Category: Lung Adenocarcinoma

LCS3 is a Glutathione Disulfide Reductase (GSR) and TXNRD1 Inhibitor

Glutathione Disulfide Reductase (GSR), also known as glutathione reductase (GR), catalyzes the reduction of glutathione disulfide (GSSG) to glutathione (GSH) in the presence of NADPH and flavin adenine dinucleotide (FAD). GSH acts as a scavenger of reactive oxygen species (ROS) such as free radicals, peroxides, lipid peroxides and heavy...

Almonertinib is an Orally Active and Irreversible EGFR Inhibitor

Lung cancer is one of the most common malignant tumors in the world. Its lethality ranks the first among many malignant tumors. In addition, the overexpression of the human ATP-binding cassette (ABC) drug transporter ABCB1 (P-gp) or ABCG2 (BCRP) in cancer cells often contributes significantly to the development of...

DT-061 is an Orally Active PP2A Activator

Protein phosphatase 2A (PP2A) comprises a family of serine/threonine phosphatases, minimally containing a well-conserved catalytic subunit. PP2A plays a prominent role in the regulation of specific signal transduction cascades. Additionally, PP2A interacts with a substantial number of other cellular and viral proteins. DT-061 is an orally bioavailable small-molecule activator...

Cilengitide is a Selective Integrin Inhibitor for αvβ3 and αvβ5 Receptor

Integrins are heterodimeric cell surface adhesion receptors that consist of two noncovalently associated alpha and beta subunits. In particular, Integrins are heterodimeric transmembrane proteins composed of one α and one β subunit. Especially, Integrins are crucially important because they are the main receptor proteins that cells use to bind...

BM-1197 is a Potent and Selective Dual Bcl-2/Bcl-xL Inhibitor

Bcl-2 and Bcl-xL are critical regulators of apoptosis. The pharmacological inhibition of Bcl-2 and Bcl-xL represents a promising strategy for cancer treatment. In addition, BM-1197 is a potent and efficacious dual inhibitor of Bcl-2 and Bcl-xL. BM-1197 binds to Bcl-2 and Bcl-xL proteins with Ki values less than 1...

BPI-9016M is an Orally Active and Selective Dual c-Met/AXL Inhibitor

c-Met is a membrane-spanning receptor tyrosine kinase. It has a high affinity for binding to hepatocyte growth factor (HGF). As we all know, HGF/c-Met signaling often involves activation of its downstream pathways. High-level Met gene amplification, mutation or protein overexpression can lead to aberrant activation of the HGF/c-Met pathway. In...

MRTX849 is an Orally Active and Covalent Inhibitor of KRAS G12C

KRAS mutations are the most common mutations. Especially, the KRAS oncogene encodes a binding protein that plays a crucial role in transmitting signals from extracellular growth factors to the cell nucleus. KRAS mutations occur commonly in colorectal carcinomas. KRASG12C mutations are present in lung and colon adenocarcinoma as well...