Tag: BRAF

Ravoxertinib is an Orally Active and Highly Selective ERK1/2 Inhibitor

The RAS/RAF/MEK/ERK (MAPK) signal transduction pathway has attracted significant interest as a therapeutic target for cancer. ERK1/2 phosphorylates more than 50 downstream substrates responsible for cell growth, proliferation, survival, angiogenesis, and differentiation. Small molecule inhibitors of BRAF and MEK have shown promising activities in a variety of solid tumors...

LY3214996 an Orally Active ERK1/2 Inhibitor with Potential Antineoplastic Activity

The Ras/Raf/MEK/ERK signaling cascade integrates extracellular clues from cell surface receptors to gene expression and regulation of multiple cellular proteins. Extracellular-signal-regulated kinases (ERKs) serve as key central nodes within this pathway. Simultaneous targeting of multiple effectors such as RAF, MEK, and ERK offers the potential for enhanced efficacy while...

SCH772984 is an ATP Competitive and Non-Competitive ERK1 and ERK2 Inhibitor

Specific inhibitors of RAF and MEK kinases to target BRAF– and RAS-mutant tumors are developing. Interestingly, BRAF/MEK inhibitor combination treatment blocks phosphorylated extracellular signal-regulated kinase (phospho-ERK) reactivation in melanoma cells, a phenomenon that may possibly reduce the emergence of clinical resistance.  ERK represents an attractive downstream target to exploit. SCH772984...

AZ304, a Dual BRAF Inhibitor Against Cancer

Cancer is the most serious disease in the world. Gene mutation always exhibits in many of human cancers, especially oncogenic BRAF mutations. Non-small cell lung cancer, ovarian cancer, leukaemia, gliomas and other malignancies have had BRAF mutations already. Although several BRAF inhibitors are launched to market, we need to...