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...
Rineterkib is an Orally Active RAF and ERK1/2 Inhibitor
ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes. It includes cell adhesion, cell cycle progression, cell migration, cell survival, differentiation, metabolism, proliferation, and transcription. MEK1/2 catalyze the phosphorylation of human...
Olafertinib is a Third-Generation EGFR TKI
Non-small-cell lung carcinoma (NSCLC) is any type of epithelial lung cancer other than small-cell lung carcinoma (SCLC). NSCLC patients with activating EGFR mutations initially respond to first-generation EGFR inhibitors. Epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein with an extracellular epidermal growth factor binding domain and an intracellular...
DBPR112 is an Orally Active EGFR (both WT and Mutant) Inhibitor
Epidermal growth factor receptor (EGFR), a transmembrane protein, is a receptor of EGF family members of extracellular protein ligands. Specifically, EGFR expresses at elevated levels in different forms of cancer and is usually positively relevant to cancer progression and adverse prognosis. Different mutant forms of this protein also contribute...
IMT1 is a First-in-Class Specific and Noncompetitive Human POLRMT Inhibitor
Mitochondria provide cellular energy through its oxidative phosphorylation system, which needs to coordinate the expression of genes encoded by nuclear and mitochondrial genomes (mtDNA). Specifically, the transcription of mtDNA in circular mammals depends on a single mitochondrial RNA polymerase (POLRMT). Besides, three proteins are required for mitochondrial transcription initiation:...
BDTX-189 is an Orally Active Inhibitor of Allosteric EGFR and HER2 Oncogenic Mutations
Epidermal growth factor receptor (EGFR) is a growth-factor-receptor tyrosine kinase. Elevated levels of the EGFR, and/or its cognate ligands act as a common component of multiple cancer types and appear to promote solid tumor growth. BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations....
CMLD-2 is Inhibits HuR and Induces Apoptosis
Hu antigen R (HuR) is an RNA binding protein. Specifically, Its overexpression in human cancer is associated with aggressive disease, drug resistance, and poor prognosis. HuR is highly abundant in many types of cancer and promotes tumorigenesis through cancer-related mRNA interactions. Besides, HuR has related to the regulation of...