Title |
Novel small molecule Raf kinase inhibitors for targeted cancer therapeutics
|
---|---|
Published in |
Archives of Pharmacal Research, May 2012
|
DOI | 10.1007/s12272-012-0403-5 |
Pubmed ID | |
Authors |
Do-Hee Kim, Taebo Sim |
Abstract |
Aberrant activation of Raf signaling pathway is frequently found in various human tumors, it has been considered as distinct and promising molecular target for cancer therapeutics. B-Raf is most attractive drug target out of three Raf isoforms (A-Raf, B-Raf and C-Raf) because it exhibits high kinase activity due to frequent mutations in human tumors. However, most recently, it has been reported that Raf isoforms show the cross-activation in the presence of specific B-Raf inhibitors, which brings about the paradoxical p-ERK activation as well as tumor promoting effect. According to these findings, it remains controversy whether pan-Raf kinase inhibitor is more valuable and promising rather than specific B-Raf inhibitor under certain conditions in terms of cancer therapeutics. In this short review, novel Raf kinase inhibitors undergoing clinical investigation are introduced. Moreover, the paradoxical p-ERK activation is discussed with specific B-Raf inhibitors, PLX4032/4720 compounds. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Canada | 1 | 5% |
Unknown | 19 | 95% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 5 | 25% |
Student > Master | 5 | 25% |
Researcher | 4 | 20% |
Student > Bachelor | 3 | 15% |
Unknown | 3 | 15% |
Readers by discipline | Count | As % |
---|---|---|
Agricultural and Biological Sciences | 5 | 25% |
Pharmacology, Toxicology and Pharmaceutical Science | 4 | 20% |
Chemistry | 3 | 15% |
Biochemistry, Genetics and Molecular Biology | 2 | 10% |
Medicine and Dentistry | 2 | 10% |
Other | 1 | 5% |
Unknown | 3 | 15% |