Biography
Biography: Dirksen Bussiere
Abstract
Several biological functions, particularly chromosome segregation, require the generation of motile force. The generation of this force relies heavily on a class of proteins known as motor proteins. Motor proteins such as Kinesin Spindle Protein (KSP), also known as Eg5, utilize the energy derived from ATP hydrolysis to generate motile force. High-throughput screening of Eg5 identified several hits which were non-competitive with ATP with micromolar IC50’s capable of inhibiting the motor protein. Using structure-based drug design, these hits were progressed to NVP-BQS481, a clinical candidate with an IC50 of 700 picomolar. The talk will present the design concepts and optimization techniques used to advance the series to the pre-clinical stage.
References:
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