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Kinome targeting

Vieth M, Higgs RE, Robertson DH, etal. (2004) Kinomics-structural biology and chemogenomics of kinase inhibitors and targets. Biochim. Biophys. Acta. 1697 243-257. [Pg.31]

Figure 5. An example of intra-family target hopping within kinases. According to SiteSorter, Braf kinase, the primary target for the clinical compound BAY 43-9006, is one of the 10 most similar kinases to c-Kit, which has also been shown to bind BAY 43-9006 with sub-micromolar affinity (60% of the binding site residues are consen/ed and colored blue non-consen/ed positions are colored yellow). This cross-reactivity cannot be predicted based on the sequence similarity of the Braf and c-Kit kinase domains, since approximately one-sixth of the human kinome is more sequence similar to Braf than c-KiL... Figure 5. An example of intra-family target hopping within kinases. According to SiteSorter, Braf kinase, the primary target for the clinical compound BAY 43-9006, is one of the 10 most similar kinases to c-Kit, which has also been shown to bind BAY 43-9006 with sub-micromolar affinity (60% of the binding site residues are consen/ed and colored blue non-consen/ed positions are colored yellow). This cross-reactivity cannot be predicted based on the sequence similarity of the Braf and c-Kit kinase domains, since approximately one-sixth of the human kinome is more sequence similar to Braf than c-KiL...
Tyner JW, Walters DK, Willis SG et al (2008) RNAi screening of the tyrosine kinome identifies therapeutic targets in acute myeloid leukemia. Blood 111 2238-2245... [Pg.95]

Cole KA, Huggins J, Laquaglia M et al (2011) RNAi screen of the protein kinome identifies checkpoint kinase 1 (CHKl) as a therapeutic target in neuroblastoma. Proc Natl Acad Sci USA 108 3336-3341... [Pg.95]

Knight ZA, Lin H, Shokat KM (2010) Targeting the cancer kinome through polypharmacology. Nat Rev Cancer 10 130-137... [Pg.163]

Tiedemann RE, Zhu YX, Schmidt J et al (2010) Kinome-wide RNAi studies in human multiple myeloma identify vulnerable kinase targets, including a lymphoid-restricted kinase, GRK6. Blood 115 1594-1604... [Pg.322]

Doerig C, Abdi A, Bland N et al (2010) Malaria targeting parasite and host cell kinomes. Biochim Biophys Acta 1804(3) 604-612... [Pg.225]

Doerig C, Billker O, Pratt D, Endicott J (2005) Protein kinases as targets for antima-larial intervention kinomics, structure-based design, transmission-blockade, and targeting host cell enzymes. Biochim Biophys Acta 1754(1-2) 132-150... [Pg.225]

Chemical Kinomics A Target Gene Family Approach in Chemical Biology 1169... [Pg.169]

The second section focuses on target families such as kinases (R. Buijsman), ion channel modulators (K.-H. Baringhaus and G. Hessler), and phosphodiesterases (M. Hendrix and C. Kallus). In addition, the contribution of molecular informatics for chemogenomics (E. Jacoby et al.), chemical kinomics (B. Klebl), as well as proteochemometrics (J. Wikberg et al.) are discussed. [Pg.480]

See other pages where Kinome targeting is mentioned: [Pg.318]    [Pg.321]    [Pg.322]    [Pg.318]    [Pg.321]    [Pg.322]    [Pg.185]    [Pg.1257]    [Pg.51]    [Pg.31]    [Pg.168]    [Pg.209]    [Pg.589]    [Pg.16]    [Pg.211]    [Pg.211]    [Pg.211]    [Pg.223]    [Pg.167]    [Pg.168]    [Pg.170]    [Pg.172]    [Pg.1257]    [Pg.262]   
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See also in sourсe #XX -- [ Pg.185 , Pg.186 , Pg.187 , Pg.188 , Pg.189 , Pg.190 , Pg.191 , Pg.192 , Pg.193 , Pg.194 , Pg.195 , Pg.196 , Pg.197 , Pg.198 , Pg.199 , Pg.200 , Pg.201 ]

See also in sourсe #XX -- [ Pg.185 , Pg.186 , Pg.187 , Pg.188 , Pg.189 , Pg.190 , Pg.191 , Pg.192 , Pg.193 , Pg.194 , Pg.195 , Pg.196 , Pg.197 , Pg.198 , Pg.199 , Pg.200 , Pg.201 ]



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Alignment of Targetable Molecular Features Across the Human Kinome

Kinome

Kinome targeting ATP site recognition

Kinome targeting applications

Kinome targeting kinase family

Kinome targeting selectivity

Kinomics

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