Results 11 to 20 of about 608,807 (260)

Protein kinase inhibitors for acute leukemia [PDF]

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. Recently, protein kinase inhibitors are on clinical trials and offer hope as new drugs for acute leukemia treatment. This
Yuan Ling   +3 more
openaire   +4 more sources

The Kinase Specificity of Protein Kinase Inhibitor Peptide [PDF]

open access: yesFrontiers in Pharmacology, 2021
G-protein-coupled-receptor (GPCR) signaling is exquisitely controlled to achieve spatial and temporal specificity. The endogenous protein kinase inhibitor peptide (PKI) confines the spatial and temporal spread of the activity of protein kinase A (PKA), which integrates inputs from three major types of GPCRs.
Yao Chen, Yao Chen, Bernardo L. Sabatini
openaire   +4 more sources

Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors

open access: yesCHIMIA, 2022
Covalent inhibitors have recently seen a revival in medicinal chemistry. Inhibitors addressing non-catalytic cysteine residues with weakly reactive electrophiles have been very successfully employed to target protein kinases, one of the major druggable ...
Laura Hillebrand, Matthias Gehringer
doaj   +1 more source

Discovery of moiety preference by Shapley value in protein kinase family using random forest models

open access: yesBMC Bioinformatics, 2022
Background Human protein kinases play important roles in cancers, are highly co-regulated by kinase families rather than a single kinase, and complementarily regulate signaling pathways.
Yu-Wei Huang   +7 more
doaj   +1 more source

Advances in RIPK1 kinase inhibitors

open access: yesFrontiers in Pharmacology, 2022
Programmed necrosis is a new modulated cell death mode with necrotizing morphological characteristics. Receptor interacting protein 1 (RIPK1) is a critical mediator of the programmed necrosis pathway that is involved in stroke, myocardial infarction ...
Lu Chen   +13 more
doaj   +1 more source

Novel protein kinase signaling systems regulating lifespan identified by small molecule library screening using Drosophila. [PDF]

open access: yesPLoS ONE, 2012
Protein kinase signaling cascades control most aspects of cellular function. The ATP binding domains of signaling protein kinases are the targets of most available inhibitors. These domains are highly conserved from mammals to flies.
Stephen R Spindler   +4 more
doaj   +1 more source

Differentiating Inhibitors of Closely Related Protein Kinases with Single- or Multi-Target Activity via Explainable Machine Learning and Feature Analysis

open access: yesBiomolecules, 2022
Protein kinases are major drug targets. Most kinase inhibitors are directed against the adenosine triphosphate (ATP) cofactor binding site, which is largely conserved across the human kinome.
Christian Feldmann, Jürgen Bajorath
doaj   +1 more source

Bivalent inhibitors of protein kinases [PDF]

open access: yesCritical Reviews in Biochemistry and Molecular Biology, 2014
Protein kinases are key players in a large number of cellular signaling pathways. Dysregulated kinase activity has been implicated in a number of diseases, and members of this enzyme family are of therapeutic interest. However, due to the fact that most inhibitors interact with the highly conserved ATP-binding sites of kinases, it is a significant ...
Carrie M, Gower   +2 more
openaire   +2 more sources

Fast in-vitro screening of FLT3-ITD inhibitors using silkworm-baculovirus protein expression system.

open access: yesPLoS ONE, 2022
We report expression and purification of a FLT3 protein with ITD mutation (FLT3-ITD) with a steady tyrosine kinase activity using a silkworm-baculovirus system, and its application as a fast screening system of tyrosine kinase inhibitors.
Naoki Yamamoto   +3 more
doaj   +1 more source

From PERK to RIPK1: Design, synthesis and evaluation of novel potent and selective necroptosis inhibitors

open access: yesFrontiers in Chemistry, 2023
Receptor-Interacting serine/threonine-Protein Kinase 1 (RIPK1) emerged as an important driver of inflammation and, consequently, inflammatory pathologies.
Camilla Scarpellini   +11 more
doaj   +1 more source

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