRs

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

Equipment

Australian Synchrotron

MASSIVE

Ramaciotti Centre for Cryo-Electron Microscopy

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