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Monday 1 February 2010

Scientists crack 20-year Aids puzzle that could revolutionise latest HIV medicines

Scientists say they have solved a crucial puzzle about the Aids virus after 20 years of research and that their findings could lead to better treatments for HIV. British and U.S. researchers said they have grown a crystal that enabled them to see the structure of an enzyme called integrase. The enzyme is found in retroviruses like HIV and is a target for some of the newest HIV medicines. It took more than 40,000 trials for them to come up with one a crystal of sufficiently high quality to allow them to see the three-dimensional structure.

'Despite initially painstakingly slow progress and very many failed attempts, we did not give up and our effort was finally rewarded,' said co-researcher Peter Cherepanov of Imperial College London.

Scientists from Imperial and Harvard university said that having the integrase structure means researchers can begin fully to understand how integrase inhibitor drugs work, how they might be improved, and how to stop HIV developing resistance to them.

When the human immunodeficiency virus (HIV) infects someone, it uses the integrase enzyme to paste a copy of its genetic information into their DNA. Some new drugs for HIV - like Isentress from Merck & Co - work by blocking integrase, but scientists are not clear exactly how they work or how to improve them.

The only way to find out was to obtain high-quality crystals - a project that had defeated scientists for many years.

'We went back to square one and started by looking for a better model of HIV integrase which could be more amenable for crystallization,' Cherepanov said.

The researchers grew a crystal using a version of integrase borrowed from another retrovirus very similar to its HIV counterpart. They tested the Merck and experimental Gilead drugs on the crystals, and were able to see for the first time how the medicines bind to, and block, integrase. (Daily Mail)