Halogen-enriched fragment libraries as leads for drug rescue of mutant p53
The destabilizing p53 cancer mutation Y220C creates a druggable surface crevice. We
developed a strategy exploiting halogen bonding for lead discovery to stabilize the mutant
with small molecules. We designed halogen-enriched fragment libraries (HEFLibs) as
starting points to complement classical approaches. From screening of HEFLibs and
subsequent structure-guided design, we developed substituted 2-(aminomethyl)-4-ethynyl-6-
iodophenols as p53-Y220C stabilizers. Crystal structures of their complexes highlight two …
developed a strategy exploiting halogen bonding for lead discovery to stabilize the mutant
with small molecules. We designed halogen-enriched fragment libraries (HEFLibs) as
starting points to complement classical approaches. From screening of HEFLibs and
subsequent structure-guided design, we developed substituted 2-(aminomethyl)-4-ethynyl-6-
iodophenols as p53-Y220C stabilizers. Crystal structures of their complexes highlight two …
[引用][C] Halogen-Enriched Fragment Libraries as Leads for Drug Rescue of Mutant p53
W Rainer, L Xiangrui - 2012
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