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C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.
Le Bihan YV, Lanigan RM, Atrash B, McLaughlin MG, Velupillai S, Malcolm AG, England KS, Ruda GF, Mok NY, Tumber A, Tomlin K, Saville H, Shehu E, McAndrew C, Carmichael L, Bennett JM, Jeganathan F, Eve P, Donovan A, Hayes A, Wood F, Raynaud FI, Fedorov O, Brennan PE, Burke R, van Montfort RLM, Rossanese OW, Blagg J, Bavetsias V. Le Bihan YV, et al. Among authors: england ks. Eur J Med Chem. 2019 Sep 1;177:316-337. doi: 10.1016/j.ejmech.2019.05.041. Epub 2019 May 17. Eur J Med Chem. 2019. PMID: 31158747 Free PMC article.
Recent Progress in Histone Demethylase Inhibitors.
McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ. McAllister TE, et al. Among authors: england ks. J Med Chem. 2016 Feb 25;59(4):1308-29. doi: 10.1021/acs.jmedchem.5b01758. Epub 2016 Feb 2. J Med Chem. 2016. PMID: 26710088 Review.
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J. Bavetsias V, et al. Among authors: england ks. J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7. J Med Chem. 2016. PMID: 26741168 Free PMC article.
Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.
Tumber A, Nuzzi A, Hookway ES, Hatch SB, Velupillai S, Johansson C, Kawamura A, Savitsky P, Yapp C, Szykowska A, Wu N, Bountra C, Strain-Damerell C, Burgess-Brown NA, Ruda GF, Fedorov O, Munro S, England KS, Nowak RP, Schofield CJ, La Thangue NB, Pawlyn C, Davies F, Morgan G, Athanasou N, Müller S, Oppermann U, Brennan PE. Tumber A, et al. Among authors: england ks. Cell Chem Biol. 2017 Mar 16;24(3):371-380. doi: 10.1016/j.chembiol.2017.02.006. Epub 2017 Mar 2. Cell Chem Biol. 2017. PMID: 28262558 Free PMC article.
Targeting histone lysine demethylases - progress, challenges, and the future.
Thinnes CC, England KS, Kawamura A, Chowdhury R, Schofield CJ, Hopkinson RJ. Thinnes CC, et al. Among authors: england ks. Biochim Biophys Acta. 2014 Dec;1839(12):1416-32. doi: 10.1016/j.bbagrm.2014.05.009. Epub 2014 May 21. Biochim Biophys Acta. 2014. PMID: 24859458 Free PMC article. Review.
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
Jones P, Storer RI, Sabnis YA, Wakenhut FM, Whitlock GA, England KS, Mukaiyama T, Dehnhardt CM, Coe JW, Kortum SW, Chrencik JE, Brown DG, Jones RM, Murphy JR, Yeoh T, Morgan P, Kilty I. Jones P, et al. Among authors: england ks. J Med Chem. 2017 Jan 26;60(2):767-786. doi: 10.1021/acs.jmedchem.6b01634. Epub 2017 Jan 4. J Med Chem. 2017. PMID: 27983835
Acidic triazoles as soluble guanylate cyclase stimulators.
Roberts LR, Bradley PA, Bunnage ME, England KS, Fairman D, Fobian YM, Fox DN, Gymer GE, Heasley SE, Molette J, Smith GL, Schmidt MA, Tones MA, Dack KN. Roberts LR, et al. Among authors: england ks. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6515-8. doi: 10.1016/j.bmcl.2011.08.071. Epub 2011 Aug 28. Bioorg Med Chem Lett. 2011. PMID: 21924901
USP30 sets a trigger threshold for PINK1-PARKIN amplification of mitochondrial ubiquitylation.
Rusilowicz-Jones EV, Jardine J, Kallinos A, Pinto-Fernandez A, Guenther F, Giurrandino M, Barone FG, McCarron K, Burke CJ, Murad A, Martinez A, Marcassa E, Gersch M, Buckmelter AJ, Kayser-Bricker KJ, Lamoliatte F, Gajbhiye A, Davis S, Scott HC, Murphy E, England K, Mortiboys H, Komander D, Trost M, Kessler BM, Ioannidis S, Ahlijanian MK, Urbé S, Clague MJ. Rusilowicz-Jones EV, et al. Life Sci Alliance. 2020 Jul 7;3(8):e202000768. doi: 10.26508/lsa.202000768. Print 2020 Aug. Life Sci Alliance. 2020. PMID: 32636217 Free PMC article.