Glioblastoma: current status, emerging targets, and recent advances
Glioblastoma (GBM) is a highly malignant brain tumor characterized by a heterogeneous
population of genetically unstable and highly infiltrative cells that are resistant to …
population of genetically unstable and highly infiltrative cells that are resistant to …
[HTML][HTML] Perspectives and new aspects of histone deacetylase inhibitors in the therapy of CNS diseases
B Han, M Wang, J Li, Q Chen, N Sun, X Yang… - European Journal of …, 2023 - Elsevier
Many populations worldwide are suffering from central nervous system (CNS) diseases such
as brain tumors, neurodegenerative diseases (Alzheimer's disease, Parkinson's disease …
as brain tumors, neurodegenerative diseases (Alzheimer's disease, Parkinson's disease …
[HTML][HTML] Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor
J Bröker, AG Waterson, C Smethurst… - Journal of Medicinal …, 2022 - ncbi.nlm.nih.gov
Activating mutations in KRAS are the most frequent oncogenic alterations in cancer. The
oncogenic hotspot position 12, located at the lip of the switch II pocket, offers a covalent …
oncogenic hotspot position 12, located at the lip of the switch II pocket, offers a covalent …
Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor
J Bröker, AG Waterson, C Smethurst… - Journal of Medicinal …, 2022 - ACS Publications
Activating mutations in KRAS are the most frequent oncogenic alterations in cancer. The
oncogenic hotspot position 12, located at the lip of the switch II pocket, offers a covalent …
oncogenic hotspot position 12, located at the lip of the switch II pocket, offers a covalent …
Development of fluorinated peptoid-based histone deacetylase (HDAC) inhibitors for therapy-resistant acute leukemia
N Reßing, J Schliehe-Diecks, PR Watson… - Journal of medicinal …, 2022 - ACS Publications
Using a microwave-assisted protocol, we synthesized 16 peptoid-capped HDAC inhibitors
(HDACi) with fluorinated linkers and identified two hit compounds. In biochemical and …
(HDACi) with fluorinated linkers and identified two hit compounds. In biochemical and …
Recent progress in histone deacetylase (HDAC) 1 inhibitors as anticancer agent
P Patel, SK Wahan, S Vishakha… - Current Cancer Drug …, 2023 - ingentaconnect.com
Histone deacetylases (HDACs) are essential for maintaining homeostasis by catalyzing
histone deacetylation. Aberrant expression of HDACs is associated with various human …
histone deacetylation. Aberrant expression of HDACs is associated with various human …
Solid‐Phase Synthesis of Peptidomimetics with Peptide Backbone Modifications
A Abdildinova, MJ Kurth… - Asian Journal of Organic …, 2021 - Wiley Online Library
Peptidomimetics are a class of compounds with promising pharmacological properties.
Peptidomimetics reduce limitations of peptides including low bioavailability, poor stability …
Peptidomimetics reduce limitations of peptides including low bioavailability, poor stability …
Bio-instructive materials on-demand–combinatorial chemistry of peptoids, foldamers, and beyond
CN Herlan, D Feser, U Schepers… - Chemical Communications, 2021 - pubs.rsc.org
Combinatorial chemistry allows for the rapid synthesis of large compound libraries for high
throughput screenings in biology, medicinal chemistry, or materials science. Especially …
throughput screenings in biology, medicinal chemistry, or materials science. Especially …
[HTML][HTML] Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics
R Raudszus, R Nowotny, CGW Gertzen… - Bioorganic & medicinal …, 2019 - Elsevier
Fluorescent tagging of bioactive molecules is a powerful tool to study cellular uptake kinetics
and is considered as an attractive alternative to radioligands. In this study, we developed …
and is considered as an attractive alternative to radioligands. In this study, we developed …
[HTML][HTML] Preferential HDAC6 inhibitors derived from HPOB exhibit synergistic antileukemia activity in combination with decitabine
M Tretbar, J Schliehe-Diecks, L von Bredow… - European Journal of …, 2024 - Elsevier
Abstract Histone deacetylase 6 (HDAC6) is an emerging drug target to treat oncological and
non-oncological conditions. Since highly selective HDAC6 inhibitors display limited …
non-oncological conditions. Since highly selective HDAC6 inhibitors display limited …