Tag: FGFR

Nintedanib is an Orally Active Triple Angiokinase Inhibitor for VEGFR, FGFR and PDGFR

VEGFR are receptors for vascular endothelial growth factor (VEGF). There are three main subtypes: VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, and VEGFR3. VEGFR1 and 2 are expressed on vascular endothelial cells, whereas VEGFR3 is expressed on lymphatic endothelial. VEGFR1 and VEGFR2 play major roles in physiological as well as pathological angiogenesis. VEGFR3 can...

IACS-010759 is a Potent Inhibitor of Complex I of OXPHOS

Oxidative phosphorylation (OXPHOS) is a metabolic pathway in which cells use enzymes to oxidize nutrients. So it releases the chemical energy stored in nutrients to produce adenosine triphosphate (ATP). Besides, mitochondria are key players in the production and regulation of cellular bioenergy. Most adenosine triphosphate molecules are produced by...

CPL304110 is an Orally Active and Selective FGFR(1-3) Inhibitor

Over the last decade, the FGFRs family has become an attractive validated therapeutic target notably in cancer. It consists of four members (FGFR1 to FGFR4) which are structurally related cell surface RTKs. This FGF-FGFR axis participates in key biological processes that play significant roles in cell functions such as...

PD-089828 is an Inhibitor of FGFR-1, PDGFR-β, EGFR and c-Src Tyrosine Kinase

Protein tyrosine kinases comprise a group of enzymes. They catalyze the phosphorylation of certain proteins on specific tyrosine residues. The growth factor receptor tyrosine kinases are a subfamily. The kinases are activated on the high-affinity binding of growth factors to their cognate receptors. Members of this subfamily include PDGFR...

PD-161570 is an Inhibitor of FGF-1R, PDGFR, EGFR and c-Src Tyrosine Kinases

Fibroblast growth factors (FGF) are a family of cell-signaling proteins, which are involved in many processes, especially as the key factor of normal development. In addition, the FGFR family consists of a group of four homologous receptor tyrosine kinases. Besides, FGF1 was a member of a family of FGF...

AZD4547 is a Potent FGFR Family Inhibitor

Fibroblast growth factors (FGF) and their receptors play important roles in multiple biologic processes, such as tissue repair, hematopoiesis, angiogenesis, and embryonic development. The FGFR family mainly comprises 4 main members (FGFR1–4). FGFRs and FGFRs FGF ligand binding can result in FGFR dimerization. In addition, receptor autophosphorylation and activation...

ASP5878 is an Oral Active Inhibitor of FGFR 1, 2, 3, and 4, With Anti-tumor Activity

Hepatocellular carcinoma represents an aggressive cancer with poor prognosis. Fibroblast growth factor 19, a member of the fibroblast growth factor family, is a ligand for fibroblast growth factor receptor 4. In addition, it plays a crucial role in the progression of hepatocellular carcinoma. A study from Takashi Futami discovered...