Thursday 6th June, 2013
4:45pm to 5:15pm
The ErbB family of receptors have been related to different types of cancers. A growing body of data from genetics, cellular biology, biochemistry, structural and computational biology has led to substantial progress in understanding the mechanisms of ErbB regulation.
We used structural and molecular modeling techniques to examine the molecular synergistic effect of several antibodies blocking ErbB2 function.
Recently we focused on exploiting EGFR structural biology to understanding acquired resistance. Drugs that competitively replace a natural substrate become ineffective by mutations that reduce the drug's affinity relative to that of the natural substrate. Understanding the underlying mechanisms is of utmost importance in efforts to design new drugs targeting mutant proteins.
We have modeled this emergence in EGFR and ErbB2 after treatment with lapatinib, by investigating the structural, dynamic and energetic effects on these kinases. The study reveals binding modes and subpopulations that are presumably normally cryptic.
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