Targeting allosteric regulatory modules in oncoproteins: "drugging the undruggable"

Oncotarget

Volumn 2, Issue 11, 2011, Pages 828-829

  Hantschel, Oliver ^a,b   Grebien, Florian ^a   Superti Furga, Giulio ^a  

^a ERICH SCHMID INSTITUTE OF MATERIALS SCIENCE   (Austria)

^b EPFL   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

BCR ABL PROTEIN; ONCOPROTEIN;

ALLOSTERISM; ANIMAL; EDITORIAL; HUMAN; METABOLISM; MOLECULARLY TARGETED THERAPY;

ALLOSTERIC REGULATION; ANIMALS; FUSION PROTEINS, BCR-ABL; HUMANS; MOLECULAR TARGETED THERAPY; ONCOGENE PROTEINS;

EID: 84858842458     PISSN: None     EISSN: 19492553     Source Type: Journal    
DOI: 10.18632/oncotarget.354     Document Type: Note

References (8)

1. O'Hare T, Eide CA, Deininger MW. Bcr-Abl kinase domain mutations, drug resistance, and the road to a cure for chronic myeloid leukemia. Blood 2007; 110(7):2242-2249.
2. Zhang X, Gureasko J, Shen K et al. An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell 2006; 125(6):1137-1149.
3. Heidorn SJ, Milagre C, Whittaker S et al. Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF. Cell 2010; 140(2):209-221.
4. Deininger M, Buchdunger E, Druker BJ. The development of imatinib as a therapeutic agent for chronic myeloid leukemia. Blood 2005; 105(7):2640-2653.
5. Hantschel O, Nagar B, Guettler S et al. A Myristoyl/Phosphotyrosine Switch Regulates c-Abl. Cell 2003; 112(6):845-857.
6. Zhang J, Adrián FJ, Jahnke W et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature 2010; 463(7280):501-506.
7. Filippakopoulos P, Kofler M, Hantschel O et al. Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation. Cell 2008; 134(5):793-803.
8. Grebien F, Hantschel O, Wojcik J et al. Targeting the SH2-Kinase Interface in Bcr-Abl Inhibits Leukemogenesis. Cell 2011; 147(2):306-319.