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/ Products Classification 点击展开+Cat. Number | 996828399288322 |
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Chemical Name | BRDT bromodomain 1 TR-FRET Assay Kit |
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References |
Background ReadingFilippakopoulos, P., Qi, J., Picaud, S., et al. Selective inhibition of BET bromodomains. Nature 468(7327) 1067-1073 (2010). Hewings, D.S., Wang, M., Philpott, M., et al. 3,5- Philpott, M., Yang, J., Tumber, T., et al. Bromodomain- Delmore, J.E., Issa, G.C., Lemieux, M.E., et al. BET bromodomain inhibition as a therapeutic strategy to target c- Zhang, J., Chung, T.D.Y., and Oldenburg, K.R. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 4(2) 67-73 (1999). Weidner-Glunde, M., Ottinger, M., and Schulz, T.F. WHAT do viruses BET on? Front Biosci 15 537-549 (2010). Day, A., Chitsaz, F., Abbasi, A., et al. The double bromodomain protein Brd4 binds to acetylated chromatin during interphase and mitosis. Proc Natl Acad Sci USA 100(15) 8758-8763 (2003). Umehara, T., Nakamura, Y., Jang, M.K., et al. Structural basis for acetylated histone H4 recognition by the human BRD2 bromodomain. J Biol Chem 2855(10) 7610-7618 (2010). Mujtaba, S., Zeng, L., and Zhou, M. Structure and acetyl- Florence, B., and Faller, D.V. You bet- LeRoy, G., Rickards, B., and Flint, S.J. The double bromodomain proteins Brd2 and Brd3 couple histone acetylation to transcription. Mol Cell 30(1) 51-60 (2008). Liu, Y., Wang, X., Zhang, J., et al. Structural basics and binding properties of the second bromodomain of Brd4 with acetylated histone tails. Biochem 47 6403-6417 (2008). Chung, C.W., Coste, H., White, J.H., et al. Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem 54(11) 3827-3838 (2011). Hargreaves, D.C., Horng, T., and Medzhitov, R. Control of inducible gene expression by signal- Umehara, T., Nakamura, Y., Wakamori, M., et al. Structural implications for K5/K12- Nicodeme, E., Jeffrey, K.L., Schaefer, U., et al. Suppression of inflammation by a synthetic histone mimic. Nature 468(7327) 1119-23 (2010). Mertz, J.A., Conery, A.R., Bryant, B.M., et al. Targeting MYC dependence in cancer by inhibiting BET bromodomains. Proc Natl Acad Sci USA 108(40) 16669-16674 (2011). Dawson, M.A., Prinjha, R.K., Dittmann, A., et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-
Description
Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of many BET family members, including BRD2, BRD3, BRD4, and BRDT, have been shown to bind acetylated histone tails, serving to couple histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease. Cayman’s BRDT Bromodomain 1 TR-
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