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Page 1
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.
Johnson CN, Adelinet C, Berdini V, Beke L, Bonnet P, Brehmer D, Calo F, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, Mevellec L, McMenamin R, Pasquier E, Patel S, Rees DC, Linders JT. Johnson CN, et al. ACS Med Chem Lett. 2014 May 23;6(1):31-6. doi: 10.1021/ml5001273. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589926 Free PMC article.
Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
Johnson CN, Berdini V, Beke L, Bonnet P, Brehmer D, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, McMenamin R, Patel S, Rees DC, Sharff A, Sommen F, Wu T, Linders JT. Johnson CN, et al. ACS Med Chem Lett. 2014 May 23;6(1):25-30. doi: 10.1021/ml5001245. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589925 Free PMC article.
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
Chessari G, Buck IM, Day JE, Day PJ, Iqbal A, Johnson CN, Lewis EJ, Martins V, Miller D, Reader M, Rees DC, Rich SJ, Tamanini E, Vitorino M, Ward GA, Williams PA, Williams G, Wilsher NE, Woolford AJ. Chessari G, et al. Among authors: johnson cn. J Med Chem. 2015 Aug 27;58(16):6574-88. doi: 10.1021/acs.jmedchem.5b00706. Epub 2015 Aug 7. J Med Chem. 2015. PMID: 26218264
MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells.
Beke L, Kig C, Linders JT, Boens S, Boeckx A, van Heerde E, Parade M, De Bondt A, Van den Wyngaert I, Bashir T, Ogata S, Meerpoel L, Van Eynde A, Johnson CN, Beullens M, Brehmer D, Bollen M. Beke L, et al. Among authors: johnson cn. Biosci Rep. 2015 Oct 2;35(6):e00267. doi: 10.1042/BSR20150194. Biosci Rep. 2015. PMID: 26431963 Free PMC article.
Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).
Tamanini E, Buck IM, Chessari G, Chiarparin E, Day JEH, Frederickson M, Griffiths-Jones CM, Hearn K, Heightman TD, Iqbal A, Johnson CN, Lewis EJ, Martins V, Peakman T, Reader M, Rich SJ, Ward GA, Williams PA, Wilsher NE. Tamanini E, et al. Among authors: johnson cn. J Med Chem. 2017 Jun 8;60(11):4611-4625. doi: 10.1021/acs.jmedchem.6b01877. Epub 2017 May 24. J Med Chem. 2017. PMID: 28492317
Fragment-to-Lead Medicinal Chemistry Publications in 2016.
Johnson CN, Erlanson DA, Jahnke W, Mortenson PN, Rees DC. Johnson CN, et al. J Med Chem. 2018 Mar 8;61(5):1774-1784. doi: 10.1021/acs.jmedchem.7b01298. Epub 2017 Oct 31. J Med Chem. 2018. PMID: 29087197 Review.
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).
Johnson CN, Ahn JS, Buck IM, Chiarparin E, Day JEH, Hopkins A, Howard S, Lewis EJ, Martins V, Millemaggi A, Munck JM, Page LW, Peakman T, Reader M, Rich SJ, Saxty G, Smyth T, Thompson NT, Ward GA, Williams PA, Wilsher NE, Chessari G. Johnson CN, et al. J Med Chem. 2018 Aug 23;61(16):7314-7329. doi: 10.1021/acs.jmedchem.8b00900. Epub 2018 Aug 9. J Med Chem. 2018. PMID: 30091600
Correction: MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells.
Beke L, Kig C, Linders JTM, Boens S, Boeckx A, van Heerde E, Parade M, De Bondt A, Van den Wyngaert I, Bashir T, Ogata S, Meerpoel L, Van Eynde A, Johnson CN, Beullens M, Brehmer D, Bollen M. Beke L, et al. Among authors: johnson cn. Biosci Rep. 2018 Nov 30;38(6):BSR-20150194_COR. doi: 10.1042/BSR-20150194_COR. Print 2018 Dec 21. Biosci Rep. 2018. PMID: 30504271 Free PMC article. No abstract available.
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: johnson cn. 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
308 results