Tag: Bcr-Abl

Bafetinib is a Lyn and Bcr-Abl Tyrosine Kinase Inhibitor

The treatment of Philadelphia chromosome-positive (Ph+) leukemias has improved markedly. There are some inhibitors of Bcr-Abl tyrosine kinase (TK) that are effective for Ph<sup>+</sup> leukemias. However, resistance to imatinib can develop by various molecular mechanisms. They include Bcr-Abl overexpression, mutations within the imatinib-binding site of Bcr-Abl, expression of a...

Rigosertib is a Multi-Kinase Inhibitor and a Selective Anti-Cancer Agent

Polo-like Kinases (PLKs) are a group of highly conserved serine/threonine protein kinases. PLKs play a key role in processes such as cell division and checkpoint regulation of mitosis. Mammalian cells contain at least four members of Plk gene family, termed Plk1, Plk2 (also known as Snk), Plk3 (also known...

Dasatinib is an Orally Active Dual Bcr-Abl and Src Family Tyrosine Kinase Inhibitor

Src is an important member of the non-receptor protein tyrosine kinase. Furthermore, Src plays a key role in the regulation of many cells through the extracellular ligand binding to the receptor and the cell adhesion molecule activation in cell cycle-specific stage. Src can affect cell adhesion, motility, proliferation, and...

SIAIS178 is a Potent and Selective PROTAC-Based BCR-ABL Degrader

Proteolysis targeting chimeras (PROTACs) work by inducing selective intracellular proteolysis rather than acting as a conventional enzyme inhibitor. Besides, PROTACs consists of two covalently linked protein-binding molecules. One can engage an E3 ubiquitin ligase, and another binds to a target protein meant for degradation. Moreover, PROTACs need only to...

A 419259 is a Potent Src Inhibitor

Chronic myelogenous leukemia (CML) is a human malignancy and affects hematopoietic progenitor cells. The CML is driven by Bcr-Abl. Additionally, Bcr-Abl is a 210 kDa chimeric tyrosine kinase that transforms fibroblasts, growth factor-dependent hematopoietic cell lines. Bcr-Abl is a constitutively active protein-tyrosine kinase and can stimulate the proliferation and...