Results 21 to 30 of about 2,078,396 (299)

Properties of FDA-approved Small Molecule Protein Kinase Inhibitors: A 2023 Update.

Pharmacological Research, 2022
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this enzyme family has become one of the most important drug targets in the 21st century.
R. Roskoski
semanticscholar   +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

Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors.

Journal of Medicinal Chemistry, 2021
Small molecule covalent kinase inhibitors (CKIs) have entered a new era in drug discovery, which have the advantage for sustained target inhibition and high selectivity.
Xiaoyun Lu, J. Smaill, A. Patterson, Ke Ding   +3 more
semanticscholar   +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

Structural features of the protein kinase domain and targeted binding by small-molecule inhibitors

Journal of Biological Chemistry, 2022
Protein kinases are key components in cellular signaling pathways as they carry out the phosphorylation of proteins, primarily on Ser, Thr, and Tyr residues.
C. Arter, Luke Trask, Sarah J. Ward, S. Yeoh, R. Bayliss   +4 more
semanticscholar   +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