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Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer.
Eno MS, Brubaker JD, Campbell JE, De Savi C, Guzi TJ, Williams BD, Wilson D, Wilson K, Brooijmans N, Kim J, Özen A, Perola E, Hsieh J, Brown V, Fetalvero K, Garner A, Zhang Z, Stevison F, Woessner R, Singh J, Timsit Y, Kinkema C, Medendorp C, Lee C, Albayya F, Zalutskaya A, Schalm S, Dineen TA. Eno MS, et al. Among authors: wilson d, wilson k. J Med Chem. 2022 Jul 28;65(14):9662-9677. doi: 10.1021/acs.jmedchem.2c00704. Epub 2022 Jul 15. J Med Chem. 2022. PMID: 35838760 Free PMC article.
A precision therapy against cancers driven by KIT/PDGFRA mutations.
Evans EK, Gardino AK, Kim JL, Hodous BL, Shutes A, Davis A, Zhu XJ, Schmidt-Kittler O, Wilson D, Wilson K, DiPietro L, Zhang Y, Brooijmans N, LaBranche TP, Wozniak A, Gebreyohannes YK, Schöffski P, Heinrich MC, DeAngelo DJ, Miller S, Wolf B, Kohl N, Guzi T, Lydon N, Boral A, Lengauer C. Evans EK, et al. Among authors: wilson d, wilson k. Sci Transl Med. 2017 Nov 1;9(414):eaao1690. doi: 10.1126/scitranslmed.aao1690. Sci Transl Med. 2017. PMID: 29093181 Clinical Trial.
Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability.
Methot JL, Zhou H, Kattar SD, McGowan MA, Wilson K, Garcia Y, Deng Y, Altman M, Fradera X, Lesburg C, Fischmann T, Li C, Alves S, Shah S, Fernandez R, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Yu H, Bass A, Kemper R, Gatto NT, LaFranco-Scheuch L, Trotter BW, Guzi T, Katz JD. Methot JL, et al. Among authors: wilson k. J Med Chem. 2019 May 9;62(9):4370-4382. doi: 10.1021/acs.jmedchem.8b01818. Epub 2019 Apr 22. J Med Chem. 2019. PMID: 30986068
Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.
Northrup AB, Katcher MH, Altman MD, Chenard M, Daniels MH, Deshmukh SV, Falcone D, Guerin DJ, Hatch H, Li C, Lu W, Lutterbach B, Allison TJ, Patel SB, Reilly JF, Reutershan M, Rickert KW, Rosenstein C, Soisson SM, Szewczak AA, Walker D, Wilson K, Young JR, Pan BS, Dinsmore CJ. Northrup AB, et al. Among authors: wilson k. J Med Chem. 2013 Mar 28;56(6):2294-310. doi: 10.1021/jm301619u. Epub 2013 Mar 18. J Med Chem. 2013. PMID: 23379595
Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor.
Methot JL, Hoffman DM, Witter DJ, Stanton MG, Harrington P, Hamblett C, Siliphaivanh P, Wilson K, Hubbs J, Heidebrecht R, Kral AM, Ozerova N, Fleming JC, Wang H, Szewczak AA, Middleton RE, Hughes B, Cruz JC, Haines BB, Chenard M, Kenific CM, Harsch A, Secrist JP, Miller TA. Methot JL, et al. Among authors: wilson k. ACS Med Chem Lett. 2014 Jan 2;5(4):340-5. doi: 10.1021/ml4004233. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900838 Free PMC article.
Discovery of a new series of PI3K-δ inhibitors from Virtual Screening.
Fradera X, Deng Q, Achab A, Garcia Y, Kattar SD, McGowan MA, Methot JL, Wilson K, Zhou H, Shaffer L, Goldenblatt P, Tong V, Augustin MA, Altman MD, Lesburg CA, Shah S, Katz JD. Fradera X, et al. Among authors: wilson k. Bioorg Med Chem Lett. 2021 Jun 15;42:128046. doi: 10.1016/j.bmcl.2021.128046. Epub 2021 Apr 16. Bioorg Med Chem Lett. 2021. PMID: 33865969
A new pyridazine series of GABAA alpha5 ligands.
van Niel MB, Wilson K, Adkins CH, Atack JR, Castro JL, Clarke DE, Fletcher S, Gerhard U, Mackey MM, Malpas S, Maubach K, Newman R, O'Connor D, Pillai GV, Simpson PB, Thomas SR, MacLeod AM. van Niel MB, et al. Among authors: wilson k. J Med Chem. 2005 Sep 22;48(19):6004-11. doi: 10.1021/jm050249x. J Med Chem. 2005. PMID: 16162003
Structural basis for selective small molecule kinase inhibition of activated c-Met.
Rickert KW, Patel SB, Allison TJ, Byrne NJ, Darke PL, Ford RE, Guerin DJ, Hall DL, Kornienko M, Lu J, Munshi SK, Reid JC, Shipman JM, Stanton EF, Wilson KJ, Young JR, Soisson SM, Lumb KJ. Rickert KW, et al. Among authors: wilson kj. J Biol Chem. 2011 Apr 1;286(13):11218-25. doi: 10.1074/jbc.M110.204404. Epub 2011 Jan 18. J Biol Chem. 2011. PMID: 21247903 Free PMC article.
Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow.
Fradera X, Methot JL, Achab A, Christopher M, Altman MD, Zhou H, McGowan MA, Kattar SD, Wilson K, Garcia Y, Augustin MA, Lesburg CA, Shah S, Goldenblatt P, Katz JD. Fradera X, et al. Among authors: wilson k. Bioorg Med Chem Lett. 2019 Sep 15;29(18):2575-2580. doi: 10.1016/j.bmcl.2019.08.004. Epub 2019 Aug 5. Bioorg Med Chem Lett. 2019. PMID: 31416665
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
Witter DJ, Harrington P, Wilson KJ, Chenard M, Fleming JC, Haines B, Kral AM, Secrist JP, Miller TA. Witter DJ, et al. Bioorg Med Chem Lett. 2008 Jan 15;18(2):726-31. doi: 10.1016/j.bmcl.2007.11.047. Epub 2007 Nov 19. Bioorg Med Chem Lett. 2008. PMID: 18060775
5,724 results