New methods for the chemical synthesis of a library of glycopeptide-based tri-component cancer vaccines. A novel method for the synthesis of tumour-associated glycopeptides will be developed in this research as well as the preparation of a library of glycopeptide-based cancer vaccines. These vaccines will be tested in immunological studies with a view to elucidating new immune-based therapies for the treatment of cancer.
Total Synthesis of Myxobacteria Metabolites and Analogues. This project will investigate the total chemical synthesis of complex myxobacteria metabolites. In addition, the synthesis of new analogues of some of these natural products will also be investigated. The project endeavours to develop new methods for chemical synthesis and also to produce new therapeutic products which may possess greater efficacy and superior biological activities than the natural compounds. Most significantly, this pro ....Total Synthesis of Myxobacteria Metabolites and Analogues. This project will investigate the total chemical synthesis of complex myxobacteria metabolites. In addition, the synthesis of new analogues of some of these natural products will also be investigated. The project endeavours to develop new methods for chemical synthesis and also to produce new therapeutic products which may possess greater efficacy and superior biological activities than the natural compounds. Most significantly, this project will deliver natural and new compounds for analysis of anti-cancer activity. The rewards of the development of new synthetic methods are enormous for the community and in the education of our scientists.Read moreRead less
Discovery Early Career Researcher Award - Grant ID: DE140101632
Funder
Australian Research Council
Funding Amount
$395,220.00
Summary
Development of Innovative Chemical Tools for Studying Glycosyltransferases . This project aims to develop chemical probes capable of selectively binding and inhibiting two classes of carbohydrate processing enzymes known as O-linked beta-N-acetylglucosamine transferase and sialyltransferases. These enzymes are overexpressed in various cancers and play critical roles in cancer progression. Probes will be developed to analyse the activities of these enzymes in cancer cells.
Discovery Early Career Researcher Award - Grant ID: DE130101673
Funder
Australian Research Council
Funding Amount
$375,000.00
Summary
Access to biomimetic carbohydrate receptors using dynamic combinatorial chemistry. This project aims to utilise novel synthetic technology for the development of cyclic peptide libraries as novel drug leads for the treatment of Dengue virus, HIV and cancer.
Breaking it down: Dissecting the mechanism and exploring new inhibition strategies for polysaccharide cleaving enzymes. Mannose, a common carbohydrate building block, is present in a wide variety of complex polysaccharides including energy storage polymers and glycans attached to proteins. The enzymes that degrade these mannose-rich polymers, termed mannosidases, are important in biofuel production and human health and disease. This project will study a range of mannosidases to chemically and st ....Breaking it down: Dissecting the mechanism and exploring new inhibition strategies for polysaccharide cleaving enzymes. Mannose, a common carbohydrate building block, is present in a wide variety of complex polysaccharides including energy storage polymers and glycans attached to proteins. The enzymes that degrade these mannose-rich polymers, termed mannosidases, are important in biofuel production and human health and disease. This project will study a range of mannosidases to chemically and structurally define their mechanisms and establish strategies to allow intervention in mannosidase-specific disease processes. This work will inform strategies to engineer new enzymes for future biotechnology and industrial applications including sustainable chemical manufacturing, and underpin the development of innovative drugs for treating fungal infections and cancer.Read moreRead less
Linking chemical synthesis with protein discovery to reveal key biological pathways. The project aims to pioneer a chemical biology technology to deliver a much better understanding of key molecules that regulate diseases such as cancer. For decades phorbol esters have been prominent molecules for controlling cell switches in complex diseases but our knowledge is incomplete because of the limited natural abundance of these molecules.
Chiral Catalysts by Rational Design. This project aims to integrate theory and experiment to design new catalysts for the synthesis of multi-stereocentre-containing molecules. Such molecules offer clear advantages in the area of drug design, owing to their potent and selective binding to biological targets, but a lack of available methods for their preparation currently limits their widespread use. This project will use theory to guide the discovery of new ways to make these molecules. It is exp ....Chiral Catalysts by Rational Design. This project aims to integrate theory and experiment to design new catalysts for the synthesis of multi-stereocentre-containing molecules. Such molecules offer clear advantages in the area of drug design, owing to their potent and selective binding to biological targets, but a lack of available methods for their preparation currently limits their widespread use. This project will use theory to guide the discovery of new ways to make these molecules. It is expected that detailed understanding of the factors that control stereocentre formation will be obtained from accurate theoretical modelling and will be applied to invent new catalysts that deliver improved performance and control over product structure.Read moreRead less
Discovery Early Career Researcher Award - Grant ID: DE120101653
Funder
Australian Research Council
Funding Amount
$375,000.00
Summary
Selective fluorination chemistry: a tool for creating bioactive, shape-controlled peptides. Fluorine atoms are desirable substituents in drug candidates because they can increase metabolic stability and hydrophobicity, and because they can be used to constrain molecules into optimal bioactive conformations. These concepts are being exploited to create shape-controlled peptides with applications in anti-cancer and anti-microbial therapy.
Electrophile induced domino reaction sequences with ion-pair chiral induction. In this project, new catalysts and procedures will be developed to improve our capacity to access and modify the structure and properties of complex molecules. These methods will be used to gain access to a number of bioactive natural products in order to better evaluate and develop their therapeutic potential.
Dissecting catalysis and inhibition of a unique endo-acting mannose-processing glycosidase. Defects in the attachment of carbohydrates to proteins are a hallmark of diseases such as cancer and viral infection. This project will dissect the molecular details of the bond-making and breaking steps that occur during the synthesis of glycoproteins assisting in the development of innovative new drugs.