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Page 1
Inhibition of monocarboxyate transporter 1 by AZD3965 as a novel therapeutic approach for diffuse large B-cell lymphoma and Burkitt lymphoma.
Noble RA, Bell N, Blair H, Sikka A, Thomas H, Phillips N, Nakjang S, Miwa S, Crossland R, Rand V, Televantou D, Long A, Keun HC, Bacon CM, Bomken S, Critchlow SE, Wedge SR. Noble RA, et al. Among authors: wedge sr. Haematologica. 2017 Jul;102(7):1247-1257. doi: 10.3324/haematol.2016.163030. Epub 2017 Apr 6. Haematologica. 2017. PMID: 28385782 Free PMC article.
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.
Myers SM, Miller DC, Molyneux L, Arasta M, Bawn RH, Blackburn TJ, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hammonds T, Hardcastle IR, Harnor SJ, Heptinstall AB, Lochhead PA, Martin MP, Martin NC, Newell DR, Owen PJ, Pang LC, Reuillon T, Rigoreau LJM, Thomas HD, Tucker JA, Wang LZ, Wong AC, Noble MEM, Wedge SR, Cano C. Myers SM, et al. Among authors: wedge sr. Eur J Med Chem. 2019 Sep 15;178:530-543. doi: 10.1016/j.ejmech.2019.05.057. Epub 2019 May 25. Eur J Med Chem. 2019. PMID: 31212132
Selective DNA-PKcs inhibition extends the therapeutic index of localized radiotherapy and chemotherapy.
Willoughby CE, Jiang Y, Thomas HD, Willmore E, Kyle S, Wittner A, Phillips N, Zhao Y, Tudhope SJ, Prendergast L, Junge G, Lourenco LM, Finlay MRV, Turner P, Munck JM, Griffin RJ, Rennison T, Pickles J, Cano C, Newell DR, Reeves HL, Ryan AJ, Wedge SR. Willoughby CE, et al. Among authors: wedge sr. J Clin Invest. 2020 Jan 2;130(1):258-271. doi: 10.1172/JCI127483. J Clin Invest. 2020. PMID: 31581151 Free PMC article.
Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein-Protein Interaction.
Chessari G, Hardcastle IR, Ahn JS, Anil B, Anscombe E, Bawn RH, Bevan LD, Blackburn TJ, Buck I, Cano C, Carbain B, Castro J, Cons B, Cully SJ, Endicott JA, Fazal L, Golding BT, Griffin RJ, Haggerty K, Harnor SJ, Hearn K, Hobson S, Holvey RS, Howard S, Jennings CE, Johnson CN, Lunec J, Miller DC, Newell DR, Noble MEM, Reeks J, Revill CH, Riedinger C, St Denis JD, Tamanini E, Thomas H, Thompson NT, Vinković M, Wedge SR, Williams PA, Wilsher NE, Zhang B, Zhao Y. Chessari G, et al. Among authors: wedge sr. J Med Chem. 2021 Apr 8;64(7):4071-4088. doi: 10.1021/acs.jmedchem.0c02188. Epub 2021 Mar 24. J Med Chem. 2021. PMID: 33761253
An Alkynylpyrimidine-Based Covalent Inhibitor That Targets a Unique Cysteine in NF-κB-Inducing Kinase.
Al-Khawaldeh I, Al Yasiri MJ, Aldred GG, Basmadjian C, Bordoni C, Harnor SJ, Heptinstall AB, Hobson SJ, Jennings CE, Khalifa S, Lebraud H, Martin MP, Miller DC, Shrives HJ, de Souza JV, Stewart HL, Temple M, Thomas HD, Totobenazara J, Tucker JA, Tudhope SJ, Wang LZ, Bronowska AK, Cano C, Endicott JA, Golding BT, Hardcastle IR, Hickson I, Wedge SR, Willmore E, Noble MEM, Waring MJ. Al-Khawaldeh I, et al. Among authors: wedge sr. J Med Chem. 2021 Jul 22;64(14):10001-10018. doi: 10.1021/acs.jmedchem.0c01249. Epub 2021 Jul 2. J Med Chem. 2021. PMID: 34212719
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
Miller DC, Reuillon T, Molyneux L, Blackburn T, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hardcastle I, Harnor SJ, Heptinstall A, Lochhead P, Martin MP, Martin NC, Myers S, Newell DR, Noble RA, Phillips N, Rigoreau L, Thomas H, Tucker JA, Wang LZ, Waring MJ, Wong AC, Wedge SR, Noble MEM, Cano C. Miller DC, et al. Among authors: wedge sr. J Med Chem. 2022 May 12;65(9):6513-6540. doi: 10.1021/acs.jmedchem.1c01756. Epub 2022 Apr 25. J Med Chem. 2022. PMID: 35468293 Free PMC article.
A Phase I Dose-escalation Study of AZD3965, an Oral Monocarboxylate Transporter 1 Inhibitor, in Patients with Advanced Cancer.
Halford S, Veal GJ, Wedge SR, Payne GS, Bacon CM, Sloan P, Dragoni I, Heinzmann K, Potter S, Salisbury BM, Chénard-Poirier M, Greystoke A, Howell EC, Innes WA, Morris K, Plummer C, Rata M, Petrides G, Keun HC, Banerji U, Plummer R. Halford S, et al. Among authors: wedge sr. Clin Cancer Res. 2023 Apr 14;29(8):1429-1439. doi: 10.1158/1078-0432.CCR-22-2263. Clin Cancer Res. 2023. PMID: 36652553 Free PMC article. Clinical Trial.
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