Výsledky vyhledávání - "Nina Reßing"

Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia

Autor: Nina Reßing, Julian Schliehe-Diecks, Paris R. Watson, Melf Sönnichsen, Abigail D. Cragin, Andrea Schöler, Jing Yang, Linda Schäker-Hübner, Arndt Borkhardt, David W. Christianson, Sanil Bhatia, Finn K. Hansen

Publikováno v: Journal of medicinal chemistry. 65(22)

Using a microwave-assisted protocol, we synthesized 16 peptoid-capped HDAC inhibitors (HDACi) with fluorinated linkers and identified two hit compounds. In biochemical and cellular assays

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c328a1ef9a9552fa48f1a4d563a8adbd
https://pubmed.ncbi.nlm.nih.gov/36351184

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Difluoromethyl-1,3,4-oxadiazoles are selective, mechanism-based, and essentially irreversible inhibitors of histone deacetylase 6

Autor: Beate König, Paris R. Watson, Nina Reßing, Abigail D. Cragin, Linda Schäker-Hübner, David W. Christianson, Finn Kristian Hansen

Histone deacetylase 6 (HDAC6) is an important drug target in oncology and non-oncological diseases. Most available HDAC6 inhibitors (HDAC6i) utilize a hydroxamic acid as zinc-binding group which limits the therapeutic opportunities due its genotoxic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea6a59ac364a0a4c932b7e028b29ef18
https://doi.org/10.26434/chemrxiv-2023-6kt1w

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The Dual Histone Deacetylase-Proteasome Inhibitor RTS-V5 Acts Synergistically With Ritonavir to Induce Endoplasmic Reticulum Stress in Bladder Cancer Cells

Autor: Finn K. Hansen, Akinori Sato, Wolfgang A. Schulz, Takako Asano, Nina Reßing, Kazuki Okubo

Publikováno v: Anticancer Research. 41:5987-5996

Background/aim Simultaneous inhibition of histone deacetylase and proteasomes induces endoplasmic reticulum (ER) stress efficiently. RTS-V5 is the first dual histone deacetylase-proteasome inhibitor, and we anticipated that combining it with the cyto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63ef7d1c390ccee333c5fa78253a8175
https://doi.org/10.21873/anticanres.15417

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Ubiquitin-proteasome System Is a Promising Target for Killing Cisplatin-resistant Bladder Cancer Cells

Autor: Makoto Isono, Wolfgang A. Schulz, Takako Asano, Finn K. Hansen, Akinori Sato, Nina Reßing, Kazuki Okubo

Publikováno v: Anticancer Research. 41:2901-2912

Background/aim Activation of the ubiquitin-proteasome system (UPS) has been shown to be associated with drug resistance in cancer. Using bladder cancer cells, we investigated the association between UPS activation and cisplatin resistance and also th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b03cc9c06f4f454c440280a90f633ac3
https://doi.org/10.21873/anticanres.15072

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Multicomponent Synthesis, Binding Mode, and Structure–Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups

Autor: David W. Christianson, Finn K. Hansen, Andrea Schöler, Alexander Jan Skerhut, Julian Schliehe-Diecks, Sanil Bhatia, Melf Sönnichsen, Arndt Borkhardt, Matthias U. Kassack, Julia Hauer, Jeremy D. Osko, Nina Reßing

Publikováno v: J Med Chem
Journal of Medicanial Chemistry

Histone deacetylase 6 (HDAC6) is an emerging target for the treatment of cancer, neurodegenerative diseases, inflammation, and other diseases. Here, we present the multicomponent synthesis and structure-activity relationship of a series of tetrazole-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e964480b85aa84ddc8e8db1653e85836
https://doi.org/10.1021/acs.jmedchem.9b01888

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Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity

Autor: Alexander Schramm, Holger Gohlke, Christoph G. W. Gertzen, Thomas Kurz, Andrea Schöler, Nina Reßing, Viktoria Marquardt, Finn K. Hansen, Marc Remke, Achim Aigner

Publikováno v: MedChemComm. 10:1109-1115

Histone deacetylases (HDACs) have been identified as promising epigenetic drug targets for the treatment of neuroblastoma and glioblastoma. In this work, we have rationally designed a novel class of peptoid-based histone deacetylase inhibitors (HDACi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd2281050b2a7307cbe79eb546f0486e
https://doi.org/10.1039/c8md00454d

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Anticancer Therapy with HDAC Inhibitors: Mechanism-Based Combination Strategies and Future Perspectives

Autor: Robert Jenke, Nina Reßing, Finn K. Hansen, Achim Aigner, Thomas Büch

Publikováno v: Cancers
Cancers, Vol 13, Iss 634, p 634 (2021)

Simple Summary Beyond mutations, epigenetic changes have been described as drivers for cancer as well. While leaving the overall DNA structure intact, they can be responsible for tumor malignancy by mediating the transcriptional upregulation of oncog

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::0ffbbce5f8d6823c79f92dbef27e3a0e
https://ul.qucosa.de/id/qucosa:84972

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Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor

Autor: Finn K. Hansen, Jeremy D. Osko, Julia Hauer, Arndt Borkhardt, Sanil Bhatia, Viktoria Krieger, David W. Christianson, Heinz Ahlert, Michael Groll, Thomas Kurz, Nina Reßing

Publikováno v: Journal of medicinal chemistry. 61(22)

Dual- or multitarget drugs have emerged as a promising alternative to combination therapies. Proteasome inhibitors (PIs) possess synergistic activity with histone deacetylase (HDAC) inhibitors due to the simultaneous blockage of the ubiquitin degrada

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::630009d8da051acdba407ac1add4f0d7
https://pubmed.ncbi.nlm.nih.gov/30365892

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