Mutant BRAF melanomas-dependence and resistance Journal Article
| Authors: | Poulikakos, P. I.; Rosen, N. |
| Article Title: | Mutant BRAF melanomas-dependence and resistance |
| Abstract: | RAF inhibitors have the unique property of transactivating RAS-dependent RAF dimers in most cells but inhibit RAF/MEK/ERK signaling in cells expressing mutant BRAF, in which RAS activity is too low to support this process. These drugs thus selectively inhibit ERK signaling in tumors with BRAF mutation. RAF inhibitors have remarkable clinical activity in melanomas with BRAFV600E mutations; however, resistance invariably develops. Three recent papers reveal that acquired resistance may be due to mechanisms that cause ERK signaling to become insensitive to RAF inhibitors, or that reduce the dependence of the tumor on ERK signaling through activation of other pathways. © 2011 Elsevier Inc. |
| Keywords: | signal transduction; mitogen activated protein kinase; raf protein; nonhuman; mutant protein; melanoma; enzyme inhibition; cancer resistance; short survey; ras protein; b raf kinase; protein inhibitor; b raf kinase inhibitor |
| Journal Title: | Cancer Cell |
| Volume: | 19 |
| Issue: | 1 |
| ISSN: | 1535-6108 |
| Publisher: | Cell Press |
| Date Published: | 2011-01-18 |
| Start Page: | 11 |
| End Page: | 15 |
| Language: | English |
| DOI: | 10.1016/j.ccr.2011.01.008 |
| PROVIDER: | scopus |
| PUBMED: | 21251612 |
| DOI/URL: | |
| Notes: | --- - "Export Date: 4 March 2011" - "CODEN: CCAEC" - "Source: Scopus" |
