Mode of action Imatinib binds close to the ATP-binding site of BCR-ABL and locks it in a closed inactive conformation which excludes ATP. This shuts down its sustained signaling, thus blocking leukemic cell growth. References [1] elisabeth buchdunger, catherine l. cioffi, norman law, david ...
Beside its direct effects to treat cancers as aTKI, imatinib can also be used as sensitizing agent for other chemotherapeutics. Some of the mechanisms have been highly related with certainABC transportersas well as other mode of actions. These results may shed the light for treatment ofMDRcancers...
Our data link for the first time the process of autophagy with the mode of action of imatinib. Induction of autophagy might represent an additional mechanism of imatinib to induce growth arrest, promote apoptosis in cancer cells and eventually even promote tumour regression....
Given the fact that lenti-Spike is replication-incompetent, imatinib mode of action does not require viral replication. Further study revealed that imatinib inhibited membrane fusion mediated by Spike and hACE2 (Fig. 3c, d). In the absence of TMPRSS2, imatinib was as potent as the cathepsin...
Treatment of chronic myeloid leukemia elderly patients in the tyrosine kinase inhibitor era. Omacetaxine mepesuccinate (omacetaxine) is a first-in-class cephalotaxine with a unique mode of action, independent of BCR-ABL, that has shown promising ac... F Cattina,V Cancelli,C Bergonzi,... -...
Mode of action Imatinib binds close to the ATP-binding site of BCR-ABL and locks it in a closed inactive conformation which excludes ATP. This shuts down its sustained signaling, thus blocking leukemic cell growth. references [1] elisabeth buchdunger, catherine l. cioffi, norman law, david ...
carbonate dehydrataseinhibitionmode of actionpoultrytestesJohnson AD, Walker GP.doi:10.1530/jrf.0.0230201Vivian OehlerS. BranfordE. PogosovaAgadjanyanN. ShahC. SawyersM. MaoP. LinsleyT. HughesJ. RadichComparative Biochemistry & Physiology Part A Physiology...
The Acta Pharmacologica Sinica www.chinaphar.com Wu LX et al npg 403 reaction was stopped by addition of 10 µL Kinase-Glo reagent, and the plate was read after a 10-min incubation time at RT on the Thermo Scientific Varioskan Flash in luminescence mode. Western blotting analysis of Bcr...
In this study, we analyzed further the mode of action of Imatinib in different appropriate cellular models of CML either sensitive or resistant to Imatinib and in CD34+ cells from CML patients. Pharmacological or short hairpin RNA-mediated inhibition of BCR-ABL triggers lysosomal membrane ...
Imatinib (IM) selectively inhibits the activity of some tyrosine kinases, including BCR-ABL1 and c-KIT. Mainly because of this mode of action, it has been registered as the first line treatment option for patients with chronic myeloid leukemia (CML) in the chronic, accelerated and blast ...