ArticleCell reports2016
Kinase Inhibitor Profiling Reveals Unexpected Opportunities to Inhibit Disease-Associated Mutant Kinases.
Article in Cell reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
24 citing papers in PubMed, 44 citations in OpenAlex.
- Comprehensive profiling of clinically approved kinase inhibitors reveals mutation-specific inhibitors and opportunities for drug repurposing.Nature biotechnology · 2026Article
- Drug screening in 3D microtumors reveals DDR1/2-MAPK12-GLI1 as a vulnerability in cancer-associated fibroblasts.Cell reports. Medicine · 2025Article
- Bosutinib-Induced Pleural Effusion-Class Effect and Cross-Intolerance to All Tyrosine Kinase Inhibitors.Hematology reports · 2025Article
- A potent MAPK13-14 inhibitor prevents airway inflammation and mucus production.American journal of physiology. Lung cellular and molecular physiology · 2023Article
- A potent MAPK13-14 inhibitor prevents airway inflammation and mucus production.bioRxiv : the preprint server for biology · 2023Article
- Artificial intelligence to guide precision anticancer therapy with multitargeted kinase inhibitors.BMC cancer · 2022Article
- Adaptive chromatin remodeling and transcriptional changes of the functional kinome in tumor cells in response to targeted kinase inhibition.The Journal of biological chemistry · 2022Review
- Repurposing existing therapeutics, its importance in oncology drug development: Kinases as a potential target.British journal of clinical pharmacology · 2022Review
- Utilizing preclinical models to develop targeted therapies for rare central nervous system cancers.Neuro-oncology · 2021Review
- Is Structure-Based Drug Design Ready for Selectivity Optimization?Journal of chemical information and modeling · 2020Article
- Inhibitors of BRAF dimers using an allosteric site.Nature communications · 2020Article
- Non-linear Deep Neural Network for Rapid and Accurate Prediction of Phenotypic Responses to Kinase Inhibitors.iScience · 2020Article
- The kinase polypharmacology landscape of clinical PARP inhibitors.Scientific reports · 2020Article
- A combined computational and experimental strategy identifies mutations conferring resistance to drugs targeting the BCR-ABL fusion protein.Communications biology · 2020Article
- Phenotypic proteomic profiling identifies a landscape of targets for circadian clock-modulating compounds.Life science alliance · 2019Article
- Are peptides a solution for the treatment of hyperactivated JAK3 pathways?Inflammopharmacology · 2019Review
- Structural Insights into Characterizing Binding Sites in Epidermal Growth Factor Receptor Kinase Mutants.Journal of chemical information and modeling · 2019Article
- KInhibition: A Kinase Inhibitor Selection Portal.iScience · 2018Article
- CAR-T cells and combination therapies: What's next in the immunotherapy revolution?Pharmacological research · 2018Article
- The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer.Best practice & research. Clinical endocrinology & metabolism · 2017Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Small-molecule kinase inhibitors have typically been designed to inhibit wild-type kinases rather than the mutant forms that frequently arise in diseases such as cancer. Mutations can have serious clinical implications by increasing kinase catalytic activity or conferring therapeutic resistance. To identify opportunities to repurpose inhibitors against disease-associated mutant kinases, we conducted a large-scale functional screen of 183 known kinase inhibitors against 76 recombinant mutant kinases. The results revealed lead compounds with activity against clinically important mutant kinases, including ALK, LRRK2, RET, and EGFR, as well as unexpected opportunities for repurposing FDA-approved kinase inhibitors as leads for additional indications. Furthermore, using T674I PDGFRα as an example, we show how single-dose screening data can provide predictive structure-activity data to guide subsequent inhibitor optimization. This study provides a resource for the development of inhibitors against numerous disease-associated mutant kinases and illustrates the potential of unbiased profiling as an approach to compound-centric inhibitor development.
Indexed as
Identifiers
What OpenQuestion holds
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.