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KDM5 inhibition offers a novel therapeutic strategy for the treatment of KMT2D mutant lymphomas.
Heward J, Konali L, D'Avola A, Close K, Yeomans A, Philpott M, Dunford J, Rahim T, Al Seraihi AF, Wang J, Korfi K, Araf S, Iqbal S, Bewicke-Copley F, Kumar E, Barisic D, Calaminici M, Clear A, Gribben J, Johnson P, Neve R, Cutillas P, Okosun J, Oppermann U, Melnick A, Packham G, Fitzgibbon J. Heward J, et al. Among authors: philpott m. Blood. 2021 Aug 5;138(5):370-381. doi: 10.1182/blood.2020008743. Blood. 2021. PMID: 33786580 Free PMC article.
Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.
Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs AP, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB, Vasta JD, Thezenas ML, Bonham S, Kessler B, Bennett J, Fedorov O, Raynaud F, Donovan A, Blagg J, Bavetsias V, Oppermann U, Bountra C, Kawamura A, Brennan PE. Vazquez-Rodriguez S, et al. Among authors: philpott m. Angew Chem Int Ed Engl. 2019 Jan 8;58(2):515-519. doi: 10.1002/anie.201810179. Epub 2018 Dec 7. Angew Chem Int Ed Engl. 2019. PMID: 30431220 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
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.
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
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
Nanopore sequencing of single-cell transcriptomes with scCOLOR-seq.
Philpott M, Watson J, Thakurta A, Brown T Jr, Brown T Sr, Oppermann U, Cribbs AP. Philpott M, et al. Nat Biotechnol. 2021 Dec;39(12):1517-1520. doi: 10.1038/s41587-021-00965-w. Epub 2021 Jul 1. Nat Biotechnol. 2021. PMID: 34211161 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.
256 results