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The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
Barrett SD, Bridges AJ, Dudley DT, Saltiel AR, Fergus JH, Flamme CM, Delaney AM, Kaufman M, LePage S, Leopold WR, Przybranowski SA, Sebolt-Leopold J, Van Becelaere K, Doherty AM, Kennedy RM, Marston D, Howard WA Jr, Smith Y, Warmus JS, Tecle H. Barrett SD, et al. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4. doi: 10.1016/j.bmcl.2008.10.054. Epub 2008 Oct 15. Bioorg Med Chem Lett. 2008. PMID: 18952427
Response and resistance to MEK inhibition in leukaemias initiated by hyperactive Ras.
Lauchle JO, Kim D, Le DT, Akagi K, Crone M, Krisman K, Warner K, Bonifas JM, Li Q, Coakley KM, Diaz-Flores E, Gorman M, Przybranowski S, Tran M, Kogan SC, Roose JP, Copeland NG, Jenkins NA, Parada L, Wolff L, Sebolt-Leopold J, Shannon K. Lauchle JO, et al. Nature. 2009 Sep 17;461(7262):411-4. doi: 10.1038/nature08279. Epub 2009 Sep 2. Nature. 2009. PMID: 19727076 Free PMC article.
Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition.
Ohren JF, Chen H, Pavlovsky A, Whitehead C, Zhang E, Kuffa P, Yan C, McConnell P, Spessard C, Banotai C, Mueller WT, Delaney A, Omer C, Sebolt-Leopold J, Dudley DT, Leung IK, Flamme C, Warmus J, Kaufman M, Barrett S, Tecle H, Hasemann CA. Ohren JF, et al. Nat Struct Mol Biol. 2004 Dec;11(12):1192-7. doi: 10.1038/nsmb859. Epub 2004 Nov 14. Nat Struct Mol Biol. 2004. PMID: 15543157
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