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Association details:
Evidence:
Evidence Level:
Sensitive: D – Preclinical
Source:
Title:

BIM Regulation Is BTK Dependent and Can be Targeted By Entospletinib in Ibrutinib Refractory Mutants

Published date:
11/06/2019
Excerpt:
...BTKC481S overexpressing cells were used to validate….Similar to ibrutinib, SYK inhibitor entospletinib leads to reduction of BIM phoshorylation in wildtype Ramos. But in contrast to ibrutinib, both BTK and BIM phosphorlyation were also reduced upon entospletinib treatment in Ramos cells expressing the BTKC481S mutant, which indicates that entospletinib can overcome ibrutinib resistance caused by BTKC481S mutation.
DOI:
https://doi.org/10.1182/blood-2019-127148