2008 Woodie Awards
Scientist finds drugs for rare HIV strain
Issue date: 4/3/08
Cap size refers to specific groups of atoms positioned on the inhibitor molecule that tailor the inhibitor to its target protein. A large and flexible cap means more possible rotation of bonds within the cap, which leads to an increased ability of the inhibitor to adapt to a mutating virus. The drugs with the largest cap are therefore the most effective in treating HIV-2.
A helpful way to understand an important aspect of drug design, Freire explained, is the "lock and key analogy," which says that if a virus is a lock, the inhibitor should be a key that fits perfectly in that lock. This view has recently been usurped, partially due to the lab's work.
"In the past, there was a dogma in drug design to make molecules that were very rigid, but a virus is able to change the lock, and if the key is rigid, it cannot adapt to the new lock. What we need is a master key that will open all locks," Freire said.
Freire listed three basic characteristics of a good inhibitor: "potency, selectivity and adaptability."
A potent inhibitor is powerful enough to keep the virus from creating more copies of itself. A selective inhibitor is singularly focused on its target, and an adaptable inhibitor can change with the virus as it mutates, while not losing the key components that allow it to function.
Freire's paper offers new insight on adaptability. "The research confirms that inhibitors that have elements that are able to adapt to changes are the ones that lose less potency when facing mutations," Freire said.
"The virus mutates when you take drugs, but the protease cannot mutate at will because it still has to work. Instead of something that is completely rigid all over, you have only specific rigid regions that target conserved parts of the protease."
Freire added that this set of three features that stemmed from this research on HIV forms "a drug development platform" that is being used to develop drugs to treat other viruses that have no cures, like Hepatitis C and Severe Acute Respiratory Syndrome (SARS).
Freire and his colleagues are proud that their findings will help patients with HIV-2 and are being applied to drug design in general. However, "there is always the frustration that despite all the research in labs all over the world, there is still no cure [for HIV]," Freire said.
A helpful way to understand an important aspect of drug design, Freire explained, is the "lock and key analogy," which says that if a virus is a lock, the inhibitor should be a key that fits perfectly in that lock. This view has recently been usurped, partially due to the lab's work.
"In the past, there was a dogma in drug design to make molecules that were very rigid, but a virus is able to change the lock, and if the key is rigid, it cannot adapt to the new lock. What we need is a master key that will open all locks," Freire said.
Freire listed three basic characteristics of a good inhibitor: "potency, selectivity and adaptability."
A potent inhibitor is powerful enough to keep the virus from creating more copies of itself. A selective inhibitor is singularly focused on its target, and an adaptable inhibitor can change with the virus as it mutates, while not losing the key components that allow it to function.
Freire's paper offers new insight on adaptability. "The research confirms that inhibitors that have elements that are able to adapt to changes are the ones that lose less potency when facing mutations," Freire said.
"The virus mutates when you take drugs, but the protease cannot mutate at will because it still has to work. Instead of something that is completely rigid all over, you have only specific rigid regions that target conserved parts of the protease."
Freire added that this set of three features that stemmed from this research on HIV forms "a drug development platform" that is being used to develop drugs to treat other viruses that have no cures, like Hepatitis C and Severe Acute Respiratory Syndrome (SARS).
Freire and his colleagues are proud that their findings will help patients with HIV-2 and are being applied to drug design in general. However, "there is always the frustration that despite all the research in labs all over the world, there is still no cure [for HIV]," Freire said.
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j hawkings
posted 9/10/08 @ 6:10 AM EST
This is a very good news that scientists at Hopkins are looking forward for the devlopment of drugs towards hiv2. I am very happy about it and wants to thank them. (Continued…)
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