Tag: cancer

Sotorasib (AMG-510) is an Orally Bioavailable KRAS G12C Covalent Inhibitor

The KRAS oncoprotein is a GTPase and an essential mediator of intracellular signaling pathways. KRAS oncoprotein regulates tumor cell growth and survival. However, KRAS also is the most frequently mutated oncogene in cancer and encodes a key signaling protein in tumors. In addition, KRASG12C mutant is present in approximately...

SH-BC-893 is an Orally Active Anti-neoplastic Sphingolipid Analog

Cancer and metabolism-related diseases have a significant impact on humans. Cancer cells are constitutively anabolic. It will cause quiescence and catabolism in normal cells because of they are unable to tolerate nutrient stress. So, oncogenic mutations will reselect the metabolic circuitry during the tumorigenic process to meet the increased...

ARN24139 is a TopoII Inhibitor with Promising Antiproliferative Activity

Topoisomerase II is a ubiquitous enzyme in all branches of life that alters DNA supercoils and breaks double-stranded DNA fragments during processes such as replication and transcription. Eukaryotic Topoisomerase II functions as a homodimer and requires ATP and divalent metal ions for overall catalytic activity. It interconverts different topologies...

YX-2-107, a PROTAC, is a Selective CDK6 Degrader

Ph+ALL (Philadelphia chromosome-positive acute lymphoblastic leukemia) is a rare subtype of leukemia characterized by the abnormal formation of the Philadelphia chromosome, which occurs when pieces of chromosomes 9 and 22 switch with each other. The incidence of Ph+ ALL increases with age, and occurs in up to 50 %...