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Items: 1 to 20 of 144

1.

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.

Fish PV, Filippakopoulos P, Bish G, Brennan PE, Bunnage ME, Cook AS, Federov O, Gerstenberger BS, Jones H, Knapp S, Marsden B, Nocka K, Owen DR, Philpott M, Picaud S, Primiano MJ, Ralph MJ, Sciammetta N, Trzupek JD.

J Med Chem. 2012 Nov 26;55(22):9831-7. doi: 10.1021/jm3010515. Epub 2012 Nov 8.

2.

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.

Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers C, Parikh M, Taylor A, Samas B, O'Mahony A, Berg E, Pallares G, Torrey AD, Treiber DK, Samardjiev IJ, Nasipak BT, Padilla-Benavides T, Wu Q, Imbalzano AN, Nickerson JA, Bunnage ME, Müller S, Knapp S, Owen DR.

J Med Chem. 2016 May 26;59(10):4800-11. doi: 10.1021/acs.jmedchem.6b00012. Epub 2016 May 3.

3.

Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.

Bamborough P, Diallo H, Goodacre JD, Gordon L, Lewis A, Seal JT, Wilson DM, Woodrow MD, Chung CW.

J Med Chem. 2012 Jan 26;55(2):587-96. doi: 10.1021/jm201283q. Epub 2012 Jan 11.

PMID:
22136469
4.

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.

Hewings DS, Wang M, Philpott M, Fedorov O, Uttarkar S, Filippakopoulos P, Picaud S, Vuppusetty C, Marsden B, Knapp S, Conway SJ, Heightman TD.

J Med Chem. 2011 Oct 13;54(19):6761-70. doi: 10.1021/jm200640v. Epub 2011 Sep 6.

5.

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition.

Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung CW, Dittmann A, Drewes G, Drewry DH, Gordon L, Grandi P, Leveridge M, Lindon M, Michon AM, Molnar J, Robson SC, Tomkinson NC, Kouzarides T, Prinjha RK, Humphreys PG.

J Med Chem. 2016 Feb 25;59(4):1425-39. doi: 10.1021/acs.jmedchem.5b00256. Epub 2015 Apr 30.

6.

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.

Law RP, Atkinson SJ, Bamborough P, Chung CW, Demont EH, Gordon LJ, Lindon M, Prinjha RK, Watson AJB, Hirst DJ.

J Med Chem. 2018 May 24;61(10):4317-4334. doi: 10.1021/acs.jmedchem.7b01666. Epub 2018 May 3.

PMID:
29656650
7.

RVX-297- a novel BD2 selective inhibitor of BET bromodomains.

Kharenko OA, Gesner EM, Patel RG, Norek K, White A, Fontano E, Suto RK, Young PR, McLure KG, Hansen HC.

Biochem Biophys Res Commun. 2016 Aug 12;477(1):62-67. doi: 10.1016/j.bbrc.2016.06.021. Epub 2016 Jun 6.

PMID:
27282480
8.

Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.

Mirguet O, Gosmini R, Toum J, Clément CA, Barnathan M, Brusq JM, Mordaunt JE, Grimes RM, Crowe M, Pineau O, Ajakane M, Daugan A, Jeffrey P, Cutler L, Haynes AC, Smithers NN, Chung CW, Bamborough P, Uings IJ, Lewis A, Witherington J, Parr N, Prinjha RK, Nicodème E.

J Med Chem. 2013 Oct 10;56(19):7501-15. doi: 10.1021/jm401088k. Epub 2013 Sep 25.

PMID:
24015967
9.

Selective inhibition of BET bromodomains.

Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, West N, Cameron MJ, Schwartz B, Heightman TD, La Thangue N, French CA, Wiest O, Kung AL, Knapp S, Bradner JE.

Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24.

10.

Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery.

Chung CW, Dean AW, Woolven JM, Bamborough P.

J Med Chem. 2012 Jan 26;55(2):576-86. doi: 10.1021/jm201320w. Epub 2012 Jan 11.

