Session 22
Symposium
New Drug Targets: Integrase Inhibitors

• S1: HIV cDNA Integration: Mechanism and Design of Inhibitors (Authored by Frederic Bushman, The Salk Institute, La Jolla, CA)

• S2: Inhibitors of HIV Integrase: Antiviral Activity and Mechanism (Authored by Daria Hazuda, Merck Res. Labs, West Point, PA)
  Click here to view the original abstract

• S3: Reverse Transcriptase-Associated Ribonuclease H Activity as a Therapeutic Target (Authored by Stuart LeGrice, National Cancer Institute, Frederick, MD)
  Click here to view the original abstract

Current anti-HIV drugs fight HIV by stopping its ability to reproduce by interfering with two separate areas involved in creating new HIV. By now we have all become aware of the limitations of the currently approved anti-HIV drugs: long list of side effects, too many pills and the ability of HIV to change, making the drugs no longer effective. It was against this backdrop that I ventured into the afternoon slide presentation titled "New Drug Targets: Integrase Inhibitors."

Integrase is quite simply the chemical agent that helps HIV become part of the core of CD4 cells; integrase inhibitors try to prevent this from occurring. As I learned today, there are several different approaches researchers have tried to block this process, until now most have been unsuccessful. Today Daria Hazuda, a researcher with Merck Pharmaceutical, discussed two new proposed compounds that prevent HIV from being integrated into the core of CD4 cells. The new compounds were identified as L-731, 988 and L-708, 706 (eventually they will be given names, but for now this is how they will be identified). Both inhibit integrase by preventing a process referred to as "strand transfer." In early laboratory studies both new compounds have seen success. Keep your eyes and ears open for new information on both of these compounds in the months that follow, hopefully they we add new options to the HIV treatment arsenal.

Please note: Knowledge about HIV changes rapidly. Note the date of this summary's publication, and before treating patients or employing any therapies described in these materials, verify all information independently. If you are a patient, please consult a doctor or other medical professional before acting on any of the information presented in this summary. For a complete listing of our most recent conference coverage, click here.