Results 321 to 330 of about 2,154,176 (393)

Non-kinase targets of protein kinase inhibitors

Nature Reviews Drug Discovery, 2017
Kinome-wide profiling platforms have comprehensively identified the relevant kinases that are targeted by numerous protein kinase inhibitors. However, recent projects have begun to discover non-kinase targets of kinase inhibitors. These non-kinase targets can contribute to the desired or undesired activities of inhibitors, or act as silent bystanders ...
L. Munoz
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Irreversible Protein Kinase Inhibitors

Current Medicinal Chemistry, 2011
Targeting cancer with small molecule irreversible inhibitors of kinases represents an emerging challenge in drug discovery. Irreversible inhibitors bind to kinase active site in a covalent and irreversible form, most frequently by reacting with a nucleophilic cysteine residue, located near the ATP binding pocket.
GARUTI, LAURA, ROBERTI, MARINELLA, BOTTEGONI, GIOVANNI   +2 more
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Protein Kinase Inhibitors

2014
The article contains sections titled: 1. Introduction 2. Approved Kinase Inhibitors and Their Syntheses 3.
A. Kleemann
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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

Benzimidazole‐based protein kinase inhibitors: Current perspectives in targeted cancer therapy

Chemical Biology and Drug Design, 2022
Targeted therapy has emerged to be the cornerstone of advanced cancer treatment, allowing for more selectivity and avoiding the common drug toxicity and resistance.
Alaa M Ali, Samar S. Tawfik, Amany S. Mostafa, M. Massoud   +3 more
semanticscholar   +1 more source

Protein kinase C inhibitors

Current Oncology Reports, 2002
Protein kinase C (PKC) is a family of serine-threonine protein kinases that are involved in signal transduction pathways that regulate growth factor response, proliferation, and apoptosis. Its central role in these processes, which are closely involved in tumor initiation, progression, and response to antitumor agents, makes it an attractive ...
Helen C, Swannie, Stanley B, Kaye
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Protein kinase inhibitors in melanoma

Expert Opinion on Pharmacotherapy, 2013
The most commonly mutated oncogene identified to date in melanoma is BRAF (∼ 50%), an upstream mediator of the mitogen-activated protein kinase (MAPK) pathway. Recently, BRAF-kinase inhibitors as well as MEK-kinase inhibitors were introduced into the clinics.Substantial Phase II and III clinical trials were searched in patients with advanced melanoma ...
Thomas K, Eigentler, Friedegund, Meier, Claus, Garbe   +2 more
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Therapeutic Protein Kinase Inhibitors

Cellular and Molecular Life Sciences, 2008
Protein kinase inhibitors represent an important and still emerging class of targeted therapeutic agents. Drug discovery and development strategies have explored numerous approaches to target the inhibition of protein kinase signaling. This review will highlight some of the strategies that have led to the successful clinical development of therapeutic ...
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JAK Protein Kinase Inhibitors

Drug News & Perspectives, 2005
In humans, the Janus protein tyrosine kinase family (JAKs) contains four members: JAK1, JAK2, JAK3 and TYK2. JAKs phosphorylate signal transducers and activators of transcription (STATs) simultaneously with other phosphorylations required for activation, and there are several cellular mechanisms in place to inhibit JAK/STAT signaling. That one might be
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