Amyotrophic lateral sclerosis (ALS), a progressive neurodegenerative disease involving loss
of motor neurons (MNs) and muscle atrophy, still has no effective treatment, despite much …

Small-molecule inhibitors of tyrosine kinases (TKIs) are the mainstay of treatment for many
malignancies and represent novel treatment options for other diseases such as idiopathic …

Tyrosine kinase inhibitors are a class of chemotherapeutic drugs that target specific protein
kinases. These tyrosine kinase inhibitors constitute a relatively new class of drugs which …

The introduction of imatinib (IM), a BCR-ABL1 tyrosine kinase inhibitor (TKI), has
represented a significant advance in the first-line treatment of chronic myeloid leukemia …

In the past decade, numerous tyrosine kinase inhibitors (TKIs) have been introduced in the
treatment of chronic myeloid leukemia. Given the significant interpatient variability in TKIs …

Abstract Imatinib, nilotinib, dasatinib, bosutinib, ponatinib, and asciminib are FDA-approved
tyrosine kinase inhibitors (TKIs) for chronic myeloid leukemia (CML), each of which has a …

Chronic myeloid leukemia was the first haematological neoplasia that benefited from a
targeted therapy with imatinib nearly 15 years ago. Since then, several studies have …

The permeability glycoprotein, encoded by the ABCB1 gene, is widely implicated in
multidrug resistance (MDR), as it has been shown to reduce the intracellular concentration …

Background Frequency relapses are common in Philadelphia chromosome-positive (Ph-
positive) acute lymphoblastic leukemia (ALL) following tyrosine kinase inhibitors (TKIs) …

We describe an atypical amine bioisostere, the trisubstituted hydroxylamine, that upon
incorporation into an approved dual cSRC/BCR-ABL1 kinase inhibitor yields 9, a compound …