ArticleJournal of medicinal chemistry2023
Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation.
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Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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15citing papers in PubMed
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15 citing papers in PubMed, 31 citations in OpenAlex.
- Probing pyrazolo-pyrimidines as SIRT2 inhibitorsRSC medicinal chemistry · 2026Article
- Prognostic, diagnostic and therapeutic value of the cancer tubulin code.Cancer metastasis reviews · 2026Review
- Structure-Guided Optimization and Biological Validation of 1,3,4-Thiadiazole-Based SIRT2 Inhibitors Reinforcing Channel Entrance Interactions.Drug development research · 2026Article
- Current Computational Approaches for the Discovery of Novel Anticancer Agents Targeting VEGFR and SIRT Signaling Pathways.Pharmaceutics · 2026Review
- From Pharmacophore to Warhead: NADAngewandte Chemie (International ed. in English) · 2025Article
- Imaging microtubule dynamics: A new frontier in biomarker development for neurodegenerative diseases.Alzheimer's & dementia : the journal of the Alzheimer's Association · 2025Review
- Development and Characterization of the First Selective Class IIb Histone Deacetylase Degraders.Journal of medicinal chemistry · 2025Article
- DCAF16-Based Covalent Molecular Glues for Targeted Protein Degradation of Histone Deacetylases.Archiv der Pharmazie · 2025Article
- Efficient Crystallization of Apo Sirt2 for Small-Molecule Soaking and Structural Analysis of Ligand Interactions.Journal of medicinal chemistry · 2025Article
- The Role of the Sirtuin Family Histone Deacetylases in Acute Myeloid Leukemia-A Promising Road Ahead.Cancers · 2025Review
- Recent Advancements in the Development of HDAC/Tubulin Dual-Targeting Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Histone deacetylase 6 inhibition promotes microtubule acetylation and facilitates autophagosome-lysosome fusion in dystrophin-deficient mdx mice.Acta physiologica (Oxford, England) · 2025Article
- Symmetrical 2,7-disubstituted 9H-fluoren-9-one as a novel and promising scaffold for selective targeting of SIRT2.Archiv der Pharmazie · 2024Article
- The Structures, Functions, and Roles of Class III HDACs (Sirtuins) in Neuropsychiatric Diseases.Cells · 2024Review
- Targeting Histone Deacetylases 6 in Dual-Target Therapy of Cancer.Pharmaceutics · 2023Review
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Authors and funding
24 authors at 7 institutions in 3 countries.
Laura SinatraInstitute for Drug Discovery, Medical Faculty, Leipzig University, Brüderstraße 34, 04103 Leipzig, Germany.
Anja VogelmannInstitute of Pharmaceutical Sciences, University of Freiburg, Albertstraße 25, 79104 Freiburg, Germany.
Florian FriedrichInstitute of Pharmaceutical Sciences, University of Freiburg, Albertstraße 25, 79104 Freiburg, Germany.
Margarita A TararinaRoy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104-6323, United States.ORCID 0000-0003-4750-2289
Emilia NeuwirtInstitute of Neuropathology, Medical Center-University of Freiburg, Faculty of Medicine, University of Freiburg, Breisacherstraße 64, 79106 Freiburg, Germany.ORCID 0000-0002-9747-3335
Arianna ColcerasaInstitute of Pharmaceutical Sciences, University of Freiburg, Albertstraße 25, 79104 Freiburg, Germany.
Philipp KönigDepartment of Pharmaceutical & Cell Biological Chemistry, Pharmaceutical Institute, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
Lara ToyDepartment of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-University Erlangen-Nürnberg, Nikolaus-Fiebiger-Straße 10, 91058 Erlangen, Germany.ORCID 0000-0001-6932-2217
Talha Z YesilogluDepartment of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther University of Halle-Wittenberg, Wolfgang-Langenbeck-Straße 2-4, 06120 Halle (Saale), Germany.
