ReviewMethods in enzymology2014
Targeting protein kinases with selective and semipromiscuous covalent inhibitors.
Review in Methods in enzymology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- High throughput screening of eukaryotic release factor 1 variants to enhance noncanonical amino acid incorporation.bioRxiv : the preprint server for biology · 2025Article
- Reversible covalent c-Jun N-terminal kinase inhibitors targeting a specific cysteine by precision-guided Michael-acceptor warheads.Nature communications · 2024Article
- Targeting a key protein-protein interaction surface on mitogen-activated protein kinases by a precision-guided warhead scaffold.Nature communications · 2024Article
- Bioconjugate Platform for Iterative BackboneACS catalysis · 2022Article
- Inhibiting a dynamic viral protease by targeting a non-catalytic cysteine.Cell chemical biology · 2022Article
- Development of a covalent inhibitor of gut bacterial bile salt hydrolases.Nature chemical biology · 2020Article
- Future prospects for noncanonical amino acids in biological therapeutics.Current opinion in biotechnology · 2019Review
- Regional perturbation of gene transcription is associated with intrachromosomal rearrangements and gene fusion transcripts in high grade ovarian cancer.Scientific reports · 2019Article
- The Allosteric Site on SHP2's Protein Tyrosine Phosphatase Domain is Targetable with Druglike Small Molecules.ACS omega · 2018Article
- Article
- Drug-Target Kinetics in Drug Discovery.ACS chemical neuroscience · 2018Article
- Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation.Journal of medicinal chemistry · 2017Article
- Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- The Search for Covalently Ligandable Proteins in Biological Systems.Molecules (Basel, Switzerland) · 2016Article
- Modular Synthesis of Novel Macrocycles Bearing α,β-Unsaturated Chemotypes through a Series of One-Pot, Sequential Protocols.Chemistry (Weinheim an der Bergstrasse, Germany) · 2016Article
- Automated computational screening of the thiol reactivity of substituted alkenes.Journal of computer-aided molecular design · 2015Article
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Authors and funding
2 authors.
Funding
Abstract
Protein kinase inhibitors are an important class of therapeutics. In addition, selective kinase inhibitors can often reveal unexpected biological insights, augmenting genetic approaches and playing a decisive role in preclinical target validation studies. Nevertheless, developing protein kinase inhibitors with sufficient selectivity and pharmacodynamic potency presents significant challenges. Targeting noncatalytic cysteines with covalent inhibitors is a powerful approach to address both challenges simultaneously. Here, we describe our efforts to design irreversible and reversible electrophilic inhibitors with varying degrees of kinase selectivity. Highly selective covalent inhibitors have been used to elucidate the roles of p90 ribosomal protein S6 kinases in animal models of atherosclerosis and diabetes. By contrast, semipromiscuous covalent inhibitors have revealed new therapeutic targets in disease-causing parasites and have shown utility as chemoproteomic probes for interrogating kinase occupancy in living cells.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.