Secondly, by not inhibiting kinases such as EGFR, KIT, CSF1R, PDGFR or the sSRC-family kinases that are associated with off-target activities of TKIs such as bosutinib, dasatinib, imatinib, nilotinib and ponatinib, asciminib is not expected to be associated with cross-intolerance. Tdoi:10.1182/blood-2020-140968P. Schuld...
Mechanism of Action Imatinib mesylate is a protein tyrosine kinase inhibitor that inhibits bcr-abl tyrosine kinase, a constitutively abnormal tyrosine kinase produced by abnormalities of the Philadelphia chromosome in chronic myeloid leukaemia (CML). It inhibits proliferation and induces apoptosis in bcr...
Mechanism of Action Interferon alpha/beta receptor 1 Agonist Interferon alpha/beta receptor 2 Agonist Identification Summary Peginterferon alfa-2b is a purified form of human interferon used to stimulate the innate antiviral response in the treatment of hepatitis B and C, genital warts, and some canc...
Dasatinib binds to the active and inactive conformation of the ABL kinase domain with a higher affinity than imatinib.6 In chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL, dasatinib inhibits cell growth. Also, dasatinib has in vitro activity ...
Dasatinib binds to the active and inactive conformation of the ABL kinase domain with a higher affinity than imatinib. Dasatinib inhibits cell growth in chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Also, dasatinib has in vitro activity ...
We report that imatinib, an Abl tyrosine kinase inhibitor, robustly decreases SARS-CoV-2 infection and uncover a mechanism of action. We show that imatinib inhibits the infection of SARS-CoV-2 and its surrogate lentivector pseudotype. In latter, imatinib inhibited both routes of viral entry, ...
Target-identification and mechanism-of-action studies have important roles in small-molecule probe and drug discovery. Biological and technological advances have resulted in the increasing use of cell-based assays to discover new biologically active small molecules. Such studies allow small-molecule action...
However, while there is a great deal of evidence detailing the effects of COS and DEH on considerable signaling pathways and cellular functions, a global view of their mechanism of action remains elusive. This review systematically summarizes the antitumor activity and mechanism of COS and DEH in ...
Mechanism of action Designed to overcome imatinib resistance resulting from Bcr-Abl kinase mutations, upon administration, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl portion of the Bcr-Abl fusion protein, resulting in the inhibition of the cons...
Foretinib is a multikinase inhibitor whose mechanism of action is incompletely understood. We investigated here the effect of Foretinib on chronic myelogenous leukemia (CML) cell lines either sensitive (IM-S) or resistant (IM-R) to the tyrosine kinase inhibitor Imatinib. Foretinib decreased viability...