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Items: 1 to 20 of 109

1.

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.

Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H, Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Che KH, Bannister A, Robson S, Kumar U, Parr N, Lee K, Lugo D, Jeffrey P, Taylor S, Vecellio ML, Bountra C, Brennan PE, O'Mahony A, Velichko S, Müller S, Hay D, Daniels DL, Urh M, La Thangue NB, Kouzarides T, Prinjha R, Schwaller J, Knapp S.

Cancer Res. 2015 Dec 1;75(23):5106-5119. doi: 10.1158/0008-5472.CAN-15-0236. Epub 2015 Nov 9.

2.

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.

Popp TA, Tallant C, Rogers C, Fedorov O, Brennan PE, Müller S, Knapp S, Bracher F.

J Med Chem. 2016 Oct 13;59(19):8889-8912. Epub 2016 Sep 27.

PMID:
27673482
3.

Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain Ligand I-CBP112.

Zucconi BE, Luef B, Xu W, Henry RA, Nodelman IM, Bowman GD, Andrews AJ, Cole PA.

Biochemistry. 2016 Jul 12;55(27):3727-34. doi: 10.1021/acs.biochem.6b00480. Epub 2016 Jul 1.

4.

Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.

Lasko LM, Jakob CG, Edalji RP, Qiu W, Montgomery D, Digiammarino EL, Hansen TM, Risi RM, Frey R, Manaves V, Shaw B, Algire M, Hessler P, Lam LT, Uziel T, Faivre E, Ferguson D, Buchanan FG, Martin RL, Torrent M, Chiang GG, Karukurichi K, Langston JW, Weinert BT, Choudhary C, de Vries P, Van Drie JH, McElligott D, Kesicki E, Marmorstein R, Sun C, Cole PA, Rosenberg SH, Michaelides MR, Lai A, Bromberg KD.

Nature. 2017 Oct 5;550(7674):128-132. doi: 10.1038/nature24028. Epub 2017 Sep 27. Erratum in: Nature. 2018 May 16;:.

5.

Salicylate, diflunisal and their metabolites inhibit CBP/p300 and exhibit anticancer activity.

Shirakawa K, Wang L, Man N, Maksimoska J, Sorum AW, Lim HW, Lee IS, Shimazu T, Newman JC, Schröder S, Ott M, Marmorstein R, Meier J, Nimer S, Verdin E.

Elife. 2016 May 31;5. pii: e11156. doi: 10.7554/eLife.11156.

6.

Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors.

Lu W, Xiong H, Chen Y, Wang C, Zhang H, Xu P, Han J, Xiao S, Ding H, Chen Z, Lu T, Wang J, Zhang Y, Yue L, Liu YC, Zhang C, Yang Y, Jiang H, Chen K, Zhou B, Luo C.

Bioorg Med Chem. 2018 Nov 1;26(20):5397-5407. doi: 10.1016/j.bmc.2018.07.048. Epub 2018 Jul 27.

PMID:
30297119
7.

A histone acetyltransferase p300 inhibitor C646 induces cell cycle arrest and apoptosis selectively in AML1-ETO-positive AML cells.

Gao XN, Lin J, Ning QY, Gao L, Yao YS, Zhou JH, Li YH, Wang LL, Yu L.

PLoS One. 2013;8(2):e55481. doi: 10.1371/journal.pone.0055481. Epub 2013 Feb 4.

8.

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.

Hammitzsch A, Tallant C, Fedorov O, O'Mahony A, Brennan PE, Hay DA, Martinez FO, Al-Mossawi MH, de Wit J, Vecellio M, Wells C, Wordsworth P, Müller S, Knapp S, Bowness P.

Proc Natl Acad Sci U S A. 2015 Aug 25;112(34):10768-73. doi: 10.1073/pnas.1501956112. Epub 2015 Aug 10.

9.

Bromodomain and histone acetyltransferase domain specificities control mixed lineage leukemia phenotype.

Santillan DA, Theisler CM, Ryan AS, Popovic R, Stuart T, Zhou MM, Alkan S, Zeleznik-Le NJ.

Cancer Res. 2006 Oct 15;66(20):10032-9.

10.

The natural anti-tumor compound Celastrol targets a Myb-C/EBPβ-p300 transcriptional module implicated in myeloid gene expression.

Coulibaly A, Haas A, Steinmann S, Jakobs A, Schmidt TJ, Klempnauer KH.

