Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity

Autor: Laura Sinatra, Jing Yang, Julian Schliehe-Diecks, Niklas Dienstbier, Melina Vogt, Philip Gebing, Luisa M. Bachmann, Melf Sönnichsen, Thomas Lenz, Kai Stühler, Andrea Schöler, Arndt Borkhardt, Sanil Bhatia, Finn K. Hansen

Publikováno v: Journal of medicinal chemistry. 65(24)

Selective histone deacetylase 6 (HDAC6) inhibitors are useful tools to study the function of the second catalytic domain of HDAC6, but they cannot interfere with (non)-enzymatic functions of HDAC6, which are mediated via the first catalytic domain or

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58716a1204f43910128642bef4d0b507
https://pubmed.ncbi.nlm.nih.gov/36473103

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

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

Therapeutic stratification of acute leukemia using high throughput drug screening

Autor: Julian Schliehe-Diecks, Melf Sönnichsen, Arndt Borkhardt, Julia Hauer, N. Dienstbier, Marc Remke, Ute Fischer, Heinz Ahlert, Sanil Bhatia

Publikováno v: Klinische Pädiatrie.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::997f53dd28015e4f4e04cfc2a93fa86a
https://doi.org/10.1055/s-0040-1709770

Therapeutic Stratification of PTEN-MYC Axis Appears to be Promising for Molecular Targeted Therapies in Refractory and Relapsed T-Cell Acute Lymphoblastic Leukemia

Autor: Sanil Bhatia, Heinz Ahlert, Julia Hauer, Ute Fischer, Marc Remke, Melf Sönnichsen, Arndt Borkhardt, Niklas Dienstbier

Publikováno v: Blood. 134:3883-3883

Therapy refractory and relapsed T-cell acute lymphoblastic leukemia (T-ALL) is still one of the most common causes for cancer related death in children. T-ALL is a highly heterogeneous disease with several established biomarkers, which promote its pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::91e92b919a3c7d1d92e6a766718fba73
https://doi.org/10.1182/blood-2019-128136