ArticleACS chemical biology2013
Structure-guided inhibitor design expands the scope of analog-sensitive kinase technology.
Article in ACS chemical biology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 58 citations in OpenAlex.
- Bulky PP1 analogs exert cellular effects independently from analog-sensitive kinase inhibition.Frontiers in chemistry · 2026Article
- A stress-responsive p38 signaling axis in choanoflagellates.RSC chemical biology · 2025Article
- MAPK Cascades in Plant Microbiota Structure and Functioning.Journal of microbiology (Seoul, Korea) · 2024Review
- Eph receptors and ephrins in cancer progression.Nature reviews. Cancer · 2024Review
- Photoswitchable Inhibitors to Optically Control Specific Kinase Activity.ACS chemical biology · 2023Article
- Strategy toward Kinase-Selective Drug Discovery.Journal of chemical theory and computation · 2023Article
- CDK9 and PP2A regulate RNA polymerase II transcription termination and coupled RNA maturation.EMBO reports · 2022Article
- Reactivity-based chemical-genetic study of protein kinases.RSC medicinal chemistry · 2022Review
- How ATP-Competitive Inhibitors Allosterically Modulate Tyrosine Kinases That Contain a Src-like Regulatory Architecture.ACS chemical biology · 2020Article
- CDK12 Activity-Dependent Phosphorylation Events in Human Cells.Biomolecules · 2019Article
- Leveraging Atropisomerism to Obtain a Selective Inhibitor of RET Kinase with Secondary Activities toward EGFR Mutants.ACS chemical biology · 2019Article
- Phosphoregulation of the oncogenic protein regulator of cytokinesis 1 (PRC1) by the atypical CDK16/CCNY complex.Experimental & molecular medicine · 2019Article
- The Bump-and-Hole Tactic: Expanding the Scope of Chemical Genetics.Cell chemical biology · 2018Review
- Reduction of protein kinase A-mediated phosphorylation of ATXN1-S776 in Purkinje cells delays onset of Ataxia in a SCA1 mouse model.Neurobiology of disease · 2018Article
- Enantioselective Synthesis of Pyrrolopyrimidine Scaffolds through Cation-Directed Nucleophilic Aromatic Substitution.Organic letters · 2018Article
- Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.Bioorganic & medicinal chemistry · 2018Article
- Inhibition of Calcium Dependent Protein Kinase 1 (CDPK1) by Pyrazolopyrimidine Analogs Decreases Establishment and Reoccurrence of Central Nervous System Disease by Toxoplasma gondii.Journal of medicinal chemistry · 2017Article
- A Chemical-Genetic Approach to Generate Selective Covalent Inhibitors of Protein Kinases.ACS chemical biology · 2017Article
- A Chemical Probe Strategy for Interrogating Inhibitor Selectivity Across the MEK Kinase Family.ACS chemical biology · 2017Article
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Authors and funding
8 authors at 5 institutions in 1 country.
Funding
Abstract
Engineered analog-sensitive (AS) protein kinases have emerged as powerful tools for dissecting phospho-signaling pathways, for elucidating the cellular function of individual kinases, and for deciphering unanticipated effects of clinical therapeutics. A crucial and necessary feature of this technology is a bioorthogonal small molecule that is innocuous toward native cellular systems but potently inhibits the engineered kinase. In order to generalize this method, we sought a molecule capable of targeting divergent AS-kinases. Here we employ X-ray crystallography and medicinal chemistry to unravel the mechanism of current inhibitors and use these insights to design the most potent, selective, and general AS-kinase inhibitors reported to date. We use large-scale kinase inhibitor profiling to characterize the selectivity of these molecules as well as examine the consequences of potential off-target effects in chemical genetic experiments. The molecules reported here will serve as powerful tools in efforts to extend AS-kinase technology to the entire kinome and the principles discovered may help in the design of other engineered enzyme/ligand pairs.
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Registered trials
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.