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Structural analysis of human KDM5B guides histone demethylase inhibitor development.
Johansson C, Velupillai S, Tumber A, Szykowska A, Hookway ES, Nowak RP, Strain-Damerell C, Gileadi C, Philpott M, Burgess-Brown N, Wu N, Kopec J, Nuzzi A, Steuber H, Egner U, Badock V, Munro S, LaThangue NB, Westaway S, Brown J, Athanasou N, Prinjha R, Brennan PE, Oppermann U. Johansson C, et al. Among authors: philpott m. Nat Chem Biol. 2016 Jul;12(7):539-45. doi: 10.1038/nchembio.2087. Epub 2016 May 23. Nat Chem Biol. 2016. PMID: 27214403
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. Filippakopoulos P, et al. Among authors: philpott m. Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24. Nature. 2010. PMID: 20871596 Free PMC article.
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. Picaud S, et al. Among authors: philpott m. Cancer Res. 2015 Dec 1;75(23):5106-5119. doi: 10.1158/0008-5472.CAN-15-0236. Epub 2015 Nov 9. Cancer Res. 2015. PMID: 26552700 Free PMC article.
Histone H3K27me3 demethylases regulate human Th17 cell development and effector functions by impacting on metabolism.
Cribbs AP, Terlecki-Zaniewicz S, Philpott M, Baardman J, Ahern D, Lindow M, Obad S, Oerum H, Sampey B, Mander PK, Penn H, Wordsworth P, Bowness P, de Winther M, Prinjha RK, Feldmann M, Oppermann U. Cribbs AP, et al. Among authors: philpott m. Proc Natl Acad Sci U S A. 2020 Mar 17;117(11):6056-6066. doi: 10.1073/pnas.1919893117. Epub 2020 Mar 2. Proc Natl Acad Sci U S A. 2020. PMID: 32123118 Free PMC article.
Inhibition of Histone H3K27 Demethylases Inactivates Brachyury (TBXT) and Promotes Chordoma Cell Death.
Cottone L, Cribbs AP, Khandelwal G, Wells G, Ligammari L, Philpott M, Tumber A, Lombard P, Hookway ES, Szommer T, Johansson C, Brennan PE, Pillay N, Jenner RG, Oppermann U, Flanagan AM. Cottone L, et al. Among authors: philpott m. Cancer Res. 2020 Oct 15;80(20):4540-4551. doi: 10.1158/0008-5472.CAN-20-1387. Epub 2020 Aug 27. Cancer Res. 2020. PMID: 32855205
A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.
Fagan V, Johansson C, Gileadi C, Monteiro O, Dunford JE, Nibhani R, Philpott M, Malzahn J, Wells G, Faram R, Cribbs AP, Halidi N, Li F, Chau I, Greschik H, Velupillai S, Allali-Hassani A, Bennett J, Christott T, Giroud C, Lewis AM, Huber KVM, Athanasou N, Bountra C, Jung M, Schüle R, Vedadi M, Arrowsmith C, Xiong Y, Jin J, Fedorov O, Farnie G, Brennan PE, Oppermann U. Fagan V, et al. Among authors: philpott m. J Med Chem. 2019 Oct 24;62(20):9008-9025. doi: 10.1021/acs.jmedchem.9b00562. Epub 2019 Oct 15. J Med Chem. 2019. PMID: 31550156
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. Ebrahimi A, et al. Among authors: philpott m. Nat Chem Biol. 2019 May;15(5):519-528. doi: 10.1038/s41589-019-0264-z. Epub 2019 Apr 8. Nat Chem Biol. 2019. PMID: 30962627 Free PMC article.
255 results