The Design And Synthesis Of Sialyltransferase Inhibitors As Anti-metastatic Agents
Funder
National Health and Medical Research Council
Funding Amount
$273,629.00
Summary
The prevalence of cancer and, in particular, cancer that spreads throughout the body has risen over the past twenty years in the human population and causes significant human mortality. A correlation between some of a cancerous cell's surface componentary and the ability of this cell to spread throughout the body has been established. This research project will provide a range of chemical entities (probes) that will intervene in this spreading process (metastasis). These probes will be the basis ....The prevalence of cancer and, in particular, cancer that spreads throughout the body has risen over the past twenty years in the human population and causes significant human mortality. A correlation between some of a cancerous cell's surface componentary and the ability of this cell to spread throughout the body has been established. This research project will provide a range of chemical entities (probes) that will intervene in this spreading process (metastasis). These probes will be the basis for a drug discovery programme that targets a particular aspect of the spreading process. Through molecular modelling, drug candidate synthesis and evaluation of these compounds in relevant test tube (in vitro) assays it is envisaged that a number of candidate compounds will then be evaluated in an animal model (in vivo assay). The technology to be used in this project is comparable to that which we used in the discovery of the recently approved influenza drug, Relenza?.Read moreRead less
An Investigation Of Vibrio Cholerae Sialidase As A Target For Drug Discovery
Funder
National Health and Medical Research Council
Funding Amount
$227,036.00
Summary
The prevalence of the disease Cholera still causes significant human mortality, in particular in underdevloped countries. The process that enables the cholera toxin to cause signficant damage is now partly understood. This research project will provide a range of chemical entities (probes) that have the potential of intervening in this process . These probes will be the basis for a drug discovery programme that targets toxin binding. Through molecular modelling based on protein structural inform ....The prevalence of the disease Cholera still causes significant human mortality, in particular in underdevloped countries. The process that enables the cholera toxin to cause signficant damage is now partly understood. This research project will provide a range of chemical entities (probes) that have the potential of intervening in this process . These probes will be the basis for a drug discovery programme that targets toxin binding. Through molecular modelling based on protein structural information, drug candidate synthesis and evaluation of these compounds in relevant test tube (in vitro) assays it is envisaged that a number of candidate compounds will be then further optimised for eventual pre-clinical investigation. The technology to be used in this project is comparable to that we have used in the discovery of the recently approved influenza drug, Relenza .Read moreRead less
Development Of Specific Inhibitors Of Parasitic Enzymes
Funder
National Health and Medical Research Council
Funding Amount
$199,413.00
Summary
Parasitic diseases such as malaria, schistosomiasis, filariasis, leishmaniasis, and american trypanosomiasis (Chaga?s disease) are a significant public health issue, especially in tropical and subtropical regions of the world. In children, they cause death or impaired growth and in adults debilitating chronic illness. These parasitic infections are increasingly being recognized as responsible for chronic illness in many industrialized countries as well. There are no vaccines currently available ....Parasitic diseases such as malaria, schistosomiasis, filariasis, leishmaniasis, and american trypanosomiasis (Chaga?s disease) are a significant public health issue, especially in tropical and subtropical regions of the world. In children, they cause death or impaired growth and in adults debilitating chronic illness. These parasitic infections are increasingly being recognized as responsible for chronic illness in many industrialized countries as well. There are no vaccines currently available for the treatment of any of the human parasitic infections. In addition, the drugs that are currently used are becoming less effective because of the spread of drug resistant strains. Schistosomiasis, is the second most prevalent parasitic disease, after malaria, and is a leading cause of severe morbidity and death in many parts of the world. The disease is caused by flatworms or blood flukes, the eggs of which indirectly cause damage to the liver and spleen of infected individuals. These parasites feed on human red blood cells and use hemoglobin as their major food source. Our collaborative team (Brindley, Abbenante, Fairlie) has identified two enzymes that these flatworms need to use to eat red blood cells. This project aims to develop compounds that will stop these enzymes from functioning. These compounds will be tested to see whether they can cause the parasites to die of starvation. If successful these new compounds can be used as drugs to treat the disease and the general strategy can be applied to other blood-feeding parasites.Read moreRead less