Results 1 to 10 of about 4,002,721 (251)

Marine-derived protein kinase inhibitors for neuroinflammatory diseases

BioMedical 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, Hui-Min David Wang, Rong Gao, Yu-Chia Chang, Fengqing Hu, Xianjun Meng, Shi-Ying Huang   +6 more
doaj   +2 more sources

PKIDB: A Curated, Annotated and Updated Database of Protein Kinase Inhibitors in Clinical Trials

Molecules, 2018
The number of protein kinase inhibitors (PKIs) approved worldwide continues to grow steadily, with 39 drugs approved in the period between 2001 and January 2018.
Fabrice Carles, Stéphane Bourg, Christophe Meyer, Pascal Bonnet   +3 more
doaj   +3 more sources

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

CHIMIA, 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

BMC 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, Yen-Chao Hsu, Yi-Hsuan Chuang, Yun-Ti Chen, Xiang-Yu Lin, You-Wei Fan, Nikhil Pathak, Jinn-Moon Yang   +7 more
doaj   +1 more source

Advances in RIPK1 kinase inhibitors

Frontiers 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, Lu Chen, Xiaoqin Zhang, Yaqing Ou, Maoyu Liu, Maoyu Liu, Dongke Yu, Dongke Yu, Zhiheng Song, Lihong Niu, Lijuan Zhang, Lijuan Zhang, Jianyou Shi, Jianyou Shi   +13 more
doaj   +1 more source

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

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

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