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Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Identification of type-specific anticancer histone deacetylase inhibitors: road to success
Nighat Noureen1, Hamid Rashid, Saima Kalsoom
1Department of Computer Science and Bioinformatics, Mohammad Ali Jinnah University, Jinnah Avenue, Blue Area, Islamabad, Pakistan. nighatnoureen@gmail.com
Abstract:
Cancer is a serious and life-eliminating disease. Majority of anticancer agents are non-selective. Along with the cancerous cells they also target the normal ones. An important aspect is to hit the developing mechanism of the tumor, which is highlighted by in silico drug designing. On the basis of novel molecular targets, in silico (computational approach) drug discovery has emerged as today's need. Histone deacetylases are an important therapeutic target for many human cancers. The first and only approved (in 2006) histone deacetylase inhibitors (HDACIs) is Zolinza. Depending on the types of the histone deacetylase (HDAC) enzymes, discovery of type-specific inhibitors is important. With continued research and development, in near future HDACIs are likely to figure prominently in cancer treatment plans. This review presents the overview of HDACs, their role in cancer, their structural classes, activity, catalytic domain and the inhibitors of HDACs for cancer therapy. Also it helps in understanding the open directions in this area of research and highlights the importance of computational approaches in discovering specific drugs for cancer therapy.
Insights
In silico drug design offers a novel approach to developing targeted cancer therapies by focusing on molecular targets like histone deacetylases (HDACs). This strategy aims to create more effective and specific histone deacetylase inhibitors (HDACIs) for cancer treatment.
Area of Science:
- Oncology
- Computational Chemistry
- Drug Discovery
Background:
- Cancer remains a significant global health challenge, with many current treatments lacking selectivity, leading to side effects on normal cells.
- Targeting tumor development mechanisms is crucial for effective cancer therapy.
- Histone deacetylases (HDACs) represent a validated therapeutic target in various human cancers.
Purpose of the Study:
- To review the role of HDACs in cancer.
- To explore the structural classes, activity, and catalytic domains of HDACs.
- To discuss HDAC inhibitors (HDACIs) for cancer therapy and highlight the importance of computational approaches in drug discovery.
Main Methods:
- Review of existing literature on HDACs and their inhibitors.
- Analysis of HDAC structure, function, and role in cancer.
- Exploration of in silico drug design strategies for HDACIs.
Main Results:
- Histone deacetylases are critical targets for cancer therapy.
- The development of type-specific HDAC inhibitors is essential.
- In silico drug design is a promising approach for discovering novel and specific HDACIs.
Conclusions:
- HDACIs are poised to play a significant role in future cancer treatment plans.
- Computational approaches are vital for identifying specific HDAC inhibitors.
- Further research into HDACs and their inhibitors holds great potential for advancing cancer therapy.
