Chemistry - A European Journal · 2009 · 59 citations · 31 references
Drug TargetBioorganic ChemistryOrganic ChemistrySelectivity AgainstChemistryChemical BiologyPharmaceutical ChemistryMedicinal ChemistryResorcylic Acid LactonesBiochemistryFluorous SynthesisCysteine ResidueDrug DevelopmentPharmacologyNatural Product SynthesisNew AnaloguesNatural SciencesRational Drug DesignMedicineResorcylic Acid LactoneSynthetic ChemistryDrug Discovery
A library of resorcylic acid lactones (RAL) containing a cis-enone moiety targeting kinases bearing a cysteine residue within the ATP-binding pocket was prepared using a fluorous-mixture synthesis and evaluated against a panel of 19 kinases thus providing important structure-activity trends. Two new analogues were then profiled for their selectivity against a panel of 402 kinases providing the broadest evaluation of this pharmacophores' selectivity.
31
Gain-of-Function Mutations of c- <i>kit</i> in Human Gastrointestinal Stromal Tumors
Seiichi Hirota, Koji Isozaki, Y Moriyama et al. · Science · 1998 · 4.4K citations
A quantitative analysis of kinase inhibitor selectivity
Mazen W. Karaman, Sanna Herrgård, Daniel K. Treiber et al. · Nature Biotechnology · 2008 · 2.4K citations
Anti-inflammatory cyclopentenone prostaglandins are direct inhibitors of IκB kinase
Antonio Rossi, Pankaj Kapahi, Gioacchino Natoli et al. · Nature · 2000 · 1.3K citations
Internal tandem duplication of the flt3 gene found in acute myeloid leukemia.
Mitsushige Nakao, S Yokota, Toshiki Iwai et al. · PubMed · 1996 · 1.2K citations