ReviewJournal of enzyme inhibition and medicinal chemistry2025
FDA-approved kinase inhibitors in PROTAC design, development and synthesis.
Review in Journal of enzyme inhibition and medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 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
5 citing papers in PubMed.
- Expanding Synthetic Lethality in DNA Damage Response-Defective Cancers Through Stress Phenotype-Guided Kinase Targeting.International journal of molecular sciences · 2026Review
- Advances in the design and discovery of small-molecule tyrosine kinase inhibitors for breast cancer.RSC advances · 2026Review
- Harnessing Ribonucleoprotein Granule Biology for Cancer Therapy: The Central Role of Protein Modifications.Research (Washington, D.C.) · 2026Review
- Recent FDA-approved kinase inhibitors for cancer therapy in 2025: A comprehensive review and perspectives.EXCLI journal · 2025Review
- Molecular docking and dynamics in protein serine/threonine kinase drug discovery: advances, challenges, and future perspectives.Frontiers in pharmacology · 2025Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
FDA-approved kinase inhibitors represent a rapidly growing class of targeted therapies with proven clinical success in oncology. However, their occupancy-driven mode of action is often associated with resistance, off-target effects, and incomplete inhibition. Proteolysis-Targeting Chimaeras (PROTACs) offer a compelling alternative by promoting complete degradation of oncogenic kinases, thereby enhancing selectivity and resistance reduction. In this review, we provide a comprehensive overview of the rational design, development, and synthetic approaches for PROTACs incorporating FDA-approved kinase inhibitors. We discuss key aspects influencing degrader efficiency, including kinase selectivity, linker design, E3 ligase recruitment, and synthetic strategies. Additionally, we highlight recent advances, emerging trends, and future directions, such as expanding the repertoire of degradable kinases, optimising linker chemistry, and broadening diversity of E3 ligases. A better understanding of these factors will facilitate the continued evolution of PROTAC technology into effective next-generation therapies for kinase-driven diseases.
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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.