Internal tandem duplication mutations in the tyrosine kinase domain of FLT3 display a higher oncogenic potential than the activation loop D835Y mutation
Sign Up to like & getrecommendations! Published in 2018 at "Annals of Hematology"
DOI: 10.1007/s00277-018-3245-5
Abstract: Acute myeloid leukemia (AML) remains the most common form of acute leukemia among adults and accounts for a large number of leukemia-related deaths. Mutations in FMS-like tyrosine kinase 3 (FLT3) is one of the most… read more here.
Keywords: kinase domain; flt3; domain; tyrosine kinase ... See more keywords
Expanding the search for significant EGFR mutations in NSCLC outside of the tyrosine kinase domain with next-generation sequencing
Sign Up to like & getrecommendations! Published in 2017 at "Medical Oncology"
DOI: 10.1007/s12032-017-0985-3
Abstract: While conventional organization of EGFR mutations in non-small cell lung cancer (NSCLC) includes classic lesions sensitive to tyrosine kinase inhibitors (TKI) and variants localized to the tyrosine kinase domain (TKD) in exons 18–21, next-generation sequencing… read more here.
Keywords: kinase domain; tyrosine kinase; egfr mutations; extra tkd ... See more keywords
Characteristics and outcome of chronic myeloid leukemia patients with E255K/V BCR–ABL kinase domain mutations
Sign Up to like & getrecommendations! Published in 2018 at "International Journal of Hematology"
DOI: 10.1007/s12185-018-2422-6
Abstract: Kinase domain (KD) mutations of ABL1 represent the most common resistance mechanism to tyrosine kinase inhibitors (TKI) in CML. Besides T315I, mutations in codon 255 are highly resistant mutations in vitro to all TKI. We… read more here.
Keywords: kinase domain; patients e255k; response; domain mutations ... See more keywords
Discovery and Structure-Based Optimization of Fragments Binding the Mixed Lineage Kinase Domain-like Protein Executioner Domain.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00686
Abstract: Necroptosis is a form of programmed cell death that in case of misregulation can lead to inflammatory diseases. Mixed lineage kinase domain-like protein (MLKL), the effector protein in the canonical necroptosis signaling pathway, becomes activated… read more here.
Keywords: protein; executioner domain; kinase domain; lineage kinase ... See more keywords
Identification of Inhibitors of the Schistosoma mansoni VKR2 Kinase Domain
Sign Up to like & getrecommendations! Published in 2022 at "ACS Medicinal Chemistry Letters"
DOI: 10.1021/acsmedchemlett.2c00248
Abstract: Schistosomiasis is a neglected tropical disease caused by parasitic flatworms. Current treatment relies on just one partially effective drug, praziquantel (PZQ). Schistosoma mansoni Venus Kinase Receptors 1 and 2 (SmVKR1 and SmVKR2) are important for… read more here.
Keywords: identification inhibitors; kinase domain; kinase; inhibitors schistosoma ... See more keywords
Binding Analysis of the Inositol-Requiring Enzyme 1 Kinase Domain
Sign Up to like & getrecommendations! Published in 2018 at "ACS Omega"
DOI: 10.1021/acsomega.8b01404
Abstract: Inositol-requiring enzyme 1 (IRE1) is an orchestrator of the unfolded protein response (UPR), the cellular response to endoplasmic reticulum (ER) stress that plays a crucial role in tumor development. IRE1 signaling is the most evolutionary… read more here.
Keywords: inositol requiring; kinase; kinase domain; ire1 kinase ... See more keywords
Millisecond dynamics of BTK reveal kinome-wide conformational plasticity within the apo kinase domain
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-10697-0
Abstract: Bruton tyrosine kinase (BTK) is a key enzyme in B-cell development whose improper regulation causes severe immunodeficiency diseases. Design of selective BTK therapeutics would benefit from improved, in-silico structural modeling of the kinase’s solution ensemble.… read more here.
Keywords: wide conformational; kinase; kinase domain; millisecond ... See more keywords
A pan-cancer assessment of alterations of the kinase domain of ULK1, an upstream regulator of autophagy
Sign Up to like & getrecommendations! Published in 2020 at "Scientific Reports"
DOI: 10.1038/s41598-020-71527-4
Abstract: Autophagy is a key clearance process to recycle damaged cellular components. One important upstream regulator of autophagy is ULK1 kinase. Several three-dimensional structures of the ULK1 catalytic domain are available, but a comprehensive study, including… read more here.
Keywords: upstream regulator; kinase domain; regulator autophagy; cancer ... See more keywords
Locking mixed-lineage kinase domain-like protein in its auto-inhibited state prevents necroptosis
Sign Up to like & getrecommendations! Published in 2020 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2017406117
Abstract: Significance Necroptosis is an emergency controlled cell-death mechanism, which only may be activated in case of impaired apoptosis. Necroptosis leads to unchecked release of proinflammatory cytoplasmatic content of the cells and is thereby implicated in… read more here.
Keywords: necroptosis; kinase domain; like protein; domain like ... See more keywords
Insight into the key features for ligand binding in Y1230 mutated c-Met kinase domain by molecular dynamics simulations
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2017.1340852
Abstract: c-Met kinase has been considered as an attractive target for developing antitumor agents. The strong interactions between Tyr1230 and the inhibitors emphasized its importance for ligand binding. The clinically related Tyr1230 mutations have made negative… read more here.
Keywords: kinase; kinase domain; ligand binding; met kinase ... See more keywords
Afatinib Achieved Remarkable Disease Control in a Chinese Patient With Lung Adenocarcinoma Harboring Rare EGFR Exon 18-25 Kinase Domain Duplication.
Sign Up to like & getrecommendations! Published in 2019 at "American Journal of Therapeutics"
DOI: 10.1097/mjt.0000000000001005
Abstract: To the Editor: Epidermal growth factor receptor (EGFR) mutations were first identified in non–small-cell lung cancers (NSCLCs) in 2004. Currently, because of the advances in detection techniques, such as next generation sequencing, rare or atypical… read more here.
Keywords: egfr; kinase; domain duplication; kinase domain ... See more keywords