Harmine-Based Dual Inhibitors Targeting Histone Deacetylase (HDAC) and DNA as a Promising Strategy for Cancer Therapy

2022 ◽  
pp. 105604
Author(s):  
Dehua Lu ◽  
Lailiang Qu ◽  
Cheng Wang ◽  
Heng Luo ◽  
Shang Li ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Histone Deacetylase ◽  
Promising Strategy ◽  
Dual Inhibitors

Discovery of novel dual c-Met/HDAC inhibitors as a promising strategy for cancer therapy

2020 ◽  
Vol 101 ◽  
pp. 103970 ◽  
Author(s):  
Hao Hu ◽  
Fei Chen ◽  
Yuhong Dong ◽  
Yajing Liu ◽  
Ping Gong
Keyword(s):  
Cancer Therapy ◽  
Hdac Inhibitors ◽  
Promising Strategy

Multi-Targeted Histone Deacetylase Inhibitors in Cancer Therapy

2012 ◽  
Vol 19 (4) ◽  
pp. 475-487 ◽  
Author(s):  
T. Ai ◽  
H. Cui ◽  
L. Chen
Keyword(s):  
Cancer Therapy ◽  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors

Dual Targeting Strategies On Histone Deacetylase 6 (HDAC6) And Heat Shock Protein 90 (Hsp90)

2021 ◽  
Vol 28 ◽  
Author(s):  
Davide Bonanni ◽  
Andrea Citarella ◽  
Davide Moi ◽  
Luca Pinzi ◽  
Elisa Bergamini ◽  
...  
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Histone Deacetylase ◽  
Single Molecule ◽  
Heat Shock Protein 90 ◽  
Histone Deacetylase 6 ◽  
Small Molecular Weight ◽  
Antitumor Effects ◽  
Target Drug ◽  
Dual Inhibitors

: The design of multi-target drugs acting simultaneously on multiple signaling pathways is a growing field in medicinal chemistry, especially for the treatment of complex diseases such as cancer. Histone deacetylase 6 (HDAC6) is an established anticancer drug target involved in tumor cells transformation. Being an epigenetic enzyme at the interplay of many biological processes, HDAC6 has become an attractive target for polypharmacology studies aimed at improving therapeutic efficacy of anticancer drugs. For example, the molecular chaperone Heat shock protein 90 (Hsp90) is a substrate of HDAC6 deacetylation, and several lines of evidence demonstrate that simultaneous inhibition of HDAC6 and Hsp90 promote synergistic antitumor effects on different cancer cell lines, highlighting the potential benefits of developing a single molecule endowed with multi-target activity. This review will summarize the complex interplay between HDAC6 and Hsp90, providing also useful hints for multi-target drug design and discovery approaches in this field. To this end, crystallographic structures of HDAC6 and Hsp90 complexes will be extensively reviewed in the light of discussing binding pockets features and pharmacophore requirements and providing useful guidelines for the design of dual inhibitors. The few examples of multi-target inhibitors obtained so far, mostly based on chimeric approaches, will be summarized and put into context. Finally, the main features of HDAC6 and Hsp90 inhibitors will be compared, and ligand- and structure-based strategies potentially useful for the development of small molecular weight dual inhibitors will be proposed and discussed.

Discovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma

2020 ◽  
Vol 63 (9) ◽  
pp. 4701-4715 ◽  
Author(s):  
Yi Zhou ◽  
Xiaoting Liu ◽  
Junxin Xue ◽  
Lulu Liu ◽  
Tao Liang ◽  
...  
Keyword(s):  
Multiple Myeloma ◽  
Histone Deacetylase ◽  
Dual Inhibitors

Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy

2019 ◽  
Vol 63 (1) ◽  
pp. 122-139 ◽  
Author(s):  
Junwei Wang ◽  
Hui Li ◽  
Guangchao He ◽  
Zhaoxing Chu ◽  
Kewen Peng ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Kinase Inhibitors ◽  
Promising Strategy ◽  
Phosphoinositide 3 Kinase

scholarly journals Design of Dual Inhibitors of Histone Deacetylase 6 and Heat Shock Protein 90

ACS Omega ◽  
2020 ◽  
Vol 5 (20) ◽  
pp. 11473-11480 ◽  
Author(s):  
Luca Pinzi ◽  
Rosaria Benedetti ◽  
Lucia Altucci ◽  
Giulio Rastelli
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Histone Deacetylase ◽  
Heat Shock Protein 90 ◽  
Histone Deacetylase 6 ◽  
Dual Inhibitors

E-pharmacophore guided discovery of pyrazolo[1,5-c]quinazolines as dual inhibitors of topoisomerase-I and histone deacetylase

2020 ◽  
Vol 94 ◽  
pp. 103409 ◽  
Author(s):  
Gaurav Joshi ◽  
Sourav Kalra ◽  
Umesh Prasad Yadav ◽  
Praveen Sharma ◽  
Pankaj Kumar Singh ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Topoisomerase I ◽  
Guided Discovery ◽  
Dual Inhibitors
Sign in / Sign up

Export Citation Format

Share Document