In English

X-ray fragment screening of MEK1 to identify allosteric fragment binders

Carl Möller
Göteborg : Chalmers tekniska högskola, 2018. 69 s.
[Examensarbete på avancerad nivå]

The drug development process includes several phases and often span over many years. The initial phases are directed towards identifying and validating a potential target. Once a target has been validated, the hit identification and lead discovery process is initiated. This project have been performed on behalf of AstraZeneca and aimed to use x-ray crystallography to screen a compound library to identify fragments that binds to the allosteric pocket of MEK1. The results from this screen have mapped how a library of selected small molecules bound to the allosteric site. In total the campaign yielded 24 bound fragments with a good diversity that probes the entire pocket in a eÿcient way.



Publikationen registrerades 2018-09-24. Den ändrades senast 2018-09-24

CPL ID: 255985

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