Category: Solid Tumors

DRF-1042 is an Orally Active DNA topoisomerase I Inhibitor

Inhibitors of the enzyme topoisomerase I are cytotoxic for tumor cells because of their ability to cause DNA damage. Specifically, DNA Topoisomerase I (Top1) is one main cellular factor controlling topological homeostasis. Top1 activity can relax negative supercoils by cutting one of the DNA strands. This can create a...

Alpelisib is a Selective and Orally Active PI3Kα Inhibitor for Metastatic Breast Cancer

Phosphatidylinositol-3-kinases (PI3Ks) are a family of important lipid kinases. PI3Ks are important in controlling the signaling pathways involved in cell proliferation, motility, cell death, and cell invasion. Moreover, PI3Ks control and deliver cellular signals in the PI3K/Akt/mTOR pathway by phosphorylating phosphatidylinositol 4,5-bisphosphate (PIP2) to phosphatidylinositol 3,4,5-trisphosphate (PIP3) on the...

AMG-510 is a First-in-Class, Orally Active, and Selective KRAS G12C Inhibitor

The KRAS oncoprotein is a GTPase and an essential mediator of intracellular signaling pathways. They are involved in tumor cell growth and survival. Somatic, activating mutations in KRAS are a hallmark of cancer. Furthermore, they prevent the association of GTPase-activating proteins, thus stabilizing effector binding and enhancing KRAS signaling....

MS645, a Bivalent BET BrD Inhibitor, Inhibits BRD4 Transcriptional Activity

Bromodomains (BrDs) in transcription proteins bind acetyl-lysine in histones and transcription factors to direct gene transcription in biology and disease conditions.  BRD4 contains two characteristic tandem BrDs. Meanwhile, BRD4 is a major drug target owing to its implicated functions in oncogenesis and inflammation. BET protein BRD4 in gene transcription...

S516 is a Potent Tubulin Polymerization Inhibitor

The microtubules act as an attractive target for anticancer drug discovery nowadays. Disruption of microtubules can induce cell cycle arrest in the G2-M phase and formation of abnormal mitotic spindles. The tubulin polymerization inhibitors have emerged as one of promising anticancer therapeutics because of their dual mechanism of action,...

MRTX849 is an Orally Active and Covalent Inhibitor of KRAS G12C

KRAS mutations are the most common mutations. Especially, the KRAS oncogene encodes a binding protein that plays a crucial role in transmitting signals from extracellular growth factors to the cell nucleus. KRAS mutations occur commonly in colorectal carcinomas. KRASG12C mutations are present in lung and colon adenocarcinoma as well...

Vorolanib is an Orally Active Inhibitor of VEGFR and PDGFR 

Vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) are cell-surface tyrosine kinase receptors. They represent targets for anticancer therapy in solid tumors. For accurately validating the therapeutic potential of these target-specific agents, the in vivo quantification of VEGFR/PDGFR activity is critically important. It is not...