ArticleNature communications2024
High-resolution cryo-EM of the human CDK-activating kinase for structure-based drug design.
Article in Nature communications, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
What it found
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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.
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Who cites it
32 citing papers in PubMed, 44 citations in OpenAlex.
- Structural basis for P-TEFb association with BRD4.bioRxiv : the preprint server for biology · 2026Article
- Cyclins and Cyclin-Dependent Kinases: Structure, Biological Functions, and Innovative Targeting Strategies in Cancer.MedComm · 2026Review
- Convergence of cryo-electron microscopy and artificial intelligence in integrative structural biology: A critical review of advances, synergies, and implications for molecular biophysics and drug discovery.Journal of microscopy · 2026Review
- Targeting CDKs in the RNAPII transcription cycle.Nature reviews. Drug discovery · 2026Review
- Beyond structure: spectroscopic imaging in cryogenic electron microscopy.Current opinion in structural biology · 2026Review
- FAIMS-GPF XL-MS: crosslinking-mass spectrometry based on gas-phase fractionation.Nature communications · 2026Article
- Atomic resolution cryo-EM at 200 keV.IUCrJ · 2026Article
- CryoWriter: a robotic solution for improved Cryo-EM grid preparation.Nature communications · 2026Article
- First GC/MS Profiling and Cytotoxic Evaluation of Physalis acutifolia (Solanaceae) Essential Oils: Insights From Molecular Docking and ADME Predictions.Chemistry & biodiversity · 2026Article
- Cryo-EM structures of the CDK11-cyclin L-SAP30BP complex reveal mechanisms of CDK11 regulation.Nature communications · 2026Article
- Developments and challenges in hit progression within fragment-based drug discovery.Nature communications · 2026Review
- CDK7 as a Target for Docking Screens.Methods in molecular biology (Clifton, N.J.) · 2026Article
- Molecular basis of XPF-ERCC1 targeting to SLX4-dependent DNA repair pathways.Nature communications · 2025Article
- Structural basis of undecaprenyl phosphate glycosylation leading to polymyxin resistance in Gram-negative bacteria.Nature communications · 2025Article
- Transcriptome-conditioned molecule generation via gene interaction-aware fragment modeling with a GPT-based architecture.Scientific reports · 2025Article
- Novel Pyrazolo [1,5-a]-1,3,5-Triazine Derivatives as CDK7 Inhibitors: Synthesis and Biological Insights in Pancreatic Ductal Adenocarcinoma Models.ChemMedChem · 2025Article
- Sub-3 Å resolution protein structure determination by single-particle cryo-EM at 100 keV.Structure (London, England : 1993) · 2025Article
- An experimental proxy of water displaceability for ligand discovery.Nature methods · 2025Article
- Article
- Target Engagement Assays in Early Drug Discovery.Journal of medicinal chemistry · 2025Review
Corrections and comments
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Authors and funding
13 authors at 5 institutions in 3 countries.
Funding
Abstract
Rational design of next-generation therapeutics can be facilitated by high-resolution structures of drug targets bound to small-molecule inhibitors. However, application of structure-based methods to macromolecules refractory to crystallization has been hampered by the often-limiting resolution and throughput of cryogenic electron microscopy (cryo-EM). Here, we use high-resolution cryo-EM to determine structures of the CDK-activating kinase, a master regulator of cell growth and division, in its free and nucleotide-bound states and in complex with 15 inhibitors at up to 1.8 Å resolution. Our structures provide detailed insight into inhibitor interactions and networks of water molecules in the active site of cyclin-dependent kinase 7 and provide insights into the mechanisms contributing to inhibitor selectivity, thereby providing the basis for rational design of next-generation therapeutics. These results establish a methodological framework for the use of high-resolution cryo-EM in structure-based drug design.
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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.