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An update on dual Src/Abl inhibitors
- Source :
- Future Medicinal Chemistry. 4:799-822
- Publication Year :
- 2012
- Publisher :
- Future Science Ltd, 2012.
-
Abstract
- c-Src and Bcr-Abl are two cytoplasmatic tyrosine kinases (TKs) involved in the development of malignancies. In particular, Bcr-Abl is the etiologic agent of chronic myeloid leukemia, where Src is also involved; the latter is hyperactivated in several solid tumors. Because of the structural homology between Src and Abl, several compounds originally synthesized as Src inhibitors have also been shown to be Abl inhibitors, useful in overcoming the onset of some types of chronic myeloid leukemia resistances, which frequently appear in the advanced phases of pathology. In recent years, the development of such compounds has been promoted by both excellent preclinical and clinical results, and by the theory that dual or multi-targeted inhibitors might be more effective than selective inhibitors. This review is an update on the most important dual inhibitors already in clinical trials and includes information regarding compounds that have appeared in the literature in recent years.
- Subjects :
- Models, Molecular
Dasatinib
Fusion Proteins, bcr-abl
Antineoplastic Agents
Pharmacology
Biology
Myelogenous
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
hemic and lymphatic diseases
Nitriles
Drug Discovery
medicine
Animals
Humans
Benzodioxoles
Proto-Oncogene Proteins c-abl
Protein Kinase Inhibitors
Aniline Compounds
ABL
Myeloid leukemia
medicine.disease
Fusion protein
Thiazoles
Leukemia
Pyrimidines
src-Family Kinases
Quinazolines
Quinolines
Cancer research
Molecular Medicine
Tyrosine kinase
medicine.drug
Proto-oncogene tyrosine-protein kinase Src
Subjects
Details
- ISSN :
- 17568927 and 17568919
- Volume :
- 4
- Database :
- OpenAIRE
- Journal :
- Future Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....8883dd8fa7eb6f63231b4b7fe62c46cf
- Full Text :
- https://doi.org/10.4155/fmc.12.29