Related Experiment Video
Updated: Jul 29, 2025

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
Published on: August 10, 2017
Recent development of selective inhibitors targeting the HDAC6 as anti-cancer drugs: Structure, function and design
Jie Peng1, Fei Xie2, Pengxia Qin1
1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan 250012, PR China.
Abstract:
HDAC6, a member of the histone deacetylase family, mainly is a cytosolic protein and regulates cell growth by acting on non-histone substrates, such as α -tubulin, cortactin, heat shock protein HSP90, programmed death 1 (PD-1) and programmed death ligand 1 (PD-L1), that are closely related to the proliferation, invasion, immune escape and angiogenesis of cancer tissues. The approved drugs targeting the HDACs are all pan-inhibitors and have many side effects due to their lack of selectivity. Therefore, development of selective inhibitors of HDAC6 has attracted much attention in the field of cancer therapy. In this review, we will summarize the relationship between HDAC6 and cancer, and discuss the design strategies of HDAC6 inhibitors for cancer treatment in recent years.
Insights
Histone deacetylase 6 (HDAC6) regulates cancer cell growth through non-histone substrates. Selective HDAC6 inhibitors are crucial for developing targeted cancer therapies with fewer side effects.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- HDAC6 is a cytosolic protein regulating cell growth via non-histone substrates like α-tubulin, cortactin, HSP90, PD-1, and PD-L1.
- These substrates are critical in cancer proliferation, invasion, immune escape, and angiogenesis.
- Current HDAC inhibitors are non-selective pan-inhibitors, leading to significant side effects.
Purpose of the Study:
- To review the role of HDAC6 in cancer.
- To discuss recent strategies for designing selective HDAC6 inhibitors for cancer therapy.
Main Methods:
- Literature review of studies on HDAC6 and cancer.
- Analysis of design strategies for HDAC6 inhibitors.
Main Results:
- HDAC6 plays a significant role in various cancer hallmarks.
- The development of selective HDAC6 inhibitors is a promising therapeutic strategy.
- Recent research focuses on novel molecular designs for targeted inhibition.
Conclusions:
- HDAC6 is a key therapeutic target in cancer.
- Selective HDAC6 inhibition offers a promising avenue for improved cancer treatment with reduced toxicity.
Related Concept Videos
Inhibition of Cdk Activity
Targeted Cancer Therapies
There are several types of targeted therapies against...
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Treatment Resistant Cancers

