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Gewählte Publikation:

Publikationstyp: Zeitschriftenaufsatz
Dokumenttyp: Übersichtsarbeit

Jahr: 2012

AutorInnen: Hantschel, O; Grebien, F; Superti-Furga, G

Titel: The growing arsenal of ATP-competitive and allosteric inhibitors of BCR-ABL.

Quelle: Cancer Res. 2012; 72(19):4890-4895

Autor/innen der Vetmeduni Vienna:

Grebien Florian

Diese Publikation wurde nicht im Namen der Vetmeduni Vienna erstellt und ist deshalb ausschließlich der persönlichen Publikationsliste des/der Autors/Autorin zugeordnet!

The BCR-ABL fusion kinase is the driving mutation of chronic myelogenous leukemias and is also expressed in a subset of acute lymphoblastic leukemias. Recent advances in elucidating the structure, regulation, and signaling of BCR-ABL have led to the identification of allosteric sites that are distant from the ATP-binding pocket and are critical for BCR-ABL-dependent oncogenic transformation. Here, we review the available data regarding the molecular mechanism of action and the specificity of ATP-competitive tyrosine kinase inhibitors targeting BCR-ABL. In addition, we discuss how targeting of allosteric sites could provide new opportunities to inhibit resistant BCR-ABL mutants, either alone or in combination with conventional ATP-competitive inhibitors.

Keywords Pubmed: Adenosine Triphosphate/metabolism*
Allosteric Site/drug effects
Allosteric Site/genetics
Binding, Competitive/drug effects
Fusion Proteins, bcr-abl/chemistry
Fusion Proteins, bcr-abl/genetics
Fusion Proteins, bcr-abl/metabolism*
Models, Molecular
Protein Binding/drug effects
Protein Kinase Inhibitors/metabolism*
Protein Kinase Inhibitors/pharmacology
Protein Structure, Tertiary

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