Sebastian HilscherDepartment of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther University of Halle-Wittenberg, Wolfgang-Langenbeck-Straße 2-4, 06120 Halle (Saale), Germany.ORCID 0009-0003-0611-7365
Lena GaitzschInstitute of Pharmaceutical Sciences, University of Freiburg, Albertstraße 25, 79104 Freiburg, Germany.ORCID 0000-0002-2084-0168
Niklas PapenkordtInstitute of Pharmaceutical Sciences, University of Freiburg, Albertstraße 25, 79104 Freiburg, Germany.ORCID 0000-0003-3420-0695
Shiyang ZhaiDepartment of Pharmaceutical & Cell Biological Chemistry, Pharmaceutical Institute, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.ORCID 0009-0005-6840-3177
Lin ZhangInstitute of Biochemistry, University of Freiburg, Albertstraße 21, 79104 Freiburg, Germany.ORCID 0000-0001-5431-5006
Christophe RomierInstitut de Génétique et de Biologie Moléculaire et Cellulaire (IGBMC), Université de Strasbourg, CNRS UMR 7104, Inserm UMR-S 1258, 1 rue Laurent Fries, F-67400 Illkirch, France.ORCID 0000-0002-3680-935X
Oliver EinsleInstitute of Biochemistry, University of Freiburg, Albertstraße 21, 79104 Freiburg, Germany.ORCID 0000-0001-8722-2893
Wolfgang SipplDepartment of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther University of Halle-Wittenberg, Wolfgang-Langenbeck-Straße 2-4, 06120 Halle (Saale), Germany.ORCID 0000-0002-5985-9261
Mike SchutkowskiDepartment of Enzymology, Charles Tanford Protein Center, Institute of Biochemistry and Biotechnology, Martin-Luther-University Halle-Wittenberg, 06120 Halle, Germany.ORCID 0000-0003-0919-7076
Olaf GrossInstitute of Neuropathology, Medical Center-University of Freiburg, Faculty of Medicine, University of Freiburg, Breisacherstraße 64, 79106 Freiburg, Germany.
Gerd BendasDepartment of Pharmaceutical & Cell Biological Chemistry, Pharmaceutical Institute, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.ORCID 0000-0002-8667-7201
David W ChristiansonRoy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104-6323, United States.ORCID 0000-0002-0194-5212
Finn K HansenInstitute for Drug Discovery, Medical Faculty, Leipzig University, Brüderstraße 34, 04103 Leipzig, Germany.ORCID 0000-0001-9765-5975
Manfred JungInstitute of Pharmaceutical Sciences, University of Freiburg, Albertstraße 25, 79104 Freiburg, Germany.ORCID 0000-0002-6361-7716
Matthias SchiedelDepartment of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-University Erlangen-Nürnberg, Nikolaus-Fiebiger-Straße 10, 91058 Erlangen, Germany.ORCID 0000-0001-7365-3617
University of Freiburg · DEMartin Luther University Halle-Wittenberg · DEUniversity of Bonn · DEFriedrich-Alexander-Universität Erlangen-Nürnberg · DEUniversity of Pennsylvania · USCentre National de la Recherche Scientifique · FRLeipzig University · DE
Funding
X-ray Scattering Technology CoreP30GM133893 · NIGMS · BROOKHAVEN SCIENCE ASSOC-BROOKHAVEN LAB · PI Vivian Stojanoff · 2019 to 2026
$38.6MUser Training and OutreachP30GM124165 · NIGMS · CORNELL UNIVERSITY · PI STEVEN E EALICK · 2018 to 2026
$34.2MStructure and Function of MetalloenzymesR01GM049758 · NIGMS · UNIVERSITY OF PENNSYLVANIA · PI CHRISTIANSON, DAVID W · 1994 to 2025
$7.6MNIGMS NIH HHS P30 GM124165NIGMS NIH HHS P30 GM133893NIGMS NIH HHS R01 GM049758
Abstract
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6 (HDAC6) has been associated with the pathogenesis of cancer and neurodegeneration, thus making these two enzymes promising targets for pharmaceutical intervention. Herein, we report the design, synthesis, and biological characterization of the first-in-class dual Sirt2/HDAC6 inhibitors as molecular tools for dual inhibition of tubulin deacetylation. Using biochemical
Indexed as
BenzamidesPyrimidinesSirtuin 2ThiazolesTubulinAcetylationHistone Deacetylase 6Histone Deacetylase InhibitorsBenzamidesHistone Deacetylase 6Histone Deacetylase InhibitorsPyrimidinesSirt2 inhibitor Mz325Sirtuin 2ThiazolesTubulin
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