Results 11 to 20 of about 2,154,176 (393)

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

PLoS 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, Rui Li, Joseph M Dhahbi, Amy Yamakawa, Frank Sauer   +4 more
doaj   +1 more source

Protein Kinase Inhibitors

, 2012
europepmc   +2 more sources

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

Biomolecules, 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

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

PLoS 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, Jiro Kikuchi, Yusuke Furukawa, Naoya Shibayama   +3 more
doaj   +1 more source

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

Frontiers in Chemistry, 2023
Receptor-Interacting serine/threonine-Protein Kinase 1 (RIPK1) emerged as an important driver of inflammation and, consequently, inflammatory pathologies.
Camilla Scarpellini, Sophie Valembois, Kenneth Goossens, Mike Vadi, Mike Vadi, Caroline Lanthier, Greta Klejborowska, Pieter Van Der Veken, Hans De Winter, Mathieu J. M. Bertrand, Mathieu J. M. Bertrand, Koen Augustyns   +11 more
doaj   +1 more source

The Kinase Specificity of Protein Kinase Inhibitor Peptide [PDF]

Frontiers 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

Pharmacological approaches to understanding protein kinase signaling networks

Frontiers 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, Jonathan M. G. Higgins   +1 more
doaj   +1 more source

ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system

Nature Chemical Biology, 2013
Sigrun Polier, Rahul S. Samant, Paul A. Clarke, Paul Workman, Chrisostomos Prodromou, Laurence H. Pearl   +5 more
openalex   +2 more sources

Protein kinase inhibitors for amyotrophic lateral sclerosis therapy

British Journal of Pharmacology, 2020
Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disorder that causes the progressive loss of motoneurons and, unfortunately, there is no effective treatment for this disease.
V. Palomo, Vanesa Nozal, Elisa Rojas-Prats, C. Gil, Ana Martínez   +4 more
semanticscholar   +1 more source

Protein Kinase Inhibitors

Folia Biologica, 2006
Since protein kinases have been found to be implicated in many diseases, first of all malignancies, they are considered as promising therapeutic targets. Many protein kinase inhibitors have been designed by now. These molecules have a low molecular weight and most of them bind to protein kinases competing with ATP for the ATP-binding site. Some protein
I, Shchemelinin, L, Sefc, E, Necas
openaire   +2 more sources