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Fluorescent Probes for Monitoring Ligand Binding and Receptor Trafficking and Internalisation

thesis
posted on 18.12.2018, 00:37 by JOSHUA WILLIAM CONNER
The Neurokinin 1 receptor (NK1R) is associated with neurogenic inflammation and nociceptive transmission through signal propagation by the endogenous agonist, substance P. Internalised NK1R in the endosome has a distinct signalling profile from that at the cell surface, resulting in unique pathophysiological outcomes. Therefore, endosomal populations of NK1R may be considered distinct therapeutic targets. The lack of clinical success of current NK1R antagonists, may be due to their inability to target endosomal NK1R. This thesis explores the utility of fluorescent probes for assessing ligand distribution and interaction with endosomal NK1R, and for developing tools to screen for endosomal NK1R ligands.

History

Campus location

Australia

Principal supervisor

Nicholas Veldhuis

Additional supervisor 1

Bim Graham

Additional supervisor 2

Peter Scammells

Year of Award

2018

Department, School or Centre

Medicinal Chemistry

Additional Institution or Organisation

Monash Institute of Pharmaceutical Sciences

Course

Doctor of Philosophy

Degree Type

DOCTORATE

Faculty

Faculty of Pharmacy and Pharmaceutical Sciences