Combining the Allosteric Inhibitor Asciminib with Ponatinib Suppresses Emergence of and Restores Efficacy against Highly Resistant BCR-ABL1 Mutants.
Allosteric Regulation
/ drug effects
Animals
Antineoplastic Combined Chemotherapy Protocols
/ pharmacology
Binding Sites
/ drug effects
Cell Line, Tumor
/ transplantation
Disease Models, Animal
Drug Resistance, Neoplasm
/ drug effects
Female
Fusion Proteins, bcr-abl
/ antagonists & inhibitors
Humans
Imidazoles
/ pharmacology
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
/ drug therapy
Mice
Molecular Docking Simulation
Molecular Dynamics Simulation
Molecular Targeted Therapy
/ methods
Mutation
Niacinamide
/ analogs & derivatives
Primary Cell Culture
Pyrazoles
/ pharmacology
Pyridazines
/ pharmacology
ABL001
allosteric inhibitors
asciminib
chronic myeloid leukemia
compound mutation
ponatinib
targeted therapy
Journal
Cancer cell
ISSN: 1878-3686
Titre abrégé: Cancer Cell
Pays: United States
ID NLM: 101130617
Informations de publication
Date de publication:
14 10 2019
14 10 2019
Historique:
received:
11
12
2017
revised:
03
04
2019
accepted:
13
08
2019
pubmed:
24
9
2019
medline:
26
5
2020
entrez:
24
9
2019
Statut:
ppublish
Résumé
BCR-ABL1 point mutation-mediated resistance to tyrosine kinase inhibitor (TKI) therapy in Philadelphia chromosome-positive (Ph
Identifiants
pubmed: 31543464
pii: S1535-6108(19)30372-1
doi: 10.1016/j.ccell.2019.08.004
pmc: PMC6893878
mid: NIHMS1059932
pii:
doi:
Substances chimiques
BCR-ABL1 fusion protein, human
0
Imidazoles
0
Pyrazoles
0
Pyridazines
0
asciminib
0
Niacinamide
25X51I8RD4
ponatinib
4340891KFS
Fusion Proteins, bcr-abl
EC 2.7.10.2
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
431-443.e5Subventions
Organisme : NHLBI NIH HHS
ID : R01 HL082978
Pays : United States
Organisme : Howard Hughes Medical Institute
Pays : United States
Organisme : NCI NIH HHS
ID : R01 CA065823
Pays : United States
Organisme : NCI NIH HHS
ID : P01 CA049639
Pays : United States
Organisme : BLRD VA
ID : I01 BX000338
Pays : United States
Organisme : NCI NIH HHS
ID : P30 CA042014
Pays : United States
Organisme : NCI NIH HHS
ID : R01 CA178397
Pays : United States
Informations de copyright
Copyright © 2019 Elsevier Inc. All rights reserved.
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