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Personal profile

Biography

Position

Principal Investigator, Class C GPCR Lab head
Faculty of Pharmacy and Pharmaceutical Sciences

Drug Discovery Biology
Monash Institute of Pharmaceutical Sciences

Biography

I am co-lab head of the Class C G protein-coupled receptor (GPCR) laboratory, which is primarily interested in understanding the structure, function, physiology and therapeutic targeting of metabotropic glutamate receptors and the calcium sensing receptor. The Class C GPCR group is interested in the modulation of this protein family by endogenous and exogenous allosteric ligands that bind to sites distinct from that of the primary endogenous (orthosteric) agonist.

Supervision interests

Honours project supervision:

  1. Probing negative allosteric modulator binding sites in the human calcium sensing receptor. Current.
  2. Allosteric modulation of the calcium sensing receptor. H2 honours, 2015.
  3. Structure-function studies of the human calcium sensing receptor. H1 honours, 2010.
  4. Pharmacological characterisation of novel allosteric ligands acting at the M1 muscarinic acetylcholine receptor. H1 honours, 2009.
  5. Structure-function studies of the M4 muscarinic acetylcholine receptor. H1 honours, Dux of Year, 2008.
  6. Muscarinic M4 receptor interactions with GSK-3: possible targets for the treatment of schizophrenia. H2a honours, 2008.
  7. Pharmacological characterisation of a M4 muscarinic acetylcholine “Designer Receptor Exclusively Activated by Designer Drugs” (DREADD). H1 honours, Dux of Year, 2007.

Masters project supervision:

  1. Probing an allosteric binding site in the human calcium sensing receptor. Final year Pharmacy masters project, 2013-2014 – awarded M.Pharm with distinction
  2. Effects of two naturally occurring amino acid mutations on the pharmacoregulation of the human calcium sensing receptor. Second year Bioengineering masters project, 2010-2011 – awarded MSc. with distinction

PhD project supervision:

  1. Allosteric modulation and stimulus-bias at CB1 cannabinoid receptors.  PhD 2012-2015 – awarded PhD.
  2. Stimulus-bias at the calcium sensing receptor.  PhD 2009-2013 – awarded PhD.

Keywords

  • G protein-coupled receptors
  • calcium sensing receptor
  • allosterism
  • molecular pharmacology
  • structure-function
  • drug-receptor interactions
  • biased agonism
  • Class C GPCR

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Projects 2012 2020

Research Output 2007 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

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

Induced pluripotent stem cell-derived podocyte-like cells as models for assessing mechanisms underlying heritable disease phenotype: Initial studies using two alport syndrome patient lines indicate impaired potassium channel activity

Haynes, J. M., Selby, J. N., Vandekolk, T. H., Abad, I. P. L., Ho, J. K., Lieuw, W-L., Leach, K., Savige, J., Saini, S., Fisher, C. L. & Ricardo, S. D., 1 Nov 2018, In : Journal of Pharmacology and Experimental Therapeutics. 367, 2, p. 335-347 13 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

Activities 2011 2011

  • 1 Submissions to industry or govt committees, commissions and inquiries

Drug Discovery Biology

Katie Leach (Member)
29 Nov 2011

Activity: External Academic EngagementSubmissions to industry or govt committees, commissions and inquiries