Results 11 to 20 of about 631,172 (117)

Pharmacological approaches to understanding protein kinase signaling networks

open access: yesFrontiers in Pharmacology, 2023
Protein kinases play vital roles in controlling cell behavior, and an array of kinase inhibitors are used successfully for treatment of disease. Typical drug development pipelines involve biological studies to validate a protein kinase target, followed ...
Elloise H. Stephenson   +1 more
doaj   +1 more source

Marine-derived protein kinase inhibitors for neuroinflammatory diseases

open access: yesBioMedical Engineering OnLine, 2018
Neuroinflammation is primarily characterized by overexpression of proinflammatory mediators produced by glial activation or immune cell infiltration. Several kinases have been shown to be critical mediators in neuroinflammation. One of the largest groups
Chong Ning   +6 more
doaj   +1 more source

Protein kinase inhibitors for acute leukemia

open access: yesBiomarker Research, 2018
Conventional treatments for acute leukemia include chemotherapy, radiation therapy, and intensive combined treatments (including bone marrow transplant or stem cell transplants). Novel treatment approaches are in active development.
Yuan Ling   +3 more
doaj   +1 more source

Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays. [PDF]

open access: yesPLoS ONE, 2013
A library of 367 protein kinase inhibitors, the GSK Published Kinase Inhibitor Set (PKIS), which has been annotated for protein kinase family activity and is available for public screening efforts, was assayed against the commonly used luciferase ...
Patricia Dranchak   +6 more
doaj   +1 more source

Binding of protein kinase inhibitors to synapsin I inferred from pair-wise binding site similarity measurements.

open access: yesPLoS ONE, 2010
Predicting off-targets by computational methods is getting increasing importance in early drug discovery stages. We herewith present a computational method based on binding site three-dimensional comparisons, which prompted us to investigate the cross ...
Enrico Defranchi   +5 more
doaj   +1 more source

Development of actionable targets of multi-kinase inhibitors (AToMI) screening platform to dissect kinase targets of staurosporines in glioblastoma cells

open access: yesScientific Reports, 2022
Therapeutic resistance to kinase inhibitors constitutes a major unresolved clinical challenge in cancer and especially in glioblastoma. Multi-kinase inhibitors may be used for simultaneous targeting of multiple target kinases and thereby potentially ...
Oxana V. Denisova   +10 more
doaj   +1 more source

Cytoprotective effect of the elongation factor-2 kinase-mediated autophagy in breast cancer cells subjected to growth factor inhibition. [PDF]

open access: yesPLoS ONE, 2010
Autophagy is a highly conserved and regulated cellular process employed by living cells to degrade proteins and organelles as a response to metabolic stress. We have previously reported that eukaryotic elongation factor-2 kinase (eEF-2 kinase, also known
Yan Cheng   +5 more
doaj   +1 more source

Analysis of the phosphoproteome of CK2α(–/–)/Δα′ C2C12 myoblasts compared to the wild-type cells

open access: yesOpen Biology, 2023
CK2 is a Ser/Thr protein kinase composed of two catalytic (α/α′) subunits and a non-catalytic β-subunit dimer, whose activity is often abnormally high in cancer cells.
Christian Borgo   +8 more
doaj   +1 more source

Requirement for the eIF4E binding proteins for the synergistic down-regulation of protein synthesis by hypertonic conditions and mTOR inhibition. [PDF]

open access: yesPLoS ONE, 2013
The protein kinase mammalian target of rapamycin (mTOR) regulates the phosphorylation and activity of several proteins that have the potential to control translation, including p70S6 kinase and the eIF4E binding proteins 4E-BP1 and 4E-BP2.
Michael J Clemens   +2 more
doaj   +1 more source

Identification of inactive conformation‐selective interleukin‐2‐inducible T‐cell kinase (ITK) inhibitors based on second‐harmonic generation

open access: yesFEBS Open Bio, 2018
Many clinically approved protein kinase inhibitors stabilize an inactive conformation of their kinase target. Such inhibitors are generally highly selective compared to active conformation inhibitors, and consequently, general methods to identify ...
Yoshiji Hantani   +8 more
doaj   +1 more source

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