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...
RLA-5331 is an Iron Activator Containing Anti-androgen
Prostate cancer (PCa) is one of the most prevalent malignancies in the world. Depending on the grade of cancer, a variable percentage of these patients experience progression to castration-resistant prostate cancer (CRPC) within 10 years. However, CRPC can develop into metastatic castration-resistant prostate cancer (MCRPC). Research has shown that...
Talotrexin, A RFC Specific Inhibitor, Targets DHFR to Inhibit Tumor Growth
In this article, we will introduce a potent RFC (reduced folate carrier) specific inhibitor Talotrexin (PT523). Talotrexin, an analog of Aminopterin, is a nonpolyglutamatable classic antifolate. Additionally, it selectively inhibits RFC transport. Mammals cannot synthesize folates de novo, their cellular uptake from the extracellular milieu is essential. Besides, The...
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...
BPDA2 is a Highly Selective and Competitive SHP2 Inhibitor
SH2-containing protein tyrosine phosphatase 2 (SHP2) is a carcinogenic phosphatase. Specifically, SHP2 participates in the downstream signal transmission of various RTK. So it is the shared signal node for analysis. The phosphatase activity of SHP2 is necessary for important cancer-related signaling pathways (such as RAS and PI3K). Besides, the...
Opnurasib (JDQ-443) is an Orally Active KRAS G12C Inhibitor
Kirsten rat sarcoma (KRAS) is a member of the RAS family. KRAS is a key regulator of signaling pathways responsible for cell proliferation, differentiation, and survival. KRAS mutations are genetic drivers of multiple cancer types, especially colorectal cancer (CRC), pancreatic ductal adenocarcinoma (PDAC), and non-small cell lung cancer (NSCLC)....
Elacestrant (RAD1901) is an Orally Available Estrogen Receptor Degrader
Breast cancer is subdivided into categories based on the tumor receptor status. Specifically, whether the tumor expresses estrogen receptor (ER), progesterone receptor (PR), or Her2. And, with ER+ disease makes up the majority of patients in the breast cancer patient population. Although there are currently available drugs against ER-positive...