ArticleBioorganic & medicinal chemistry letters2009
Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening.
Article in Bioorganic & medicinal chemistry letters, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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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
20 citing papers in PubMed.
- Pharmacophore Modeling of Janus Kinase Inhibitors: Tools for Drug Discovery and Exposition Prediction.Molecules (Basel, Switzerland) · 2025Article
- Bruton tyrosine kinase inhibitors for multiple sclerosis.Nature reviews. Neurology · 2023Review
- The JAK2 pathway is activated in idiopathic pulmonary fibrosis.Respiratory research · 2018Article
- A Novel Selective JAK2 Inhibitor Identified Using Pharmacological Interactions.Frontiers in pharmacology · 2018Article
- How Does the L884P Mutation Confer Resistance to Type-II Inhibitors of JAK2 Kinase: A Comprehensive Molecular Modeling Study.Scientific reports · 2017Article
- Article
- The Jak2 small molecule inhibitor, G6, reduces the tumorigenic potential of T98G glioblastoma cells in vitro and in vivo.PloS one · 2014Article
- The small molecule inhibitor G6 significantly reduces bone marrow fibrosis and the mutant burden in a mouse model of Jak2-mediated myelofibrosis.The American journal of pathology · 2012Article
- Identification of novel SAR properties of the Jak2 small molecule inhibitor G6: significance of the para-hydroxyl orientation.Bioorganic & medicinal chemistry letters · 2012Article
- A46, a benzothiophene-derived compound, suppresses Jak2-mediated pathologic cell growth.Experimental hematology · 2012Article
- The Jak2 inhibitor, G6, alleviates Jak2-V617F-mediated myeloproliferative neoplasia by providing significant therapeutic efficacy to the bone marrow.Neoplasia (New York, N.Y.) · 2011Article
- Cell death induced by the Jak2 inhibitor, G6, correlates with cleavage of vimentin filaments.Biochemistry · 2011Article
- Using free energy of binding calculations to improve the accuracy of virtual screening predictions.Journal of chemical information and modeling · 2011Article
- The use of structural biology in Janus kinase targeted drug discovery.Current drug targets · 2011Review
- The stilbenoid tyrosine kinase inhibitor, G6, suppresses Jak2-V617F-mediated human pathological cell growth in vitro and in vivo.The Journal of biological chemistry · 2011Article
- Structural determinants of PERK inhibitor potency and selectivity.Chemical biology & drug design · 2010Article
- The constitutive activation of Jak2-V617F is mediated by a π stacking mechanism involving phenylalanines 595 and 617.Biochemistry · 2010Article
- Comprehensive structural and functional characterization of the human kinome by protein structure modeling and ligand virtual screening.Journal of chemical information and modeling · 2010Article
- Structure-function correlation of G6, a novel small molecule inhibitor of Jak2: indispensability of the stilbenoid core.The Journal of biological chemistry · 2010Article
- The recent medicinal chemistry development of Jak2 tyrosine kinase small molecule inhibitors.Current medicinal chemistry · 2010Review
Corrections and comments
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Authors and funding
12 authors.
Funding
Abstract
Janus kinase 2 (JAK2) plays a crucial role in the pathomechanism of myeloproliferative disorders and hematologic malignancies. A somatic mutation of JAK2 (Val617Phe) was previously shown to occur in 98% of patients with polycythemia vera and 50% of patients with essential thrombocythemia and primary myelofibrosis. Thus, effective JAK2 kinase inhibitors may be of significant therapeutic importance. Here, we applied a structure-based virtual screen to identify novel JAK2 inhibitors. One JAK2 inhibitor in particular, G6, demonstrated remarkable potency as well as specificity, which makes it as a potential lead candidate against diseases related to elevated JAK2 tyrosine kinase activity.
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Registered trials
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