Venoms To Drugs: Characterizing The Molecular Interactions Between Venom Peptides And Ion Channels With A View To Rational Drug Design
Funder
National Health and Medical Research Council
Funding Amount
$316,449.00
Summary
The conventional approach to drug development is reaching a state of crisis as it is producing fewer new drugs at increasing cost. A promising alternative is to harness the rich and diverse chemistry of venom peptides. This project aims to understand the mechanism by which venom peptides achieve their pharmacological activity. This knowledge is essential for venom-based drug design for treating diseases ranging from nervous systems disorders, stroke, chronic pain and psychiatric illnesses.
Developing Drugs To Prevent Prostate Cancer Spread.
Funder
National Health and Medical Research Council
Funding Amount
$99,248.00
Summary
Current therapies for prostate cancer lose their efficacy as the cancer advances. Moreover, despite the spread of cancer being the major cause of prostate cancer mortality, there is no therapy available which selectively targets this process, thus new agents are needed. By using computer modelling to predict molecules that bind to the cell surface protein CD151 and testing these in biological assays, we aim to discover molecules that reduce cell migration of prostate cancer and that can be devel ....Current therapies for prostate cancer lose their efficacy as the cancer advances. Moreover, despite the spread of cancer being the major cause of prostate cancer mortality, there is no therapy available which selectively targets this process, thus new agents are needed. By using computer modelling to predict molecules that bind to the cell surface protein CD151 and testing these in biological assays, we aim to discover molecules that reduce cell migration of prostate cancer and that can be developed into anti-migration drugs.Read moreRead less
Enhanced force fields for computational drug design and materials research. This project aims to improve the atomic interaction functions used to calculate the structural, dynamic and thermodynamic properties of molecules that alter net charge or structure in different environments. Predicting the stability of alternative protonation and tautomeric states for molecules bound to therapeutic targets is a major challenge in computational drug design. It is key to identifying the therapeutically act ....Enhanced force fields for computational drug design and materials research. This project aims to improve the atomic interaction functions used to calculate the structural, dynamic and thermodynamic properties of molecules that alter net charge or structure in different environments. Predicting the stability of alternative protonation and tautomeric states for molecules bound to therapeutic targets is a major challenge in computational drug design. It is key to identifying the therapeutically active chemical species as well as understanding drug transport and off-target effects. The work will expand the utility of modelling software used by over 13,000 researchers worldwide. In addition, the improved interaction functions will also help in the understanding of a wide range of other materials at an atomic level.Read moreRead less
Structural Biology Of Bacterial Lipid II-glycopeptide Antibiotic Interactions
Funder
National Health and Medical Research Council
Funding Amount
$605,190.00
Summary
Drug resistant bacteria are threatening our ability to successfully treat serious life-endangering infections, with many common antibiotics no longer effective. We will study in atomic detail how one class of antibiotics interacts with bacteria in order to design new members of this group that can overcome resistance.
Designer RNA-binding Proteins For Research And Therapeutic Purposes
Funder
National Health and Medical Research Council
Funding Amount
$557,480.00
Summary
It has become clear recently that ribonucleic acids play many roles in the switching on and off of genes in humans and other organisms. These molecules play roles in a number of diseases, including HIV-AIDS, hepatitis, and a large number of inherited disorders. We propose to build a library of protein molecules that can bind specifically to a wide range of RNA targets and modulate their function. These molecules have the capacity to act as therapeutics for a wide range of diseases.
Theoretical modelling and design of safe covalent anti-cancer drugs. Covalent drugs are a new class of drugs with outstanding potential in cancer therapy. Detailed computer modelling studies will be performed to determine how these drugs interact with an important target in cancer therapy, the epithelial growth factor receptor, and thereby aid the development of new cancer treatments.
