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2017 ; 12
(5
): 378-400
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Chemical probes targeting epigenetic proteins: Applications beyond oncology
#MMPMID28080202
Ackloo S
; Brown PJ
; Müller S
Epigenetics
2017[May]; 12
(5
): 378-400
PMID28080202
show ga
Epigenetic chemical probes are potent, cell-active, small molecule inhibitors or
antagonists of specific domains in a protein; they have been indispensable for
studying bromodomains and protein methyltransferases. The Structural Genomics
Consortium (SGC), comprising scientists from academic and pharmaceutical
laboratories, has generated most of the current epigenetic chemical probes.
Moreover, the SGC has shared about 4 thousand aliquots of these probes, which
have been used primarily for phenotypic profiling or to validate targets in cell
lines or primary patient samples cultured in vitro. Epigenetic chemical probes
have been critical tools in oncology research and have uncovered mechanistic
insights into well-established targets, as well as identify new therapeutic
starting points. Indeed, the literature primarily links epigenetic proteins to
oncology, but applications in inflammation, viral, metabolic and
neurodegenerative diseases are now being reported. We summarize the literature of
these emerging applications and provide examples where existing probes might be
used.