ArticleJournal of medicinal chemistry2021
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof.
Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers, 1 of them a synthesis that pooled it.
What it found
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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
53 citing papers in PubMed, 1 synthesis or guideline pooled it, 106 citations in OpenAlex.
- Pharmacokinetics and Pharmacodynamics of Ruxolitinib: A Review.Clinical pharmacokinetics · 2023Pooled it
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- Unc-51 like kinase 3 (ULK3) contributes to autophagy and cell survival in multiple myeloma.Nature communications · 2026Article
- Identification of Novel Small-Molecule Janus Kinase 1 and 2 Inhibitors Through Structure-Based Virtual Screening,ACS omega · 2026Article
- Design and synthesis of pyrrolo[2,3-d]pyrimidine linked diazospiro and piperazine - piperidine libraries as anticancer agents.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Article
- Enantioselective Pyrazole Alkylation via Iridium and Squaramide Catalyzed N-H Insertion.Journal of the American Chemical Society · 2026Article
- FMOPhore for hotspot identification and efficient fragment-to-lead growth strategies.Nature communications · 2026Article
- Deciphering the molecular mechanism of sesamol in inflammatory bowel disease through an integrative computational and biological evaluation of the JAK1 signalling pathway.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Assessment of flonoltinib maleate versus ruxolitinib phosphate in intermediate- to high-risk myelofibrosis (FMF-02): study protocol for a multicenter, randomized, open-label phase IIB trial.Therapeutic advances in hematology · 2026Article
- Stability-Driven Pose Prediction and Ligand Design via Contact Persistence Analysis from Molecular Dynamics Simulations.Computational and structural biotechnology journal · 2026Article
- Revisiting Janus kinases as molecular drug targets for rheumatic diseases.Frontiers in medicine · 2026Review
- Identification of Novel JAK2 Inhibitors from Amino Derivatives of Epoxyalantolactone: In Silico and In Vitro Studies.International journal of molecular sciences · 2025Article
- Consensus Virtual Screening andACS omega · 2025Article
- Targeting JAK2 with a multifunctional nanoinhibitor for long-lasting anti-inflammatory effects and bone repair.Journal of nanobiotechnology · 2025Article
- Exploring the macrocyclic chemical space for heuristic drug design with deep learning models.Communications chemistry · 2025Article
- Combination of ligand‑based and structure‑based virtual screening for the discovery of novel Janus kinase 2 inhibitors against philadelphia-negative myeloproliferative neoplasms.Molecular diversity · 2025Article
- Suppressing protein damage response to overcome multidrug resistance in cancer therapy.Cell discovery · 2025Article
- An Interpretable Deep Learning and Molecular Docking Framework for Repurposing Existing Drugs as Inhibitors of SARS-CoV-2 Main Protease.Molecules (Basel, Switzerland) · 2025Article
- Targeting Intracellular Pathways in Atopic Dermatitis with Small Molecule Therapeutics.Current issues in molecular biology · 2025Review
- Pharmacophore Modeling of Janus Kinase Inhibitors: Tools for Drug Discovery and Exposition Prediction.Molecules (Basel, Switzerland) · 2025Article
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
Abstract
The discovery that aberrant activity of Janus kinase 2 (JAK2) is a driver of myeloproliferative neoplasms (MPNs) has led to significant efforts to develop small molecule inhibitors for this patient population. Ruxolitinib and fedratinib have been approved for use in MPN patients, while baricitinib, an achiral analogue of ruxolitinib, has been approved for rheumatoid arthritis. However, structural information on the interaction of these therapeutics with JAK2 remains unknown. Here, we describe a new methodology for the large-scale production of JAK2 from mammalian cells, which enabled us to determine the first crystal structures of JAK2 bound to these drugs and derivatives thereof. Along with biochemical and cellular data, the results provide a comprehensive view of the shape complementarity required for chiral and achiral inhibitors to achieve highest activity, which may facilitate the development of more effective JAK2 inhibitors as therapeutics.
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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 Socratic graph.