Journal
PHARMACOLOGICAL RESEARCH
Volume 131, Issue -, Pages 128-142Publisher
ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD
DOI: 10.1016/j.phrs.2018.03.001
Keywords
Cancer; Histone deacetylase; HDAC8 inhibitor; Non-hydroxamates; Zinc binding group; Structure-activity relationship (SAR)
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Funding
- University Grants Commission (UGC), New Delhi, India
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Histone deacetylase inhibitors (HDACIs) have a paramount importance in the acetylation process of histone and non-histone proteins that are crucial players in the cellular epigenetic modifications. HDACIs exert effective antiproliferation through DNA repairing, cell cycle arrest, apoptosis induction and alteration of genetic expression. HDAC8 is one of the crucial HDACs, affects the epigenetic gene silencing process and cancer progression. Hence, HDAC8 is one of the key cancer targets among class I HDACs that may be effectively blocked as a benchmark therapy to combat malignancy. In the current review, a special emphasis has been given for the non-hydroxamate type of HDAC8 inhibitors. It may provide some fruitful structural information to design newer better active candidates to fight against target specific malignancies in future.
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