ML-097 (CID-2160985) is a Pan Ras-related GTPases Activator
Ras, is a family of related proteins expressed in all animal cell lineages and organs. All Ras protein family members belong to a class of protein called small GTPase. Furthermore, Ras is a prototypical member of the Ras protein superfamily that regulates a variety of cellular behaviors. As a...
ML-099 is a pan Ras-Related GTPases Activator
To date, we identified 167 small GTPases in humans which are key signal transducing enzymes. Small GTPases comprise five main families whose eponymous members are Ras, Rho, Rab, ADP-ribosylation factor (Arf) and Ran. Small GTPases link extracellular cues to the neuronal responses required for the construction of neuronal networks,...
Lonafarnib is an Orally Active FPTase Inhibitor
Farnesyl transferase (FTase) is a zinc-dependent enzyme, which coordinates a zinc cation on its β subunit at the lip of the active site. FTase has two subunits: a 48kDa α-subunit and a 46kDa β-subunit. And it adds a 15-carbon isoprenoid called a farnesyl group to proteins bearing a CaaX...
APS6-45, an Orally Active Tumor-Calibrated Inhibitor, Inhibits RAS/MAPK Signaling
Medullary thyroid cancer is a form of thyroid carcinoma which originates from the parafollicular cells, which produce the hormone calcitonin. Synthetic tailoring of approved drugs for new indications is often difficult, as the most appropriate targets may not be readily apparent and therefore few roadmaps exist to guide chemistry....
MCP110 is an Inhibitor of Ras/Raf-1 Interaction
Ras is a small GTPase and interacts with the protein Raf to create activated Ras-Raf complex that activates the downstream effectors in the ERK pathway. Malfunctioning Ras-Raf switches cause cancer. Ras-Raf interaction has taken a center stage in cancer research. Ras is a peripheral membrane protein that acts as...
CID-1067700 is a Ras GTPases pan-Inhibitor with High Efficacy Towards Rab7
Alteration of small GTPase functions is a hallmark of genetic and sporadic human diseases, making GTPase family members attractive though understudied targets. Specifically, the Ras superfamily of GTPases includes Arf, Rho, Ras and Rab GTPase subfamilies. Besides, they regulate a broad range of cellular processes ranging from membrane trafficking...
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...