Graduate Students Choice Lecture
GRADUATE STUDENTS CHOICE LECTURE 2010
Title: Harnessing the power of organic synthesis to address the challenges of today's medicine
Presented by: Dr. Arun K. Ghosh
Time: 12:30 pm
Location: College of Pharmacy Room B36
Aspartic acid proteases are involved in the pathogenesis of many of human diseases and not surprisingly, aspartyl proteases have become important targets for drug-design and development. The introduction of HIV protease inhibitors in highly active antiretroviral therapy (HAART) continues to be the major treatment regimen for HIV/AIDS. However, one of the major challenges of HAART-therapy is the emergence of multidrug-resistant HIV-1 variants. In this context, our research efforts targeting the protein backbone led to structurally diverse new classes of potent HIV-1 protease inhibitors with impressive resistance profiles. Darunavir, designed based upon our ‘backbone binding concept’ has been recently approved for the treatment of experienced HIV/AIDS patients harboring multidrug-resistant HIV. Another aspartyl protease, memapsin 2 (β-secretase, BACE-1), has also become an important drug-design target for the treatment of Alzheimer’s disease. Our structure-based design has led to the development of a number of potent and selective inhibitors of memapsin 2 for clinical development. This presentation will feature novel design-concepts, general strategies and development tools for HIV-1 protease inhibitors against HIV/AIDS and β-secretase inhibitors against Alzheimer’s disease.
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