Category: Lymphoma

E7820 is an α2 Integrin Inhibitor with Anti-Tumor Activity

Vascular endothelial growth factor (VEGF) is a prime contributor to tumor angiogenesis. Most tumor cells produce high levels of VEGF and VEGF receptors associated with tumor endothelial cells. E7820 is an aromatic sulfonamide derivative and an Angiogenesis inhibitor. E7820 inhibits in vitro proliferation and tube formation of human umbilical...

BSJ-03-204 is a Selective Palbociclib-Based CDK4/6 Dual Degrader (PROTAC)

The chimeric proteolytic enzyme (PROTAC) is a heterobifunctional small molecule. Specifically, it is composed of two active domains and an adaptor that can remove specific proteins that are not needed. Besides, PROTAC does not act as a conventional enzyme inhibitor, but by inducing selective intracellular proteolysis. Moreover, PROTAC includes...

Telomestatin, a Potent Telomerase Inhibitor, Facilitates the Formation of Intramolecular G-quadruplexes

Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. It selectively facilitates the formation of intramolecular G-quadruplexes, in particular, that produced from the human telomeric sequence d[T2AG3]4. Firstly, in vitro, Telomestatin promotes or stabilizes the formation of the intramolecular G-quadruplex. When the DNA concentrations are at 0.005...

CMLD012612 is a Potent Eukaryotic Initiation Factor 4A (eIF4A) Inhibitor

Small molecules show targeting the translation machinery that can be used for the research of cancer, viral infection, and neurodegeneration. In particular, a class of translation inhibitors that possess potent cytotoxic activity against tumor cells is in the development. In this article, we will introduce a potent eukaryotic initiation...

EEDi-5285 is an Orally Active Embryonic Ectoderm Development (EED) Inhibitor

Polycomb protein EED is a member of the Polycomb-group (PcG) family. Specifically, the Polycomb group (PCG) is a class of proteins responsible for cell differentiation during development through transcriptional inhibition. In mammals, PcG protein is part of two major transcriptional inhibition complexes, known as PRC1 and PRC2. Besides, the...

Ilorasertib is an Orally Active ATP-Competitive Multitargeted Kinase Inhibitor

Aurora kinases are key regulators of mitosis that overexpress in many cancer types. Ilorasertib (ABT-348) is a potent inhibitor of all three Aurora kinases, although it has greater activity versus Aurora B and C than Aurora-A. In addition, Ilorasertib also inhibits VEGFRs and PDGFRs, and the Src families of...