CHED 1300 |
| The recently approved inhibitor of Human Immunodeficiency Virus 1 Integrase (HIV-1 IN) raltegravir belongs to a class of compounds called diketo acids (DKA). L-chicoric acid (L-CA) shares a common binding pocket with the DKAs but is significantly larger, and as such has substantially more contact residues within the active site. Gleevec (STI571 or imatinib mesylate) represents a major advance in the treatment of CML by inhibiting the bcr-abl fusion protein. the molecular cause of chronic myelogenous leukemia (CML). C-Kit, a receptor tyrosine kinase implicated in the pathogenesis of human cancers, is also inhibited by STI571. Unfortunately there have been reports of CML cases with established Gleevec resistance. Likewise IN mutations investigated to date show substantial cross-resistance to L-CA and certain DKAs. We have undertaken two parallel docking studies, L-CA with HIV IN and STI571 with c-Kit, in order to better understand the challenges posed in determining the path future drug resistance. The contrasting challenges of these two very different systems is examined.
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Undergraduate Research Poster Session: Medicinal Chemistry
2:00 PM-4:00 PM, Monday, April 7, 2008 Morial Convention Center -- Hall A, Poster
Division of Chemical Education |
