Category: Non-Small Cell Lung Cancer

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,...

BT5528 is a Bicyclic Peptide Toxin Conjugate, an EphA2 Activator.

The tyrosine kinase EphA2 belongs to the Eph receptor family and is produced in large quantities in tumor tissues. Specifically, its content is relatively low in most normal adult tissues. The liver ligand receptor (Eph) is the most important receptor tyrosine kinase (RTK). Besides, Eph receptor signal transduction contributes...

G12Si-5 is a K-Ras G12S Mutant Covalent Inhibitor

KRAS (Kirsten rat sarcoma virus) is one of the most commonly altered oncogenes in human cancers. Recurrent oncogenic mutations in KRAS can reprogram glutamine metabolism to increase the production of NADPH to control ROS. Besides, mutant KRAS promotes the expression of nucleotide synthesis genes and controls glucose uptake and...

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...

Seliciclib (Roscovitine) is an Orally Active and Selective CDKs Inhibitor

Cyclin-dependent kinases (CDKs) are serine/threonine kinases whose activity depends on a regulatory subunit-a cyclin. Based on the sequence of the kinase domain, CDKs belong to the CMGC group of kinases, along with MAPKs, Gsk3β, DYRK family and CDK-like kinases. There are around 20 Cyclin-dependent kinases (CDK1-20) known till date....

Rigosertib is a Multi-Kinase Inhibitor and a Selective Anti-Cancer Agent

Polo-like Kinases (PLKs) are a group of highly conserved serine/threonine protein kinases. PLKs play a key role in processes such as cell division and checkpoint regulation of mitosis. Mammalian cells contain at least four members of Plk gene family, termed Plk1, Plk2 (also known as Snk), Plk3 (also known...

Avitinib is an Irreversible, Mutant-Selective EGFR Inhibitor

The epidermal growth factor receptor (EGFR) belongs to the ErbB family (also known as the EGFR family) of receptor tyrosine kinases (RTK). EGFR family comprises four distinct receptors: the EGFR (ErbB1, HER1), ErbB-2 (HER2, neu in rodents), ErbB-3 (HER3) and ErbB-4 (HER4). It is worth mentioning that EGFR family...