Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class

E Salah, E Ugochukwu, AJ Barr… - Journal of medicinal …, 2011 - ACS Publications
ABL2 (also known as ARG (ABL related gene)) is closely related to the well-studied Abelson
kinase cABL. ABL2 is involved in human neoplastic diseases and is deregulated in solid …

Structure of the ABL2/ARG kinase in complex with dasatinib

BH Ha, MA Simpson, AJ Koleske… - … Section F: Structural …, 2015 - journals.iucr.org
ABL2/ARG (ABL-related gene) belongs to the ABL (Abelson tyrosine-protein kinase) family
of tyrosine kinases. ARG plays important roles in cell morphogenesis, motility, growth and …

Abl inhibitor BMS354825 binding mode in Abelson kinase revealed by molecular docking studies

C Gambacorti-Passerini, M Gasser, S Ahmed… - Leukemia, 2005 - nature.com
A new SRC-Abl dual inhibitor, BMS354825, has recently been presented as a possible tool
to overcome resistance to imatinib in neoplasias caused by oncogenic variants of the …

A new series of antileukemic agents: Design, synthesis, in vitro and in silico evaluation of thiazole-based ABL1 kinase inhibitors

E Zeytün, MD Altıntop, B Sever… - Anti-Cancer Agents …, 2021 - ingentaconnect.com
Background: After the approval of imatinib, more than 25 antitumor agents targeting kinases
have been approved, and several promising candidates are at various stages of clinical …

The crystal structure of Abl kinase with BMS-354825, a dual SRC/ABL kinase inhibitor.

JS Tokarski, J Newitt, FY Lee, L Lombardo, R Borzilleri… - Blood, 2004 - Elsevier
Chronic myeloid leukemia (CML) is a stem cell disorder caused by a constitutively activated
tyrosine kinase, the BCR-ABL oncoprotein. Imatinib (STI571, Gleevec) is a small-molecule …

Crystal structure of the T315I mutant of Abl kinase

T Zhou, L Parillon, F Li, Y Wang, J Keats… - Chemical biology & …, 2007 - Wiley Online Library
Imatinib (Gleevec) is currently the frontline therapy for chronic myeloid leukemia (CML), a
disease characterized by the presence of a constitutively activated chimeric tyrosine kinase …

Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680

MA Young, NP Shah, LH Chao, M Seeliger, ZV Milanov… - Cancer research, 2006 - AACR
We present a high-resolution (2.0 Å) crystal structure of the catalytic domain of a mutant
form of the Abl tyrosine kinase (H396P; Abl-1a numbering) that is resistant to the Abl …

Discovery of (E)-N-(4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl) phenyl)-3-((3-(2-(pyridin-2-yl) vinyl)-1H-indazol-6-yl) thio) propanamide (CHMFL-ABL-121) …

X Liu, B Wang, C Chen, Z Jiang, C Hu, H Wu… - European Journal of …, 2018 - Elsevier
There is still a great demand in the clinic for the drugs which can overcome a variety of
imatinib resistant ABL mutants. Starting from a type I inhibitor axitinib, which has been …

Direct binding assay for the detection of type IV allosteric inhibitors of Abl

R Schneider, C Becker, JR Simard… - Journal of the …, 2012 - ACS Publications
Abelson (Abl) tyrosine kinase is an important cellular enzyme that is rendered constitutively
active in the breakpoint cluster region (BCR)-Abl fusion protein, contributing to several forms …

The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants

JS Tokarski, JA Newitt, CYJ Chang, JD Cheng… - Cancer research, 2006 - AACR
Chronic myeloid leukemia (CML) is caused by the constitutively activated tyrosine kinase
breakpoint cluster (BCR)-ABL. Current frontline therapy for CML is imatinib, an inhibitor of …