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- W1551174692 abstract "Bromodomains are modulators of protein–protein interactions essential for epigenetic mechanisms of transcriptional control. The recent disclosure of potent, selective, small molecule inhibitors of the BET bromodomain subfamily and their profound in vivo activity in several disease models suggests that the druggable genome should be extended to include this epi–reader target class. This chapter reviews the progress in bromodomain inhibitor drug discovery. The role of reader proteins in epigenetic gene regulation and the concept of the histone code are introduced. The therapeutic potential of bromodomain modulation in oncology, inflammation, metabolic and infectious disease is summarized. Methods of lead identification including use of phenotypic–, cell mechanistic–, biochemical– and fragment–based screens are described, as are selectivity considerations for this emerging target class. Difficulties in exploring this target class are also highlighted. Bromodomain chemical tractability is discussed using published examples, where SAR and the X–ray crystal structures exemplify how potency and selectivity can be achieved." @default.
- W1551174692 created "2016-06-24" @default.
- W1551174692 creator A5059463978 @default.
- W1551174692 date "2012-01-01" @default.
- W1551174692 modified "2023-10-13" @default.
- W1551174692 title "Small Molecule Bromodomain Inhibitors" @default.
- W1551174692 cites W1493972516 @default.
- W1551174692 cites W1517862272 @default.
- W1551174692 cites W1561092615 @default.
- W1551174692 cites W1584376310 @default.
- W1551174692 cites W1625510017 @default.
- W1551174692 cites W1792088282 @default.
- W1551174692 cites W1964337986 @default.
- W1551174692 cites W1965314855 @default.
- W1551174692 cites W1967018334 @default.
- W1551174692 cites W1967764418 @default.
- W1551174692 cites W1968568016 @default.
- W1551174692 cites W1968604097 @default.
- W1551174692 cites W1970330767 @default.
- W1551174692 cites W1971364991 @default.
- W1551174692 cites W1971407164 @default.
- W1551174692 cites W1971708895 @default.
- W1551174692 cites W1972091733 @default.
- W1551174692 cites W1973046803 @default.
- W1551174692 cites W1974266360 @default.
- W1551174692 cites W1974384304 @default.
- W1551174692 cites W1975232450 @default.
- W1551174692 cites W1976033223 @default.
- W1551174692 cites W1976109331 @default.
- W1551174692 cites W1976122783 @default.
- W1551174692 cites W1978431886 @default.
- W1551174692 cites W1978661875 @default.
- W1551174692 cites W1979187818 @default.
- W1551174692 cites W1980131884 @default.
- W1551174692 cites W1982619775 @default.
- W1551174692 cites W1984879354 @default.
- W1551174692 cites W1986721429 @default.
- W1551174692 cites W1988335148 @default.
- W1551174692 cites W1989804575 @default.
- W1551174692 cites W1990174038 @default.
- W1551174692 cites W1991770236 @default.
- W1551174692 cites W1991820123 @default.
- W1551174692 cites W1992902970 @default.
- W1551174692 cites W1993137394 @default.
- W1551174692 cites W1995979404 @default.
- W1551174692 cites W1999144014 @default.
- W1551174692 cites W1999993792 @default.
- W1551174692 cites W2000106654 @default.
- W1551174692 cites W2001097406 @default.
- W1551174692 cites W2001486015 @default.
- W1551174692 cites W2002698073 @default.
- W1551174692 cites W2005405421 @default.
- W1551174692 cites W2006192061 @default.
- W1551174692 cites W2007139310 @default.
- W1551174692 cites W2007835479 @default.
- W1551174692 cites W2007916651 @default.
- W1551174692 cites W2008285831 @default.
- W1551174692 cites W2009949436 @default.
- W1551174692 cites W2010510740 @default.
- W1551174692 cites W2010614766 @default.
- W1551174692 cites W2012220765 @default.
- W1551174692 cites W2013339218 @default.
- W1551174692 cites W2014941193 @default.
- W1551174692 cites W2015681476 @default.
- W1551174692 cites W2017251757 @default.
- W1551174692 cites W2017297735 @default.
- W1551174692 cites W2017466857 @default.
- W1551174692 cites W2017789254 @default.
- W1551174692 cites W2018046436 @default.
- W1551174692 cites W2019127581 @default.
- W1551174692 cites W2021049963 @default.
- W1551174692 cites W2021346554 @default.
- W1551174692 cites W2022807116 @default.
- W1551174692 cites W2024926989 @default.
- W1551174692 cites W2027417589 @default.
- W1551174692 cites W2029121336 @default.
- W1551174692 cites W2029572722 @default.
- W1551174692 cites W2029599359 @default.
- W1551174692 cites W2030007406 @default.
- W1551174692 cites W2031930309 @default.
- W1551174692 cites W2032025865 @default.
- W1551174692 cites W2033078160 @default.
- W1551174692 cites W2034420630 @default.
- W1551174692 cites W2034562270 @default.
- W1551174692 cites W2035915355 @default.
- W1551174692 cites W2036158314 @default.
- W1551174692 cites W2037844360 @default.
- W1551174692 cites W2040256969 @default.
- W1551174692 cites W2040321376 @default.
- W1551174692 cites W2040599377 @default.
- W1551174692 cites W2041535798 @default.
- W1551174692 cites W2045772671 @default.
- W1551174692 cites W2046833816 @default.
- W1551174692 cites W2047132220 @default.
- W1551174692 cites W2051152566 @default.
- W1551174692 cites W2052214665 @default.
- W1551174692 cites W2052762012 @default.
- W1551174692 cites W2055611175 @default.