Sentences with phrase «kinase domain»

The phrase "kinase domain" refers to a specific part or region of a protein called a kinase. Kinases are enzymes that help regulate and control various cellular processes by adding a phosphate group to other molecules. The kinase domain is the part of the kinase protein that carries out this phosphorylation process. It acts like a molecular machine, attaching phosphate groups to specific targets, which helps to activate or deactivate certain cellular pathways and signals. Full definition
This work, and that of colleagues Brian Druker and Novartis, led to the development of the kinase inhibitor imatinib (Gleevec) as primary therapy for chronic myelogenous leukemia (CML), and the discovery that imatinib resistance is caused by BCR - ABL kinase domain mutations.
To visualize the Phe958 to Val mutation, we used the crystal structure of the JAK1 kinase domain with CMP6 inhibitor (Figure 2C).
WEHI - 435 was obtained by analysis of the RIPK2 / ponatinib structure and the necrostatin - 1 / murine RIPK1 structure to obtain a structural face for the murine RIPK2 kinase domain (18 — 249)(Nachbur et al., 2015).
We show that TNF administration damaged the liver vascular endothelium and induced phosphorylated mixed lineage kinase domain - like (phospho - MLKL) reactivity in endothelial cells isolated from TNF / zVAD - treated WT, but not Ripk1D138N / D138N, mice.
An in silico model of the potential interaction between methotrexate and the the JAK2 kinase domain.
Kinase domain mutants of Bcr - Abl exhibit altered transformation potency, kinase activity, and substrate utilization, irrespective of sensitivity to imatinib
Dissecting specificity in the Janus kinases: the structures of JAK - specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains
[citation needed] In 2000 Dr. John Kuriyan determined the mechanism by which STI - 571 inhibits the Abl kinase domain.
Subjects can be enrolled from a local test result if they have any of the following FLT3 mutations: FLT3 internal tandem duplication (ITD), FLT3 tyrosine kinase domain (TKD) / D835 or FLT3 - TKD / I836.
This is due to the replacement of the myristoylated cap region, which when present induces a conformational change rendering the kinase domain inactive, with a truncated portion of the BCR protein.
The alterations comprise short internal tandem duplication (ITD) mutations located in the regulatory juxtamembrane region (JM) as well as point mutations in the second tyrosine kinase domain (TKD).
This lack of activation occurs because C - RAF lacks a constitutive charge within a motif in the kinase domain called the N - region.
The NTRK fusions involved a gene segment encoding a tyrosine kinase domain.
LabPMM, our internationally harmonized network of accredited laboratories, are the only reference laboratories that provide internationally harmonized, regulatory compliant testing for FLT3 internal tandem duplication (ITD), and Tyrosine Kinase Domain (TKD) mutations.
Here patients treated with imatinib become resistant because of the acquisition of mutations in the ABL kinase domain.13
Results While most JAK1 mutants were sensitive to ATP - competitive JAK inhibitors, mutations targeting Phe958 and Pro960 in the hinge region of the kinase domain rendered JAK1 constitutively active but also resistant to all tested JAK inhibitors.
Structural data from recently solved crystal structure of JAK1 kinase domain in complex with CPM, an ATP - competitive inhibitor (PDB 3EYH), 21 were used to analyze more precisely the impact of the kinase domain - located JAK1 mutations.
Recently, Chirieleison et al. (2016) summarized the uniqueness of RIPK2 kinase domain within the RIPK family that could not be substituted for the kinase domain from RIPK1 or RIPK4.
We also solved the first ever structures of CDPKs (from plants or parasites) with both the kinase domain and the calcium - binding domain intact.
This bound to the ATP binding pocket of the kinase domain and inhibited RIPK2 with an IC50 of 5 — 50 nM, depending on the assay.
«We figured that if there were going to be mutations that constitutively activated these enzymes, and that would thus be targetable by drugs, the kinase domains would be the ones to go for,» said Vogelstein.
The second most common mutation type in the FLT3 gene is a Tyrosine Kinase Domain (TKD) point mutation in the codon for an aspartate (D835) or an isoleucine (I836) residue that is located in the activation loop of the FLT3 protein.
The researchers first identified the kinase domains of 138 tyrosine kinases and similar enzymes from the kinome database.
Their studies revealed mutations within the kinase domains in 14 genes.
The assay identifies both internal tandem duplication (ITD) and tyrosine kinase domain (TKD) mutations, and identifies even large ITD mutations, missed using many current NGS - based assays.
«Most importantly, they were in positions of the kinase domains predicted to alter function, based on analogous mutations that have been seen before in other kinases,» he said.
To reduce the amount of gene sequencing required, they focused their search on mutations in the «kinase domain» of these enzymes, which is the region that is principally responsible for enzymatic activity.
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