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Background: Tip60, the founding member of MYST histone acetyltransferase family, was originally identified as a cellular acetyltransferase protein that interacts with HIV-1 Tat. Tip60 plays roles in many processes such as cellular signaling transmission, DNA damage repair, cell cycle and checkpoint control and apoptosis by acetylating its histone or non-histone substrates. Results: Dysfunction of Tip60 could promote or suppress diseases including different kinds of cancers. Conclusion: Here, main functions and its known inhibitors were summarized. >