Tag: ERK

JBJ-04-125-02 is a Mutant-Selective and Orally Active EGFR Inhibitor

Epidermal growth factor receptor (EGFR) is a transmembrane receptor protein in humans. The discovery of activating mutations in EGFR detected in 10% to 30% of patients with non–small cell lung cancer (NSCLC). In addition, it has revolutionized the treatment of this disease. Until recently, EGFR tyrosine kinase inhibitors (TKI), including...

JTE-013 is a Specific S1P2 Antagonist in Neuroblastoma

Sphingosine-1-phosphate ( S1P ), the bioactive sphingolipid metabolite, is a critical regulator of many physiological and pathophysiological processes, including cancer, atherosclerosis, diabetes and osteoporosis. S1P and its receptors (S1P1-5) play critical roles in many pathologic processes, including cancer. S1P/sphingosine-1-phosphate receptor (S1PR) axis plays critical role in a wide variety...

FR 180204 is an ATP-competitive and Selective ERK Inhibitor

An extracellular signal-regulated kinase (ERK) is a serine/threonine-protein kinase of the mitogen-activated protein kinase superfamily. Selective inhibition of ERK represents a potential approach for the treatment of cancer and other diseases. Simultaneous targeting of multiple effectors such as RAF, MEK, and ERK offers the potential for enhanced efficacy while...

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...

BAY 61-3606, a Syk Inhibitor, Sensitizes TRAIL-Induced Apoptosis by Downregulating Mcl-1 in Breast Cancer

Breast cancer cells usually develop resistance to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). TRAIL shows cancer-selective killing activity. TRAIL ligand selectively kills cancer cells by initiating apoptotic signaling through the engagement of its pro-apoptotic receptors, death receptors-4 and -5. In particular, myeloid cell leukemia sequence-1 (Mcl-1) is a member...