Engineered extrasynaptic GABAA receptors: Towards novel analgesics. Engineered extrasynaptic GABAA receptors: Towards novel analgesics. This project intends to alleviate neuropathic pain by developing drugs and good tool molecules targeting GABA-A receptors. About 20% of Australian adults suffer from neuropathic pain. Delta-containing GABA-A receptors represent attractive and novel targets for developing non-opioid analgesics. However, no drugs or good tool molecules target these receptors. This ....Engineered extrasynaptic GABAA receptors: Towards novel analgesics. Engineered extrasynaptic GABAA receptors: Towards novel analgesics. This project intends to alleviate neuropathic pain by developing drugs and good tool molecules targeting GABA-A receptors. About 20% of Australian adults suffer from neuropathic pain. Delta-containing GABA-A receptors represent attractive and novel targets for developing non-opioid analgesics. However, no drugs or good tool molecules target these receptors. This project intends to develop the needed enabling technologies, including screening assays, tool molecules and radioligands; and perform brain slice electrophysiology to confirm activity in neuronal cells. This project is expected to benefit the research community and future rational drug-discovery endeavours for drugs that modulate delta-containing receptors.Read moreRead less
Discovery and development of novel insulin sensitising compounds for the treatment of Type 2 diabetes. Diabetes is one of the major health problems facing Australia today, and current treatments are proving inadequate to combat this disease. We previously discovered a new drug with potential for development for the treatment of diabetes. In this project, we will identify how this drug works to combat diabetes in cell and animal models, and use novel chemistry approaches to modify the drug to imp ....Discovery and development of novel insulin sensitising compounds for the treatment of Type 2 diabetes. Diabetes is one of the major health problems facing Australia today, and current treatments are proving inadequate to combat this disease. We previously discovered a new drug with potential for development for the treatment of diabetes. In this project, we will identify how this drug works to combat diabetes in cell and animal models, and use novel chemistry approaches to modify the drug to improve its properties and reduce potential side-effects. The outcomes of this project will be understanding of a new biological process that contributes to the development of diabetes, and the discovery and characterisation of new chemical compounds that could be developed as drugs to treat diabetes.Read moreRead less
Bioactive Peptides as Pharmacological Tools and Novel Drug Leads. Bioactive peptides are produced by all organisms and play numerous critical physiological roles, including in cellular communication, host defence and capture of prey. Peptides have huge potential as tools for studying roles of signalling pathways and as novel drugs due to their high affinity and selectivity for various therapeutically relevant targets. However their use has been limited by poor in vivo stability. This project is ....Bioactive Peptides as Pharmacological Tools and Novel Drug Leads. Bioactive peptides are produced by all organisms and play numerous critical physiological roles, including in cellular communication, host defence and capture of prey. Peptides have huge potential as tools for studying roles of signalling pathways and as novel drugs due to their high affinity and selectivity for various therapeutically relevant targets. However their use has been limited by poor in vivo stability. This project is focused on studying structural features of a range of peptides and their contributions to both activity and to resistance against degradation, with the aim to develop stabilised bioactive peptide sequences for in vivo applications, allowing the full potential of peptides as drugs to be realised.Read moreRead less
Ultrasound-assisted fabrication of biofunctional materials. The project aims to develop a fundamental understanding of the mechanism involved in the synthetic process in order to control the physical and functional properties of core-shell biomaterials. Biofunctional core-shell materials are of scientific interest due to their potential use in a variety of applications including food manufacturing. Among existing methodologies for the synthesis of core-shell biomaterials, ultrasonic technology o ....Ultrasound-assisted fabrication of biofunctional materials. The project aims to develop a fundamental understanding of the mechanism involved in the synthetic process in order to control the physical and functional properties of core-shell biomaterials. Biofunctional core-shell materials are of scientific interest due to their potential use in a variety of applications including food manufacturing. Among existing methodologies for the synthesis of core-shell biomaterials, ultrasonic technology offers versatility and a wider choice of core and shell materials possessing specific biofunctionality. The outcomes of this project may include the establishment of a versatile technology for the fabrication of tailor-made biofunctional materials suitable for specific applications.Read moreRead less