Category: Non-Small Cell Lung Cancer

Rapamycin is a Specific mTOR Inhibitor

mTOR (mammalian target of Rapamycin) is a protein that in humans is encoded by the mTOR gene. mTOR is a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. In addition, mTOR links with other proteins and serves as a core...

Nimotuzumab is a Humanized IgG1 Monoclonal Antibody Targeting EGFR

The epidermal growth factor receptor (EGFR) is a transmembrane protein. The dimerization of EGFR stimulates the activity of intracellular protein tyrosine kinase. Therefore, several tyrosine (y) residues in the C-terminal domain of EGFR undergo autophosphorylation. These include y992, y1045, y1068, y1148, and y1173, as shown in the adjacent chart....

LP-261 is a Potent and Orally Active Anti-Mitotic Agent

In this article, we will introduce a potent  anti-mitotic agent, LP-261. LP-261 shows inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM. Firstly, in vitro, LP-261 exhibits potent G2/M block activity in multiple cell lines and exhibits a range of activity from 0.01 μM to 0.38 μM. Besides, the...

Rociletinib (CO-1686) is an Orally Active EGFR-Mutant Inhibitor

NSCLC accounts for almost 85% of all lung cancers. Additionally, lung cancer continues to be the most common cause of cancer-related deaths worldwide. Activating mutations in the epidermal growth factor receptor (EGFR) are key drivers of NSCLC malignancy. Patients with the most common EGFR mutations (L858R mutation in exon...

DGY-06-116 is an Irreversible Covalent and Selective Src Inhibitor

Src kinase family is a family of non-receptor tyrosine kinases. DGY-06-116 is a selective Src inhibitor. DGY-06-116 is an SRC-directed covalent kinase inhibitor that displays efficient covalent target labeling and irreversible cellular inhibition of SRC signaling. Furthermore, DGY-06-116 inhibits SRC for an extended duration, likely due to its ability...

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...

LC-2 is a First-in-Class PROTAC-Based KRAS G12C Degrader

KRAS gene is one of the most frequently mutated oncogenes in cancer. KRAS encodes a small, membrane-bound GTPase that relays signals from receptor tyrosine kinases (RTKs). It promotes cell proliferation, cell differentiation, or cell survival. In normal cells, KRAS functions as a molecular switch, cycling between an inactive, GDP-bound “off” state and...