When are the BET factors the most sensitive to bromodomain inhibitors?

Transcription

Volumn 4, Issue 2, 2013, Pages

  Khochbin, Saadi ^a  

^a INSERM   (France)

Author keywords

Acetylation; Brd2; Brd3; Brd4; Brdt; Cancer; Chromatin; Histone; Infertility; pTEFb; Spermatogenesis

Indexed keywords

BROMODOMAIN AND EXTRA TERMINAL PROTEIN; BROMODOMAIN TESTIS SPECIFIC PROTEIN; CELL PROTEIN; JQ1 PROTEIN INHIBITOR; PROTEIN; PROTEIN INHIBITOR; UNCLASSIFIED DRUG; (+)-JQ1 COMPOUND; AZEPINE DERIVATIVE; BRD2 PROTEIN, MOUSE; BRD3 PROTEIN, MOUSE; BRD4 PROTEIN, MOUSE; BRDT PROTEIN, MOUSE; CELL SURFACE RECEPTOR; DNER PROTEIN, MOUSE; NERVE PROTEIN; NONHISTONE PROTEIN; NUCLEAR PROTEIN; PROTEIN SERINE THREONINE KINASE; TRANSCRIPTION FACTOR; TRIAZOLE DERIVATIVE;

ARTICLE; CCNA1 GENE; DOWN REGULATION; GENE; GENE EXPRESSION REGULATION; GENETIC ASSOCIATION; HISTONE ACETYLATION; INHIBITION KINETICS; MOLECULAR MODEL; NONHUMAN; PHASE TRANSITION; PHENOTYPIC VARIATION; PROMOTER REGION; PROTEIN DOMAIN; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN TARGETING; SENSITIVITY ANALYSIS; SPERMATOCYTE; SPERMATOGENESIS; TRANSCRIPTION INITIATION SITE; ANIMAL; ANTAGONISTS AND INHIBITORS; DRUG EFFECTS; GENETICS; MALE; METABOLISM; MOUSE;

ANIMALS; AZEPINES; CHROMOSOMAL PROTEINS, NON-HISTONE; GENE EXPRESSION REGULATION; MALE; MICE; NERVE TISSUE PROTEINS; NUCLEAR PROTEINS; PROTEIN-SERINE-THREONINE KINASES; RECEPTORS, CELL SURFACE; SPERMATOGENESIS; TRANSCRIPTION FACTORS; TRIAZOLES;

EID: 85052488824     PISSN: 21541264     EISSN: 21541272     Source Type: Journal    
DOI: 10.4161/trns.23191     Document Type: Article

References (18)

