ArticleBioorganic & medicinal chemistry letters2013
Identification of potent Yes1 kinase inhibitors using a library screening approach.
Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 35 citations in OpenAlex.
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- Identification of a novel spirocyclic Nek2 inhibitor using high throughput virtual screening.Bioorganic & medicinal chemistry letters · 2023Article
- Structure-activity relationship studies and bioactivity evaluation of 1,2,3-triazole containing analogues as a selective sphingosine kinase-2 inhibitors.European journal of medicinal chemistry · 2020Article
- A quantitative trait locus on chromosome 2 was identified that accounts for a substantial proportion of phenotypic variance of the yellow plumage color in chicken.Poultry science · 2020Article
- How polypharmacologic is each chemogenomics library?Future drug discovery · 2020Article
- TYRO3: A potential therapeutic target in cancer.Experimental biology and medicine (Maywood, N.J.) · 2019Review
- SPVec: A Word2vec-Inspired Feature Representation Method for Drug-Target Interaction Prediction.Frontiers in chemistry · 2019Article
- Targeting loss of the Hippo signaling pathway inOncotarget · 2018Article
- An iterative compound screening contest method for identifying target protein inhibitors using the tyrosine-protein kinase Yes.Scientific reports · 2017Article
- Applications of chemogenomic library screening in drug discovery.Nature reviews. Drug discovery · 2017Review
- The metabolic waste ammonium regulates mTORC2 and mTORC1 signaling.Scientific reports · 2017Article
- Identifying and Analyzing Novel Epilepsy-Related Genes Using Random Walk with Restart Algorithm.BioMed research international · 2017Article
- Identification of Novel Plasmodium falciparum Hexokinase Inhibitors with Antiparasitic Activity.Antimicrobial agents and chemotherapy · 2016Article
- A phosphotyrosine switch regulates organic cation transporters.Nature communications · 2016Article
- Bioluminescence Methods for Assaying Kinases in Quantitative High-Throughput Screening (qHTS) Format Applied to Yes1 Tyrosine Kinase, Glucokinase, and PI5P4Kα Lipid Kinase.Methods in molecular biology (Clifton, N.J.) · 2016Article
- Identification of potential inhibitors based on compound proposal contest: Tyrosine-protein kinase Yes as a target.Scientific reports · 2015Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
Abstract
Yes1 kinase has been implicated as a potential therapeutic target in a number of cancers including melanomas, breast cancers, and rhabdomyosarcomas. Described here is the development of a robust and miniaturized biochemical assay for Yes1 kinase that was applied in a high throughput screen (HTS) of kinase-focused small molecule libraries. The HTS provided 144 (17% hit rate) small molecule compounds with IC₅₀ values in the sub-micromolar range. Three of the most potent Yes1 inhibitors were then examined in a cell-based assay for inhibition of cell survival in rhabdomyosarcoma cell lines. Homology models of Yes1 were generated in active and inactive conformations, and docking of inhibitors supports binding to the active conformation (DFG-in) of Yes1. This is the first report of a large high throughput enzymatic activity screen for identification of Yes1 kinase inhibitors, thereby elucidating the polypharmacology of a variety of small molecules and clinical candidates.
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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.