TAI-1 is an Orally Active and Highly Potent Hec1 Inhibitor
Hec1 (Ndc80) is one of the outer kinetochore proteins and forms heterotetramers with proteins NUF2, SPC25, and SPC24. Specifically, drugs that interfere with mitosis are part of the most successful chemotherapeutic compounds for cancer in clinical practice. Hec1, a component of mitochondria, is overexpressed in a variety of human...
GMB-475, a BCR-ABL1 Inhibitor Based on PROTAC, Has Potential to Overcome BCR-ABL1-Dependent Drug Resistance
Chronic myeloid leukemia is a myeloproliferative disorder characterized by the presence of the oncogenic fusion protein BCR-ABL1. ABL1, one of the fusion partners in the BCR-ABL1 protein, contains an allosteric myristoylation binding site. Especially, the proteolysis targeting chimera (PROTAC) technology provides a unique toolkit for probing the non-kinase roles...
CHMFL-ABL-039, a Selective Type II Native and Drug-Resistant Mutant BCR-ABL Inhibitor for Chronic Myeloid Leukemia
Chronic myeloid leukemia (CML) is a white blood cell disorder, accounting for about 15% of the adult leukemias. The critical driving force of pathogenesis of CML identified is BCR gene and ABL kinase gene fusion. It results in the constitutive activation of ABL kinase. And the activation is essential...