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...
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...
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...
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...
Tiragolumab is An Immune Checkpoint Inhibitor Binding to T-cell Immunoglobulin and TIGIT
Tiragolumab is a potent TIGIT inhibitor. Tiragolumab alone or in combination with the PD-L1 inhibitor Atezolizumab has effects on solid cancers. Additionally, at two recent medical meetings, the agent achieves statistically significant results in multiple solid malignancies. Especially in small cell lung cancer (NSCLC). Lung cancer is the most...