PLoS One. 2018 Feb 2;13(2):e0190934. doi: 10.1371/journal.pone.0190934. eCollection 2018.

11.

Bromodomain inhibition of the coactivators CBP/EP300 facilitate cellular reprogramming.

Ebrahimi A, Sevinç K, Gürhan Sevinç G, Cribbs AP, Philpott M, Uyulur F, Morova T, Dunford JE, Göklemez S, Arı Ş, Oppermann U, Önder TT.

Nat Chem Biol. 2019 May;15(5):519-528. doi: 10.1038/s41589-019-0264-z. Epub 2019 Apr 8.

PMID:
30962627
12.

Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents.

Yang H, Pinello CE, Luo J, Li D, Wang Y, Zhao LY, Jahn SC, Saldanha SA, Chase P, Planck J, Geary KR, Ma H, Law BK, Roush WR, Hodder P, Liao D.

Mol Cancer Ther. 2013 May;12(5):610-20. doi: 10.1158/1535-7163.MCT-12-0930. Epub 2013 Apr 26. Erratum in: Mol Cancer Ther. 2013 Aug;12(8):1688. Chase, Peter [added].

13.

Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor.

Bowers EM, Yan G, Mukherjee C, Orry A, Wang L, Holbert MA, Crump NT, Hazzalin CA, Liszczak G, Yuan H, Larocca C, Saldanha SA, Abagyan R, Sun Y, Meyers DJ, Marmorstein R, Mahadevan LC, Alani RM, Cole PA.

Chem Biol. 2010 May 28;17(5):471-82. doi: 10.1016/j.chembiol.2010.03.006.

14.

Small-molecule inhibition of CBP/catenin interactions eliminates drug-resistant clones in acute lymphoblastic leukemia.

Gang EJ, Hsieh YT, Pham J, Zhao Y, Nguyen C, Huantes S, Park E, Naing K, Klemm L, Swaminathan S, Conway EM, Pelus LM, Crispino J, Mullighan CG, McMillan M, Müschen M, Kahn M, Kim YM.

Oncogene. 2014 Apr 24;33(17):2169-78. doi: 10.1038/onc.2013.169. Epub 2013 Jun 3.

15.

CBP/p300 Bromodomains Regulate Amyloid-like Protein Aggregation upon Aberrant Lysine Acetylation.

Olzscha H, Fedorov O, Kessler BM, Knapp S, La Thangue NB.

Cell Chem Biol. 2017 Jan 19;24(1):9-23. doi: 10.1016/j.chembiol.2016.11.009. Epub 2016 Dec 15.

16.

An inhibitor of the acetyltransferases CBP/p300 exerts antineoplastic effects on gastrointestinal stromal tumor cells.

Gu ML, Wang YM, Zhou XX, Yao HP, Zheng S, Xiang Z, Ji F.

Oncol Rep. 2016 Nov;36(5):2763-2770. doi: 10.3892/or.2016.5080. Epub 2016 Sep 12.

PMID:
27633918
17.

A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach.

Milite C, Feoli A, Sasaki K, La Pietra V, Balzano AL, Marinelli L, Mai A, Novellino E, Castellano S, Tosco A, Sbardella G.

J Med Chem. 2015 Mar 26;58(6):2779-98. doi: 10.1021/jm5019687. Epub 2015 Mar 10.

PMID:
25730130
18.

Structural basis of site-specific histone recognition by the bromodomains of human coactivators PCAF and CBP/p300.

Zeng L, Zhang Q, Gerona-Navarro G, Moshkina N, Zhou MM.

Structure. 2008 Apr;16(4):643-52. doi: 10.1016/j.str.2008.01.010.

19.

Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.

Chaikuad A, Lang S, Brennan PE, Temperini C, Fedorov O, Hollander J, Nachane R, Abell C, Müller S, Siegal G, Knapp S.

J Med Chem. 2016 Feb 25;59(4):1648-53. doi: 10.1021/acs.jmedchem.5b01719. Epub 2016 Jan 13.

20.

Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains.

Hay DA, Fedorov O, Martin S, Singleton DC, Tallant C, Wells C, Picaud S, Philpott M, Monteiro OP, Rogers CM, Conway SJ, Rooney TP, Tumber A, Yapp C, Filippakopoulos P, Bunnage ME, Müller S, Knapp S, Schofield CJ, Brennan PE.

J Am Chem Soc. 2014 Jul 2;136(26):9308-19. doi: 10.1021/ja412434f. Epub 2014 Jun 19.

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