Balixafortide is a Selective and Well-Tolerated Peptidic CXCR4 Antagonist
Despite the introduction of new targeted therapies and cytotoxic agents, chemotherapy-pretreated metastatic breast cancer (MBC) remains an essentially incurable disease with only moderate median overall survival (OS). over 20 human tumor types overexpress C-X-C chemokine receptor type 4 (CXCR4). CXCR4 levels correlate with aggressive metastatic phenotypes and negative prognosis...
DB1976 is a Fully Efficacious Transcription Factor PU.1 Inhibitor
ETS transcription factors mediate a wide array of cellular functions and are attractive targets for pharmacological control of gene regulation. Transcription factors (TFs) are central to many cellular processes and account for 5-10% of genes in eukaryotes. Besides, sequence-specific binding is an obligate step in ETS-mediated gene activation. So...
JBJ-04-125-02 is a Mutant-Selective and Orally Active EGFR Inhibitor
Epidermal growth factor receptor (EGFR) is a transmembrane receptor protein in humans. The discovery of activating mutations in EGFR detected in 10% to 30% of patients with non–small cell lung cancer (NSCLC). In addition, it has revolutionized the treatment of this disease. Until recently, EGFR tyrosine kinase inhibitors (TKI), including...
PS315, an Allosteric PKC Inhibitor Binding to the PIF-Pocket
Members of the protein kinase C (PKC) family are regulated by phosphorylation and by an N-terminal extension of the catalytic domain. In addition, AGC kinases are a group of protein kinases comprising PKA, protein kinase G, and PKC families. They typically have three conserved phosphorylation sites. Besides, all PKCs...
CCT36776 is a PROTAC-based Pirin Protein Degradation Probe
Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules. It induces rapid and selective protein degradation, via the proteasome. PROTACs contain two different ligands connected by a linker, one portion of the molecule engages the target protein. While the other, attach via a flexible linker, recruits an E3 ubiquitin ligase to...
CM-272, a First-in-class, Reversible and Dual G9a/DNMTs Inhibitor
Therapy of hematological malignancies is undergoing a paradigm shift. It is away from the traditional chemotherapy towards the targeting of proteins driving the cancer phenotype. The novel therapeutic approach relies on the use of epigenetic drugs. It aims to reverse critical epigenetic events underlying human cancer pathogenesis, particularly abnormalities...
Ro 90-7501, a Radiosensitizer, is an Aβ42 Fibril Assembly and PP5 Inhibitor
Cervical cancer is one of the most common cancers among women worldwide. Ro 90-7501 is an inhibitor of the amyloid β42 (Aβ42) fibril assembly. It is associated with Alzheimer’s disease. The usual method for Cervical cancer treatment is Radiotherapy, especially for locally advanced cancer. However, the treatment results are...