Histone deacetylase (HDAC) inhibitors in cancer: a patent review (2017-present)

Chunlong Zhao1, Hang Dong1, Qifu Xu1

  • 1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Ji'nan, China.

Insights

Histone deacetylase (HDAC) inhibitors are vital for treating cancers by regulating protein acetylation. Recent research focuses on novel HDAC inhibitors for improved cancer therapy and other diseases.

Area of Science:

  • Epigenetics
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Histone deacetylase (HDAC) inhibitors are critical for managing acetylation/deacetylation balance in histones and non-histone proteins.
  • HDACs represent significant epigenetic targets, with their inhibitors being key compounds in cancer treatment.
  • Recent advancements focus on selective and multitarget HDAC inhibitors.

Purpose of the Study:

  • To review recent advancements in the synthesis and application of HDAC inhibitors and hybrid inhibitors.
  • To highlight the progress and challenges in developing novel HDAC inhibitors.
  • To explore emerging therapeutic applications of HDAC inhibitors beyond cancer.

Main Methods:

  • Literature review of scientific publications and patents from 2017-2019.
  • Analysis of synthetic strategies for novel HDAC inhibitors.
  • Evaluation of therapeutic applications and pharmacokinetic profiles.

Main Results:

  • Significant progress in developing selective and multitarget HDAC inhibitors.
  • Identification of a need for novel zinc-binding groups to overcome pharmacokinetic limitations of hydroxamic acids.
  • Exploration of HDAC inhibitors for treating alcohol use disorder, neurological disorders, and age-related diseases.

Conclusions:

  • HDAC inhibitors are crucial in cancer therapy and show promise for other diseases.
  • Development of novel HDAC inhibitors with improved pharmacokinetic profiles is essential.
  • Continued research into HDAC inhibitors offers new therapeutic strategies for various human conditions.

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