Hydroxamic Acids Immobilized on Resins (HAIRs): Synthesis of Dual‐Targeting HDAC Inhibitors and HDAC Degraders (PROTACs)

Autor: Finn K. Hansen, Alexandra Hamacher, Jens Meiler, Jan J. Bandolik, Martin Roatsch, Clara T. Schoeder, Andrea Schöler, Laura Sinatra, Sanil Bhatia, Matthias U. Kassack, Melf Sönnichsen, Arndt Borkhardt

Publikováno v: Sinatra, L, Bandolik, J J, Roatsch, M, Soennichsen, M, Schoeder, C T, Hamacher, A, Schoeler, A, Borkhardt, A, Meiler, J, Bhatia, S, Kassack, M U & Hansen, F K 2020, ' Hydroxamic Acids Immobilized on Resins (HAIRs) : Synthesis of Dual-Targeting HDAC Inhibitors and HDAC Degraders (PROTACs) ', Angewandte Chemie International Edition, vol. 59, no. 50, pp. 22494-22499 . https://doi.org/10.1002/anie.202006725
Angewandte Chemie (International Ed. in English)

Inhibition of more than one cancer‐related pathway by multi‐target agents is an emerging approach in modern anticancer drug discovery. Here, based on the well‐established synergy between histone deacetylase inhibitors (HDACi) and alkylating age

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82d75b9c011e7cc21cadd59c1622e90e
https://doi.org/10.1002/anie.202006725

Structure‐Based Screening of Tetrazolylhydrazide Inhibitors versus KDM4 Histone Demethylases

Autor: Martin Roatsch, Andreas Link, Oxana Krylova, Udo Heinemann, Nicole Rüger, Manfred Jung, Piotr H. Małecki, Manfred S. Weiss

Publikováno v: Małecki, P H, Rüger, N, Roatsch, M, Krylova, O, Link, A, Jung, M, Heinemann, U & Weiss, M S 2019, ' Structure-Based Screening of Tetrazolylhydrazide Inhibitors versus KDM4 Histone Demethylases ', ChemMedChem, vol. 14, no. 21, pp. 1828-1839 . https://doi.org/10.1002/cmdc.201900441
Chemmedchem

Human histone demethylases are known to play an important role in the development of several tumor types. Consequently, they have emerged as important medical targets for the treatment of human cancer. Herein, structural studies on tetrazolylhydrazid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e7971ae548e2e8f2e478ba5abdcbece
https://doi.org/10.1002/cmdc.201900441

Proteolysis-Targeting Chimeras (PROTACs) Based on Macrocyclic Tetrapeptides Selectively Degrade Class I Histone Deacetylases 1–3

Autor: Martin Roatsch, Daniel Herp, Anja Vogelmann, Christian A. Olsen, Manfred Jung

Histone deacetylases (HDACs) remove acetyl groups from histone proteins and are implicated in gene regulation. They have been recognized as drug targets for treatment of cancer and other human diseases and several inhibitors are already clinically us

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b6852e810ed762b7a4ac62c3b125ecf5
https://doi.org/10.26434/chemrxiv.12416303

The Clinically Used Iron Chelator Deferasirox is an Inhibitor of Epigenetic JumonjiC Domain-Containing Histone Demethylases

Autor: Manfred Jung, Martin Roatsch, Inga Hoffmann, Martine I. Abboud, Rebecca L. Hancock, Hanna Tarhonskaya, Kuo-Feng Hsu, Sarah E. Wilkins, Tzu-lan Yeh, Kerstin Lippl, Kerstin Serrer, Isabelle Moneke, Theresa D. Ahrens, Dina Robaa, Sandra Wenzler, Henriette Franz, Wolfgang Sippl, Silke Lassmann, Sven Diederichs, Erik Schleicher, Christopher J. Schofield, Akane Kawamura, Roland Schüle

Fe(II)- and 2-oxoglutarate (2OG)-dependent JumonjiC domain-containing histone demethylases (JmjC KDMs) are epigenetic eraser enzymes involved in the regulation of gene expression and are emerging drug targets in oncology. We screened a set of clinica

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e472f20dd442521931b9fcd32e8099d
https://doi.org/10.26434/chemrxiv.7699853

Tetrazolylhydrazides as Selective Fragment-Like Inhibitors of the JumonjiC-Domain-Containing Histone Demethylase KDM4A

Autor: Martin Roatsch, Nicole Rüger, Manfred Jung, Roland Schüle, Henriette Franz, Thomas Emmrich, Andreas Link

Publikováno v: ChemMedChem. 10:1875-1883

The JumonjiC-domain-containing histone demethylase 2A (JMJD2A, KDM4A) is a key player in the epigenetic regulation of gene expression. Previous publications have shown that both elevated and lowered enzyme levels are associated with certain types of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b147516899763b69de6995ce792d7076
https://doi.org/10.1002/cmdc.201500335