Izalontamab (SI-B001) is a Bispecific Anti-EGFR/HER3 mAb for Cancer Research
EGFR (epidermal growth factor receptor) is a member of the ErbB receptor family1. Besides, EGFR is a common therapeutic strategy in epithelioma such as lung adenocarcinoma, colon cancer, head and neck cancer, and esophageal cancer, where the over-expression of EGFR caused by gene mutation plays an essential role in...
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...
Navitoclax (ABT-263) is an Orally Active Bcl-2 Inhibitor for Chronic Lymphocytic Leukemia Research
Bcl-2 family proteins, known as B-cell lymphoma 2, are regulators of programmed cell death. Additionally, the bcl-2 family includes pro-apoptotic and anti-apoptotic proteins. Anti-apoptotic proteins refer to Bcl-2, Bcl-x (L), Bcl-w, and Mcl-1. They block apoptosis by isolating pro-apoptotic proteins Bax and Bak. Therefore, one of the main methods...
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)....
MC2590, a Potent HDAC Inhibitor, inhibits HDAC1-3, -6, -8, and -10
Histone deacetylase (HDAC) is an epigenetic enzyme that regulates gene expression through histone deacetylation. It leads to more closed chromatin structure and gene expression inhibition. Many non-histones are also targets of HDAC, such as α Microtubulin, heat shock protein (HSP) 90, and hypoxia-inducible factor HIF-1 α. Specifically, HDAC is...
Amivantamab (JNJ-61186372) is a Human EGFR-MET Bispecific Antibody
Epidermal growth factor (EGF) is a protein that stimulates cell proliferation, differentiation, and survival by binding to its receptor EGFR. Additionally, It exists in platelets, urine, saliva, milk, tears, and blood plasma. The mesenchymal-epithelial transition (MET) is the reverse process of the epithelial-mesenchymal transition (EMT). Moreover, MET involves morphological...
OTS193320 is a SUV39H2 Methyltransferase Activity Inhibitor
SUV39H2 is a histone lysine-specific methyltransferase. Specifically, SUV39H2 introduced H3K9me3 to induce transcriptional inhibition. This plays a key role in heterochromatin maintenance, DNA repair, more recently, carcinogenesis. Besides, the genetic ablation of SUV39H1 and SUV39H2 genes leads to severe chromosome instability. For example, abnormally long telomeres are less bound...