PMID:
22136404
11.

Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes.

Baud MGJ, Lin-Shiao E, Cardote T, Tallant C, Pschibul A, Chan KH, Zengerle M, Garcia JR, Kwan TT, Ferguson FM, Ciulli A.

Science. 2014 Oct 31;346(6209):638-641. doi: 10.1126/science.1249830. Epub 2014 Oct 16.

12.

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.

Sutherell CL, Tallant C, Monteiro OP, Yapp C, Fuchs JE, Fedorov O, Siejka P, Müller S, Knapp S, Brenton JD, Brennan PE, Ley SV.

J Med Chem. 2016 May 26;59(10):5095-101. doi: 10.1021/acs.jmedchem.5b01997. Epub 2016 May 11.

13.

Naphthyridines as novel BET family bromodomain inhibitors.

Mirguet O, Lamotte Y, Chung CW, Bamborough P, Delannée D, Bouillot A, Gellibert F, Krysa G, Lewis A, Witherington J, Huet P, Dudit Y, Trottet L, Nicodeme E.

ChemMedChem. 2014 Mar;9(3):580-9. doi: 10.1002/cmdc.201300259. Epub 2013 Sep 2.

PMID:
24000170
14.

Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors.

Bennett MJ, Wu Y, Boloor A, Matuszkiewicz J, O'Connell SM, Shi L, Stansfield RK, Del Rosario JR, Veal JM, Hosfield DJ, Xu J, Kaldor SW, Stafford JA, Betancort JM.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1811-1816. doi: 10.1016/j.bmcl.2018.04.016. Epub 2018 Apr 10.

PMID:
29657099
15.

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.

Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, Bradner JE, Taniere P, O'Sullivan B, Müller S, Schwaller J, Stankovic T, Knapp S.

Cancer Res. 2013 Jun 1;73(11):3336-46. doi: 10.1158/0008-5472.CAN-12-3292. Epub 2013 Apr 10.

16.

Potent and selective bivalent inhibitors of BET bromodomains.

Waring MJ, Chen H, Rabow AA, Walker G, Bobby R, Boiko S, Bradbury RH, Callis R, Clark E, Dale I, Daniels DL, Dulak A, Flavell L, Holdgate G, Jowitt TA, Kikhney A, McAlister M, Méndez J, Ogg D, Patel J, Petteruti P, Robb GR, Robers MB, Saif S, Stratton N, Svergun DI, Wang W, Whittaker D, Wilson DM, Yao Y.

Nat Chem Biol. 2016 Dec;12(12):1097-1104. doi: 10.1038/nchembio.2210. Epub 2016 Oct 24.

PMID:
27775716
17.

NMR Fragment Screening Hit Induces Plasticity of BRD7/9 Bromodomains.

Wang N, Li F, Bao H, Li J, Wu J, Ruan K.

Chembiochem. 2016 Aug 3;17(15):1456-63. doi: 10.1002/cbic.201600184. Epub 2016 Jun 27.

PMID:
27194508
18.

The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.

Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E.

J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24.

PMID:
25249180
19.

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins.

Raux B, Voitovich Y, Derviaux C, Lugari A, Rebuffet E, Milhas S, Priet S, Roux T, Trinquet E, Guillemot JC, Knapp S, Brunel JM, Fedorov AY, Collette Y, Roche P, Betzi S, Combes S, Morelli X.

J Med Chem. 2016 Feb 25;59(4):1634-41. doi: 10.1021/acs.jmedchem.5b01708. Epub 2016 Jan 6.

PMID:
26735842
20.

Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.

Hewings DS, Fedorov O, Filippakopoulos P, Martin S, Picaud S, Tumber A, Wells C, Olcina MM, Freeman K, Gill A, Ritchie AJ, Sheppard DW, Russell AJ, Hammond EM, Knapp S, Brennan PE, Conway SJ.

J Med Chem. 2013 Apr 25;56(8):3217-27. doi: 10.1021/jm301588r. Epub 2013 Apr 5.

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