Title : The new allosteric inhibitor asciminib is susceptible to resistance mediated by ABCB1 and ABCG2 overexpression in vitro.

Pub. Date : 2018 Mar 2

PMID : 29568367






2 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Asciminib (previously ABL001), which binds the myristate-binding pocket of the Bcr-Abl kinase domain, is in phase I clinical trials as monotherapy and in combination with imatinib, nilotinib and dasatinib for the treatment of patients with refractory CML or Ph+ ALL. asciminib BCR activator of RhoGEF and GTPase Homo sapiens
2 In K562 asciminib-resistant cells, ABCG2 expression increased prior to BCR-ABL1 overexpression and remained high (up to 7.6-fold greater levels in resistant vs control cells, p < 0.001). asciminib BCR activator of RhoGEF and GTPase Homo sapiens