c‐Abl tyrosine kinase regulates neutrophil crawling behavior under fluid shear stress via Rac/PAK/LIMK/cofilin signaling axis
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Cellular Biochemistry"
DOI: 10.1002/jcb.26453
Abstract: The excessive recruitment and improper activation of polymorphonuclear neutrophils (PMNs) often induces serious injury of host tissues, leading to inflammatory disorders. Therefore, to understand the molecular mechanism on neutrophil recruitment possesses essential pathological and physiological… read more here.
Keywords: abl kinase; kinase; shear stress; cofilin signaling ... See more keywords
Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112710
Abstract: Breakpoint cluster region-Abelson (Bcr-Abl) kinase is a key driver in the pathophysiology of chronic myelogenous leukemia (CML). Broadening the chemical diversity of Bcr-Abl kinase inhibitors with novel chemical entities possessing favorable target potency and cellular… read more here.
Keywords: target; bcr abl; activity; abl kinase ... See more keywords
Imatinib can act as an allosteric activator of Abl kinase.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of molecular biology"
DOI: 10.1016/j.jmb.2021.167349
Abstract: Imatinib is an ATP-competitive inhibitor of Bcr-Abl kinase and the first drug approved for chronic myelogenous leukemia (CML) treatment. Here we show that imatinib binds to a secondary, allosteric site located in the myristoyl pocket… read more here.
Keywords: allosteric pocket; kinase; imatinib; abl kinase ... See more keywords
Discovery of a Candidate Containing an (S)-3,3-Difluoro-1-(4-methylpiperazin-1-yl)-2,3-dihydro-1H-inden Scaffold as a Highly Potent Pan-Inhibitor of the BCR-ABL Kinase Including the T315I-Resistant Mutant for the Treatment of Chronic Myeloid Leukemia.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00082
Abstract: BCR-ABL kinase inhibition is an effective strategy for the treatment of chronic myeloid leukemia (CML). Herein, we report compound 3a-P1, bearing a difluoro-indene scaffold, as a novel potent pan-inhibitor against BCR-ABL mutants, including the most… read more here.
Keywords: bcr; abl kinase; bcr abl; t315i ... See more keywords
c-Abl kinase regulates neutrophil extracellular trap formation and lung injury in abdominal sepsis
Sign Up to like & getrecommendations! Published in 2021 at "Laboratory Investigation"
DOI: 10.1038/s41374-021-00683-6
Abstract: Sepsis is associated with exaggerated neutrophil responses although mechanisms remain elusive. The aim of this study was to investigate the role of c-Abelson (c-Abl) kinase in neutrophil extracellular trap (NET) formation and inflammation in septic… read more here.
Keywords: sepsis; abl kinase; kinase; formation ... See more keywords
In silico design and computational evaluation of novel 2-arylaminopyrimidine-based compounds as potential multi-targeted protein kinase inhibitors: application for the native and mutant (T315I) Bcr-Abl tyrosine kinase
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2022.2062784
Abstract: Abstract An integrated computational approach to drug discovery was used to identify novel potential inhibitors of the native and mutant (T315I) Bcr-Abl tyrosine kinase, the enzyme playing a key role in the pathogenesis of chronic… read more here.
Keywords: mutant t315i; kinase; native mutant; t315i bcr ... See more keywords
Conformational states dynamically populated by a kinase determine its function
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DOI: 10.1126/science.abc2754
Abstract: A moving target Abl kinase is an important signaling protein that is dysregulated in leukemia and other cancers and is the target of inhibitors such as imatinib. Like other kinases, Abl kinase is dynamic, and… read more here.
Keywords: inactive states; abl kinase; kinase; conformational states ... See more keywords
Mapping the conformational energy landscape of Abl kinase using ClyA nanopore tweezers
Sign Up to like & getrecommendations! Published in 2022 at "Nature Communications"
DOI: 10.21203/rs.3.rs-1153833/v1
Abstract: Protein kinases play central roles in cellular regulation by catalyzing the phosphorylation of target proteins. Kinases have inherent structural flexibility allowing them to switch between active and inactive states. Quantitative characterization of kinase conformational dynamics… read more here.
Keywords: energy landscape; nanopore tweezers; kinase; abl kinase ... See more keywords