Category: Colorectal Cancer

Pimasertib is a Highly Selective and ATP non-Competitive Allosteric Inhibitor of MEK1/2

The RAS/RAF/MEK/MAPK and the PTEN/PI3K/AKT/mTOR pathways are key regulators of proliferation and survival in human cancer cells. RAF is a serine/threonine kinase that activates downstream signals in response to activated GTP-bound RAS by phosphorylating MEK  (MEK1 and MEK2). They in turn phosphorylate and activate MAPK (or ERK1 and ERK2)....

Lomeguatrib is a O6-Methylguanine-DNA Methyltransferase (MGMT) Inhibitor

O6-alkylguanine DNA alkyltransferase (also known as AGT, MGMT or AGAT) is a protein that in humans is encoded by the O6-methylguanine DNA methyltransferase (MGMT) gene. MGMT repairs the naturally occurring mutagenic DNA lesion O6-methylguanine back to guanine and prevents mismatch and errors during DNA replication and transcription. MGMT repairs...

Dovitinib is a Multi-Targeted Tyrosine Kinase Inhibitor

Tyrosine kinase is an enzyme that can transfer phosphate groups from ATP to tyrosine residues of specific proteins in cells. Specifically, this covalent post-translational modification is a key component of normal cell communication and homeostasis maintenance. Tyrosine kinase is an important mediator of signal cascade reaction. Besides, it plays...

Axitinib is a Multi-Targeted Tyrosine Kinase Inhibitor

Vascular endothelial growth factor (VEGF) is an important signal protein. Importantly, it is involved in angiogenesis and angiogenesis (blood vessels grow from a pre-existing vascular system). All members of VEGF family stimulate cell response by binding to tyrosine kinase receptors (VEGFRs) on the cell surface. Thus they dimerize and...

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...

Ganetespib (STA-9090) is a HSP90 Inhibitor

Hsp90 is a molecular chaperone that regulates the posttranslational folding, stability, and function of its protein substrates (client proteins), many of which play critical roles in cell growth, differentiation, and survival. The Hsp90 machinery serves as a biochemical buffer for a number of oncogenic signaling proteins causally implicated in...

Birinapant (TL32711), a Bivalent Smac Mimetic, is an Antagonist for XIAP and cIAP1

XIAP is a protein that prevents apoptosis. XIAP is a member of apoptosis protein family (IAP) inhibitors. Specifically, IAP blocks cell death in vitro and in vivo by inhibiting different caspases. The caspase inhibitory activity of XIAP is negatively regulated by at least two XIAP interacting proteins XAF1 and...