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HIV research attracts Nature's interest

Angus Morgan

02 July, 2015

Tachedjian Laboratory researchers Dr Catherine Latham, Associate Professor Gilda Tachedjian and Adam Johnson

Burnet research into chemical building blocks that inhibit a proven HIV drug target in new ways has been reviewed and promoted in the prestigious journal, Nature Reviews Drug Discovery.

Originally published in The Proceedings of the National Academy of Sciences of the United States of America (PNAS), the research reveals the discovery of new drug building blocks that target a critical HIV molecule in ways distinct to drugs currently used for HIV treatment and prevention.

The discovery is critical for the development of more potent drugs able to combat virus that are resistant to currently available HIV inhibitors.

Head of Burnet’s Retroviral Biology and Antivirals Laboratory, Associate Professor Gilda Tachedjian, said the research team led by Jennifer La and Dr Catherine Latham is excited by Nature Reviews Drug Discovery’s interest.

“It’s really about recognition of the work and the quality of the work being highlighted in such a prestigious journal,” Associate Professor Tachedjian said.

PNAS is high impact in itself, but Nature is telling the drug discovery community that this paper is something worth looking at, which is pretty good. It’s recognition that the work is significant and increasing awareness of the work.

Associate Professor Tachedjian said there were several aspects of the research that may have attracted Nature’s interest.

“It’s a fragment-based drug discovery, but it’s unique in that we’ve used functional assays very early on in the fragment drug discovery process,” she said.

“This is different from other approaches to fragment based drug discovery, and it’s a new way to find novel drugs to an old target.”

The research focuses on the use of antiretroviral drugs in Pre-exposure prophylaxis (PrEP), which is gaining momentum as a tool to protect high-risk individuals from HIV infection.

PrEP urgently needs to be made accessible to prevent the 2.1 million new infections globally, however, the drugs that are being used are the same antiretroviral drugs that are used for HIV treatment.

“Our long-term concern is that, in a real-world setting, PrEP could lead to the generation and transmission of drug-resistant strains of HIV that could compromise first line drug regimens, particularly in individuals from resource-poor settings,” Associate Professor Tachedjian said.

“To address this concern, a relatively new paradigm in drug discovery (fragment based drug design) was used to identify very small chemicals called ‘fragments’ that are half the size of conventional drugs that are efficient at binding to new drug sites on the viral target.

“Despite their small size, these fragments were found to bind and block the functioning of the critical HIV molecule.

“Notably, three of these fragments inhibited the function of this molecule in ways that are distinct to licensed drugs that target this protein and would be expected to block virus resistant to these licensed drugs.

“Using these building blocks we can now start to grow these molecules into larger and more potent inhibitors to develop new drugs that are effective against drug-resistant HIV that can be used in the future for HIV treatment and prevention.”

Burnet collaborated with researchers from Monash Institute for Pharmaceutical Sciences and the University of Pittsburgh School of Medicine.

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Contact Details

For more information in relation to this news article, please contact:

Professor Gilda Tachedjian

Head of Life Sciences; Head of Tachedjian Laboratory (Retroviral Biology and Antivirals)

Telephone

+61392822256

Email

gilda.tachedjian@burnet.edu.au

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