title: Selective histone deacetylase small molecule inhibitors: recent progress and perspectives.
abstract: Since the first pan-HDAC inhibitor SAHA was approved by U.S. FDA 10 years ago, HDACs including SIRT1-7 have received significant attention due to the fact that aberrant histone deacetylase activtiy has been implicated in a variety of human diseases, such as cancers, virus infection, and neurodegenerative diseases. During the past years, a considerable achievement of development of isoform- or class-selective HDAC inhibitors has been made, yielding many drug candidates for further clinical studies, which represents a state-of-the-art technology in the drug discovery arena. Areas covered: This review covers new patents and articles about isoform- or class-selective HDAC inhibitors during the last four years, as well as the therapeutic potential of these compounds. Expert opinion: HDACs represent one of the most promising therapeutic targets, particularly for tumor therapy though their roles in cancer are still blurry. From 2012 to present, along with the advances of structural biology and homology models, lots of isoform- or class-selective HDAC inhibitors, such as hydroxamic acids and benzamides with various capping groups were found, providing a promising way to circumvent drug toxicity and side-effect issues, as well as providing chemical probes for further better understanding of the biological process related to specific isoform.
authors.affiliation: a Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases and Department of Medicinal Chemistry , College of Pharmaceutical Sciences, Soochow University , Suzhou , PR China.
authors.forename: Hai-Tao
authors.initials: HT
authors.lastname: Qin
authors.affiliation: b Department of Medicinal Chemistry , College of Pharmaceutical Sciences, Soochow University , Suzhou , PR China.
authors.forename: Huan-Qiu
authors.initials: HQ
authors.lastname: Li
authors.affiliation: a Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases and Department of Medicinal Chemistry , College of Pharmaceutical Sciences, Soochow University , Suzhou , PR China.
authors.forename: Feng
authors.initials: F
authors.lastname: Liu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D015195:Drug Design; D056572:Histone Deacetylase Inhibitors / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D006655:Histone Deacetylases / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology; D019636:Neurodegenerative Diseases / Q000188:drug therapy / Q000201:enzymology; D010330:Patents as Topic; D014777:Virus Diseases / Q000188:drug therapy / Q000201:enzymology
chemical_list: D000970:Antineoplastic Agents; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases
keywords: Histone deacetylases; anti-cancer; epigenetics; selective inhibitors; sirtuin