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...
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)....
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...
Adagrasib (MRTX849), a Potent KRAS G12C Inhibitor for KRAS G12C-mutated Locally Advanced or Metastatic NSCLC Research
On December 12, 2022, FDA granted accelerated approval to Adagrasib (Krazati), for adult patients with KRAS G12C-mutated locally advanced or metastatic NSCLC. In 2021, FDA approved the selective KRASG12C mutant inhibitor Sotorasib (AMG 510) as a second-line treatment of KRASG12C mutation-positive NSCLC. As a result, Adagrasib (MRTX849) is the...
A947 is a Selective and Efficacious SMARCA2 PROTAC in SMARCA4 Mutant Cancers
SWI/SNF complex has two important ATP-dependent helicases, SMARCA2 and SMARCA4. In fact, SMARCA2 and SMARCA4 share strong protein sequence homology. But SWI/SNF helicase SMARCA4 is frequently mutated in cancer. The inactivation of SMARCA4 results in a cellular dependence on SMARCA2. Thus, SMARCA2 becomes an attractive synthetic lethal target. Proteolysis...
Mitonafide is a Cytostatic Agent, Inhibiting DNA and RNA Synthesis
Cytostatic agents are cell components or drugs that inhibit cell division. Specifically, cell growth arrest is an important prerequisite for structured multicellular organisms. Cell inhibitors achieve these growth-inhibitory effects through specific mechanisms of action. Some cell inhibitors are not only used in cancer treatment, but also for other diseases...
BI-0474 is a Potent KRAS G12C inhibitor
K-Ras protein is a kind of GTPase. Specifically, it is a kind of enzyme that converts nucleotide guanosine triphosphate (GTP) to guanosine diphosphate (GDP). In this way, the K-Ras protein acts like a switch. Besides, KRAS is the most frequently changed homotype in NSCLC cases with RAS mutation. Moreover,...