Structural Studies Of The Jak And Abl Kinases: A Prerequisite For Drug Design
Funder
National Health and Medical Research Council
Funding Amount
$360,965.00
Summary
Protein tyrosine kinases (PTK) are a large, pivotal family of signalling molecules implicated in diseases such as cancer and immune related disorders. This fellowship aims to develop more potent kinase inhibitors of a number of PTKs using Cytopia’s drug discovery capability coupled with the X-ray crystallography expertise within Monash University. This innovative approach will permit a rational structure-based drug discovery platform to be established and will lead to the creation of a portfolio ....Protein tyrosine kinases (PTK) are a large, pivotal family of signalling molecules implicated in diseases such as cancer and immune related disorders. This fellowship aims to develop more potent kinase inhibitors of a number of PTKs using Cytopia’s drug discovery capability coupled with the X-ray crystallography expertise within Monash University. This innovative approach will permit a rational structure-based drug discovery platform to be established and will lead to the creation of a portfolio of phase I therapeutics, which will be of substantial benefit in the medical health area.Read moreRead less
Structure Determination Of Fms And Kit Kinases And Their Inhibtors For Directed Drug Design
Funder
National Health and Medical Research Council
Funding Amount
$373,250.00
Summary
Tyrosine kinases are a large and important family of enzymes that play a fundamental role in the control and communication between cells. When damaged or uncontrolled, these enzymes can contribute to the development of diseases such as cancer and immune related disorders. This proposal aims to develop therapeutics targeted at the tyrosine kinases using a combination of the Structure Biology expertise at Monash University and the drug discovery platform technologies of Cytopia Pty Ltd. Promising ....Tyrosine kinases are a large and important family of enzymes that play a fundamental role in the control and communication between cells. When damaged or uncontrolled, these enzymes can contribute to the development of diseases such as cancer and immune related disorders. This proposal aims to develop therapeutics targeted at the tyrosine kinases using a combination of the Structure Biology expertise at Monash University and the drug discovery platform technologies of Cytopia Pty Ltd. Promising drug candidates already identified by Cytopia will be analysed at their site of action using X-ray crystallography. This information will enable a rational process of modification and improvement of the candidate drugs. The development of a range of therapeutics for Phase I clinical trials will be of enormous benefit to Australia�s medical industry and pubic health.Read moreRead less
The body’s normal function depends upon maintaining energy balance matching demand and supply. The body senses its energy status by monitoring metabolite concentrations. I have discovered a metabolite that controls multiple enzymes critical for energy homeostasis and appetite in the body that may provide new approaches to tackle obesity related disease. I have found the metabolite-binding pocket in many proteins and it may represent a major new regulatory network.
Investigating The Substrate Specificity Of The Master Kinase LKB1 And The Pharmacological Targeting Of Its Substrate NUAK2 To Treat Cancers
Funder
National Health and Medical Research Council
Funding Amount
$384,768.00
Summary
Kinases are key regulators of cell signaling and emerging drug targets. LKB1 kinase specifically activates a set of substrates to modulate cellular processes, and its substrate NUAK2 is a novel target for cancer. I will elucidate the structural basis of how LKB1 recognizes its substrates and develop inhibitors targeting LKB1-NUAK2 interaction for cancer treatment. My project will provide key insights into kinase-dependent signaling and establish a new framework for therapeutics development.