mickwish
12-14-2004, 10:16 PM
Thanks to tgxiii for orginally posting about this.
Some new HIV drugs (http://ur.rutgers.edu/medrel/viewArticle.html?ArticleID=2571) are almost ready for large scale trials. Belgian and American scientists have collaborated in discovering several new potential anti-AIDS drugs, including compounds that can block all known drug-resistant strains of the virus....A third compound (R278474), scheduled for Phase I trials, is even more active against common HIV strains and all the mutants tested, according to the researchers.I like the following quote by one of the chief scientists, as it shows what we are doing with the drug-related DC projects is very valid. :cool:
"A drug may be thought of as a key that fits a specific lock," said chemistry Professor Eddy Arnold, a Rutgers member of the team. "The appropriate drug or key should be able to disrupt the functioning of the AIDS virus without causing serious side effects for the patient. Drug-resistant variants may be seen as an array of locks that require different keys to prevent the spread of viral infection." Arnold, who is also a member of the Center for Advanced Biotechnology and Medicine (CABM) based at Rutgers and the University of Medicine and Dentistry of New Jersey, explained that an ideal drug needs to work like a "master key" that can fit into and block as many of the locks (HIV variants) as possible.
To reach the goal of a "master-key," chemists on the team first synthesized hundreds of molecules and used them to search for useful drug candidates. Computer calculations of the structures of the drug and the drug target (the key and the lock) helped predict the best molecules to synthesize. The resulting drug candidates were tested against drug-resistant HIV, leading the researchers to the DAPY family of compounds.
Arnold and his colleagues Kalyan Das and Art Clark at CABM and Rutgers' department of chemistry and chemical biology worked with Stephen Hughes and co-workers at the NIH National Cancer Institute in Frederick, Md., to produce images that showed exactly how the drugs bind to their HIV targets. This information was used to modify the drugs in ways to improve their ability to bind to HIV.
The design work was carried out at Janssen's Center for Molecular Design in Belgium. Using a supercomputer, researchers there compared millions of potential molecular designs in order to select candidates for chemical synthesis. Hundreds of these candidates were then synthesized at Janssen in the United States and then tested against drug-resistant strains at Tibotec/Virco. Two of the most promising drugs, Dapivirine and R165335, have been tested in Phase II clinical trials. When R165335 was given as a single drug, viral loads were reduced to a level comparable to that achieved with a five-drug combination.
Keep crunchin for cures and better treatments, everyone!! :D
Cheers
Mick
Some new HIV drugs (http://ur.rutgers.edu/medrel/viewArticle.html?ArticleID=2571) are almost ready for large scale trials. Belgian and American scientists have collaborated in discovering several new potential anti-AIDS drugs, including compounds that can block all known drug-resistant strains of the virus....A third compound (R278474), scheduled for Phase I trials, is even more active against common HIV strains and all the mutants tested, according to the researchers.I like the following quote by one of the chief scientists, as it shows what we are doing with the drug-related DC projects is very valid. :cool:
"A drug may be thought of as a key that fits a specific lock," said chemistry Professor Eddy Arnold, a Rutgers member of the team. "The appropriate drug or key should be able to disrupt the functioning of the AIDS virus without causing serious side effects for the patient. Drug-resistant variants may be seen as an array of locks that require different keys to prevent the spread of viral infection." Arnold, who is also a member of the Center for Advanced Biotechnology and Medicine (CABM) based at Rutgers and the University of Medicine and Dentistry of New Jersey, explained that an ideal drug needs to work like a "master key" that can fit into and block as many of the locks (HIV variants) as possible.
To reach the goal of a "master-key," chemists on the team first synthesized hundreds of molecules and used them to search for useful drug candidates. Computer calculations of the structures of the drug and the drug target (the key and the lock) helped predict the best molecules to synthesize. The resulting drug candidates were tested against drug-resistant HIV, leading the researchers to the DAPY family of compounds.
Arnold and his colleagues Kalyan Das and Art Clark at CABM and Rutgers' department of chemistry and chemical biology worked with Stephen Hughes and co-workers at the NIH National Cancer Institute in Frederick, Md., to produce images that showed exactly how the drugs bind to their HIV targets. This information was used to modify the drugs in ways to improve their ability to bind to HIV.
The design work was carried out at Janssen's Center for Molecular Design in Belgium. Using a supercomputer, researchers there compared millions of potential molecular designs in order to select candidates for chemical synthesis. Hundreds of these candidates were then synthesized at Janssen in the United States and then tested against drug-resistant strains at Tibotec/Virco. Two of the most promising drugs, Dapivirine and R165335, have been tested in Phase II clinical trials. When R165335 was given as a single drug, viral loads were reduced to a level comparable to that achieved with a five-drug combination.
Keep crunchin for cures and better treatments, everyone!! :D
Cheers
Mick