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2015 ; 2
(ä): 27
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Evolution and intelligent design in drug development
#MMPMID26052517
Agafonov RV
; Wilson C
; Kern D
Front Mol Biosci
2015[]; 2
(ä): 27
PMID26052517
show ga
Sophisticated protein kinase networks, empowering complexity in higher organisms,
are also drivers of devastating diseases such as cancer. Accordingly, these
enzymes have become major drug targets of the twenty-first century. However, the
holy grail of designing specific kinase inhibitors aimed at specific cancers has
not been found. Can new approaches in cancer drug design help win the battle with
this multi-faced and quickly evolving enemy? In this perspective we discuss new
strategies and ideas that were born out of a recent breakthrough in understanding
the molecular basis underlying the clinical success of the cancer drug Gleevec.
An "old" method, stopped-flow kinetics, combined with old enzymes, the ancestors
dating back up to about billion years, provides an unexpected outlook for future
intelligent design of drugs.