Antitumor activity of the new tyrphostin briva against BRAFV600E-mutant colorectal carcinoma cells

Saleh, Khaled; Al Sakhen, Mai; Kanaan, Sana; Yasin, Salem; Höpfner, Michael; Tahtamouni, Lubna; Biersack, Bernhard

doi:10.1007/s10637-023-01402-2

Cited by 1 publication

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References 39 publications

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“…RAF265 in combination with the PI3K inhibitor ZSTK474 showed synergistic effects in thyroid carcinoma cells, including BRAF mutant cell lines [171]. A new tyrphostin derivative with VEGFR2 inhibitory activity was particularly antiproliferative against BRAF V600E CRC cell lines (HT-29 and COLO-201) and showed pro-apoptotic and anti-migratory activities [172].…”

Section: Clinical Trials Of Egfr Inhibitors In Braf Mutant Cancers An...mentioning

confidence: 99%

Role and Function of Receptor Tyrosine Kinases in BRAF Mutant Cancers

Biersack,

Tahtamouni,

Höpfner

2024

Receptors

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The development of potent BRAF inhibitors has revolutionized the treatment of BRAF mutant cancers, in particular, melanomas. However, BRAF mutant cancers of other entities, e.g., colorectal cancers, display distinctly reduced responses to BRAF inhibitors. In addition, the emergence of cancer resistance to BRAF inhibitor treatment poses a severe problem. The reactivation of MAPK/ERK signaling was identified as an important mode of BRAF inhibitor resistance. Receptor tyrosine kinases (RTKs), which are prominent anticancer drug targets in their own right, play a crucial role in the development of drug resistance to BRAF inhibitors and the reactivation of MAPK/ERK signal transduction, as well as the establishment of bypassing signaling pathways. MAPK reactivation can occur via increased expression of RTKs, altered RTK signaling, and post-translational processes, among others. This review summarizes the influence of pertinent RTKs on BRAF mutant cancers and BRAF inhibitor resistance and outlines possible and proven ways to circumvent BRAF-associated resistance mechanisms.

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Section: Clinical Trials Of Egfr Inhibitors In Braf Mutant Cancers An...mentioning

confidence: 99%