Novel Soluble Guanylate Cyclase Activators For Pulmonary Artery Hypertension
Funder
National Health and Medical Research Council
Funding Amount
$474,087.00
Summary
Pulmonary hypertension (elevated blood pressure in the lungs) is a life-threatening condition with few treatment options. We have recently identified a new class of drug that may improve blood vessel function in the lungs and thereby provide a new drug for the management of this group of patients.
Development Of Fragment Hits Into Effective Antimalarials; Targeting Malaria Eradication
Funder
National Health and Medical Research Council
Funding Amount
$676,798.00
Summary
We have used a novel method that samples the diversity of natural products with a small sub-set of compounds, and observed direct interaction between these compounds and proteins important in the malaria parasite life cycle. This project will develop these identified active compounds towards the goal of producing a drug to fight stages of the malaria parasite’s life cycle that are not targeted by currently available antimalarial drugs.
OctapeptinX Potentiators To Treat XDR Gram-negative Infections
Funder
National Health and Medical Research Council
Funding Amount
$1,377,149.00
Summary
There is an urgent need for the development of new antibiotics to treat drug-resistant infections, with the World Health Organisation and other agencies warning of a critical threat to human health. Potentiators are drugs that help obsolete antibiotics regain activity against resistant bacteria. We aim to develop a novel class of potentiators, the octapeptins, to resurrect the activity of old antibiotics so they can be used to treat infections caused by highly-resistant Gram-negative bacteria.
Mechanism Of Action And Targeting Of Hexokinase II In Glioblastoma
Funder
National Health and Medical Research Council
Funding Amount
$643,607.00
Summary
Deaths from the brain cancer, glioblastoma, are as common as from the skin cancer in Australia. For most patients diagnosed with glioblastoma there is no realistic possibility of cure or even survival beyond a few years. We propose to understand and target glioblastomas aberrant metabolism of glucose, which may lead to better treatments for this devastating cancer.
Prostaglandin D2 (PGD2) is a key driver of asthma and allergic rhinitis. We have developed drug-like compounds that block the synthesis of PGD2 by inhibiting the hematopoietic prostaglandin D2 synthase (HPGD2S) enzyme. This project aims to develop these compounds further to ultimately treat a subset of the asthma population that are not well treated, refractory asthmatics.
Discovery Of New And Better Treatments For Human African Trypanosomiasis
Funder
National Health and Medical Research Council
Funding Amount
$837,615.00
Summary
Sleeping sickness, or human African trypanosomiasis, is present in 36 countries where there are 60 million people at risk of infection, with 50,000-70,000 new cases and 48,000 deaths per annum. Transmitted by the bite of the tsetse fly, this disease is caused by the protozoan parasite Trypanosoma brucei, and without treatment, death is inevitable. We have discovered some compounds that weakly inhibit T.brucei and the aim of this project is to make them potent enough to become drug candidates.
Small Molecule Therapeutics: From Infectious And Parasitic Diseases To Cancers
Funder
National Health and Medical Research Council
Funding Amount
$763,845.00
Summary
I will lead a team of medicinal chemists to discover better treatments of diseases focused in two major domains. On one hand, I will discover new drugs to treat certain parasitic diseases such as Sleeping Sickness, Chagas disease and malaria, all caused by protozoal parasites. On the other hand, I will discover new drugs to treat certain cancers, in particular acute myeloid leukemia and Burkitt’s lymphoma, caused by dysfunction of certain types of enzymes called histone acetyltransferases.
Glycine Transporters regulate the concentration of glycine in the spinal cord and brain. It has been suggested that elevating glycine levels in these regions may be useful in treating pain and schizophrenia. This project will provide the basis for the development of new glycine transport inhibitors that may be used to treat these conditions.
Development Of Small Molecules For The Treament Of Colon Cancer
Funder
National Health and Medical Research Council
Funding Amount
$684,379.00
Summary
Colon cancer remains one of the leading causes of cancer related deaths in Australia and in the developed world. Despite improvements in prevention and therapies, there remains a considerable need for efficacious therapeutic options. We have identified a lead compound inhibiting the growth of cancer cells. We will progress this series further toward clinical trials and aim to provide patients with a new orally available molecule with potent activity against colon cancer.