Results 121 to 130 of about 3,327,333 (431)

Identification of Quinazolinone Analogs Targeting CDK5 Kinase Activity and Glioblastoma Cell Proliferation

open access: yesFrontiers in Chemistry, 2020
CDK5/p25 kinase plays a major role in neuronal functions, and is hyperactivated in several human cancers including glioblastoma and neurodegenerative pathologies such as Alzheimer's and Parkinson's.
Marion Peyressatre   +7 more
doaj   +1 more source

On‐treatment dynamics of circulating extracellular vesicles in the first‐line setting of patients with advanced non‐small cell lung cancer: the LEXOVE prospective study

open access: yesMolecular Oncology, EarlyView.
The LEXOVE prospective study evaluated plasma cell‐free extracellular vesicle (cfEV) dynamics using Bradford assay and dynamic light scattering in metastatic non‐small cell lung cancer patients undergoing first‐line treatments, correlating a ∆cfEV < 20% with improved median progression‐free survival in responders versus non‐responders.
Valerio Gristina   +17 more
wiley   +1 more source

Giant Hub Src and Syk Tyrosine Kinase Thermodynamic Profiles Recapitulate Evolution [PDF]

open access: yes, 2016
Thermodynamic scaling theory, previously applied mainly to small proteins, here analyzes quantitative evolution of the titled functional network giant hub enzymes. The broad domain structure identified homologically is confirmed hydropathically using amino acid sequences only.
arxiv   +1 more source

1,2,6-thiadiazinones as novel narrow spectrum calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) inhibitors [PDF]

open access: yes, 1983
We demonstrate for the first time that 4H-1,2,6-thiadiazin-4-one (TDZ) can function as a chemotype for the design of ATP-competitive kinase inhibitors. Using insights from a co-crystal structure of a 3,5-bis(arylamino)-4H-1,2,6-thiadiazin-4-one bound to ...
Asquith, Christopher R.M.   +11 more
core   +3 more sources

Differential regulation of anti-inflammatory genes by p38 MAP kinase and MAP kinase kinase 6. [PDF]

open access: yes, 2014
BackgroundConventional p38α inhibitors have limited efficacy in rheumatoid arthritis, possibly because p38 blockade suppresses the counter-regulatory mechanisms that limit inflammation.
Boyle, David L   +3 more
core   +3 more sources

Kinase-targeted cancer therapies: progress, challenges and future directions

open access: yesMolecular Cancer, 2018
The human genome encodes 538 protein kinases that transfer a γ-phosphate group from ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with human cancer initiation and progression.
Khushwant S. Bhullar   +6 more
semanticscholar   +1 more source

Targeting rapid TKI‐induced AXL upregulation overcomes adaptive ERK reactivation and exerts antileukemic effects in FLT3/ITD acute myeloid leukemia

open access: yesMolecular Oncology, EarlyView.
Adaptive ERK reactivation hinders FLT3 tyrosine kinase inhibitor (TKI) treatment in FLT3/ITD acute myeloid leukemia. Here, we report that FLT3 TKI treatment rapidly induces AXL expression and upregulation that is temporally associated with the adaptive ERK reactivation.
Tessa S. Seale   +9 more
wiley   +1 more source

Systematic screening for potential therapeutic targets in osteosarcoma through a kinome-wide CRISPR-Cas9 library

open access: yesCancer Biology & Medicine, 2020
Objective: Osteosarcoma is the most common primary malignant bone tumor. However, the survival of patients with osteosarcoma has remained unchanged during the past 30 years, owing to a lack of efficient therapeutic targets.
Yuanzhong Wu   +6 more
doaj   +1 more source

The dynamic switch mechanism that leads to activation of LRRK2 is embedded in the DFGψ motif in the kinase domain. [PDF]

open access: yes, 2019
Leucine-rich repeat kinase 2 (LRRK2) is a large multidomain protein, and LRRK2 mutants are recognized risk factors for Parkinson's disease (PD). Although the precise mechanisms that control LRRK2 regulation and function are unclear, the importance of the
Boassa, Daniela   +7 more
core  

Mechanism of regulation of Raf-1 by Ca2+/Calmodulin-dependent kinase II [PDF]

open access: yes, 2011
The calcium-calmodulin dependent kinase II (CaMKII) is an ubiquitous serine/threonine protein kinase involved in multiple signalings and biological functions.
Salzano, Marcella
core   +1 more source

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