Newswise — The 2004 GlaxoSmithKline (GSK) Drug Discovery and Development Research Grants have recently been awarded to three scientists working on novel approaches to combat HIV, the virus that causes AIDS. The recipients, who will share equally in a total of $250,000 in grant monies, are: Yaoxing Huang, Ph.D., from the Aaron Diamond AIDS Research Center; Olaf Kutsch, Ph.D., from the University of Alabama at Birmingham; and Hugh D. Robertson, Ph.D., from the Weill Medical College of Cornell University.

"These research grants are given in recognition of outstanding scientists who have focused their creativity and talent on developing new weapons in the fight against HIV," said Doug Manion, M.D., vice president for HIV Clinical Research for the Infectious Diseases Medicines Development Center (MDC) at GSK.

Design of a Protein to Block All Steps of HIV Entry Yaoxing Huang, Ph.D., was awarded a Drug Discovery and Development Research Grant for his work to design a single protein that will block all three steps of the viral entry process. "We have demonstrated in our laboratory that a 'bi-active' protein may be effective at blocking the first two entry steps, whereas a second protein appears to block the third," Dr. Huang said. "The goal is to combine the inhibitors into a single, tri-active protein capable of blocking all three steps of viral entry before the HIV cell reaches the host cells," he said. The GSK award will be used to further test these and other proteins.

A New Method for Screening Compounds with Potential to Inhibit HIV ReplicationOlaf Kutsch, Ph.D., received a 2004 Drug Discovery and Development Research Grant for his novel, cell-based high throughput drug screening system to identify potential inhibitors of HIV transcription. "HIV gene expression is dependent on a unique viral protein, called HIV-1 transactivator (HIV-1 Tat)," Dr. Kutsch said. "All previous attempts to identify HIV-1 transcription inhibitors, however, have failed to produce a clinically useful drug. "For the first time, our system allows us to screen for HIV-1 Tat inhibitors with the capacity to immediately block HIV-1 expression," Dr. Kutsch said. "This capacity is considered essential for a transcription inhibitor to be effective in the clinical setting."

A Novel Strategy to Interrupt the Life Cycle of HIVDr. Hugh Robertson, Ph.D. was awarded a Drug Discovery and Development Research Grant for his study of internal ribosome entry sites (IRESs), which are highly structured regions present in the RNA of some viruses. IRES regions are believed to direct the synthesis of viral proteins in host cells. Dr. Robertson and his colleagues have discovered a target site within the IRES regions of several viruses, allowing them to be inhibited by a host enzyme called RNase P. "Research by other scientists has suggested that the RNA of HIV has an IRES similar to those we have studied in other viruses, such as the one that causes hepatitis C. We have shown in our work that RNase P may inhibit gene expression within the proposed HIV IRES sequence," Dr. Robertson said.

Winners of the Drug Discovery and Development Research Grant are selected by an Expert Review Board comprised of independent researchers who are leaders in the field of HIV/AIDS. Members of the Board that judged and selected this year's winners, are: John A. Bartlett, M.D., professor of medicine, Duke University Medical Center; David D. Ho, M.D., professor, Rockefeller University and scientific director, Aaron Diamond AIDS Research Center; and Michael Saag, M.D., associated professor of medicine and director of the AIDS Outpatient Clinic, University of Alabama at Birmingham.

Since the Drug Discovery and Development Research Grant program was initiated in 2001, GSK has awarded $1.5 million to further the development of inventive treatments for HIV/AIDS. These include therapies designed to prevent HIV infection or prevent transmission of the virus from one human to another. Applicants interested in more information about the Drug Discovery and Development Research Grant program can visit dddresearchgrant.com or call 1-888-527-6935.

GlaxoSmithKline is one of the world's leading research-based pharmaceutical and healthcare companies and an industry leader in HIV research and therapies. The company is engaged in basic research programs designed to investigate new targets to treat HIV. In addition to the Drug Discovery and Development Research Grant program, the company provides grants to community-based organizations that serve individuals whose lives are affected by HIV/AIDS.

GSK's Bridges to Access program can help provide qualified individuals with access to GSK's antiretroviral medications, as well as help identify insurance or other support for medications. Patients may be eligible for this program if they are not eligible for prescription drug benefits through any other private or public insurer, payer, or program. In 2003, GlaxoSmithKline donated more than $205 million worth of prescription drugs to 400,000 patients. For more information, visit http://www.bridgestoaccess.gsk.com or call 1-866-PATIENT.

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