1. Dhalluin C, Carlson JE, Zeng L, He C, Aggarwal AK, Zhou MM. Structure and ligand of a histone acetyl-transferase bromodomain. Nature 1999; 399:491-6; PMID:10365964; http://dx.doi.org/10.1038/20974.
2. Filippakopoulos P, Picaud S, Mangos M, Keates T, Lambert JP, Barsyte-Lovejoy D, et al. Histone recognition and large-scale structural analysis of the human bromodomain family. Cell 2012; 149:214-31; PMID:22464331; http://dx.doi.org/10.1016/j. cell.2012.02.013.
3. Muller S, Filippakopoulos P, Knapp S. Bromodomains as therapeutic targets. Expert Rev Mol Med 2011; 13:e29; PMID:21933453; http://dx.doi.org/10.1017/S1462399411001992.
4. Florence B, Faller DV. You bet-cha: a novel family of transcriptional regulators. Front Biosci 2001; 6:D1008-18; PMID:11487468; http://dx.doi.org/10.2741/Florence.
5. Belkina AC, Denis GV. BET domain co-regulators in obesity, inflammation and cancer. Nat Rev Cancer 2012; 12:465-77; PMID:22722403; http://dx.doi.org/10.1038/nrc3256.
6. Matzuk MM, McKeown MR, Filippakopoulos P, Li Q, Ma L, Agno JE, et al. Small-molecule inhibition of BRDT for male contraception. Cell 2012; 150:673-84; PMID:22901802; http://dx.doi.org/10.1016/j.cell.2012.06.045.
7. Gaucher J, Boussouar F, Montellier E, Curtet S, Buchou T, Bertrand S, et al. Bromodomain-dependent stage-specific male genome programming by Brdt. EMBO J 2012; 31:3809-20; PMID:22922464; http://dx.doi.org/10.1038/emboj.2012.233.
8. Gaucher J, Reynoird N, Montellier E, Boussouar F, Rousseaux S, Khochbin S. From meiosis to postmeiotic events: the secrets of histone disappearance. FEBS J 2010; 277:599-604; PMID:20015078; http://dx.doi.org/10.1111/j.1742-4658.2009.07504.x.
9. Bryant JM, Berger SL. Low-hanging fruit: targeting Brdt in the testes. EMBO J 2012; 31:3788-9; PMID:22960636; http://dx.doi.org/10.1038/emboj.2012.259.
10. Pivot-Pajot C, Caron C, Govin J, Vion A, Rousseaux S, Khochbin S. Acetylation-dependent chromatin reorganization by BRDT, a testis-specific bromodomain-containing protein. Mol Cell Biol 2003; 23:5354-65; PMID:12861021; http://dx.doi.org/10.1128/MCB.23.15.5354-5365.2003.
11. Morinière J, Rousseaux S, Steuerwald U, Soler-López M, Curtet S, Vitte AL, et al. Cooperative binding of two acetylation marks on a histone tail by a single bromodomain. Nature 2009; 461:664-8; PMID:19794495; http://dx.doi.org/10.1038/nature08397.
12. Shang E, Nickerson HD, Wen D, Wang X, Wolgemuth DJ. The first bromodomain of Brdt, a testis-specific member of the BET sub-family of double-bromodomain-containing proteins, is essential for male germ cell differentiation. Development 2007; 134:3507-15; PMID:17728347; http://dx.doi.org/10.1242/dev.004481.
13. Berkovits BD, Wolgemuth DJ. The first bromodo-main of the testis-specific double bromodomain protein Brdt is required for chromocenter organization that is modulated by genetic background. Dev Biol 2011; 360:358-68; PMID:22020252; http://dx.doi.org/10.1016/j.ydbio.2011.10.005.
14. Shang E, Salazar G, Crowley TE, Wang X, Lopez RA, Wang X, et al. Identification of unique, differentiation stage-specific patterns of expression of the bromodomain-containing genes Brd2, Brd3, Brd4, and Brdt in the mouse testis. Gene Expr Patterns 2004; 4:513-9; PMID:15261828; http://dx.doi.org/10.1016/j.modgep.2004.03.002.
15. Rahman S, Sowa ME, Ottinger M, Smith JA, Shi Y, Harper JW, et al. The Brd4 extraterminal domain confers transcription activation independent of pTEFb by recruiting multiple proteins, including NSD3. Mol Cell Biol 2011; 31:2641-52; PMID:21555454; http://dx.doi.org/10.1128/MCB.01341-10.
16. Nicodeme E, Jeffrey KL, Schaefer U, Beinke S, Dewell S, Chung CW, et al. Suppression of inflammation by a synthetic histone mimic. Nature 2010; 468:1119-23; PMID:21068722; http://dx.doi.org/10.1038/nature09589.
17. Shang E, Wang X, Wen D, Greenberg DA, Wolgemuth DJ. Double bromodomain-containing gene Brd2 is essential for embryonic development in mouse. Dev Dyn 2009; 238:908-17; PMID:19301389; http://dx.doi.org/10.1002/dvdy.21911.
18. Houzelstein D, Bullock SL, Lynch DE, Grigorieva EF, Wilson VA, Beddington RS. Growth and early postimplantation defects in mice deficient for the bromodomain-containing protein Brd4. Mol Cell Biol 2002; 22:3794-802; PMID:11997514; http://dx.doi.org/10.1128/MCB.22.11.3794-3802.2002.