Abstract
Chemoresistance is one of the most important challenges in the clinical management of lung cancer. SIRT1 is a NAD dependent protein deacetylase and implicated in diverse cellular processes such as DNA damage repair, and cancer progression. SIRT1 is upregulated in chemoresistant lung cancer cells, genetic knockdown or chemical inhibition of SIRT1 reversed chemoresistance by enhancing DNA damage and apoptosis activation, accompanied with XRCC1 degradation. E3 ligase β-TrCP catalyzed the poly-ubiquitination of XRCC1 to promote its proteasome-dependent degradation. SIRT1 bound and deacetylated XRCC1 at lysine K260, K298 and K431, preventing it from β-TrCP-dependent ubiquitination. Mutations of these three lysine sites in XRCC1 abrogated the interaction with β-TrCP and prolonged the half-life of XRCC1 protein. Here, we describes SIRT1 confers chemoresistance to lung cancer cells by deacetylating and stabilizing XRCC1. Therefore, targeting SIRT1 might be a new strategy to manage the chemoresistance of lung cancer, and probably other cancers.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Animals
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Antineoplastic Agents / pharmacology
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Apoptosis / drug effects
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Apoptosis / genetics
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Carbazoles / pharmacology
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Cell Line, Tumor / drug effects
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Cell Line, Tumor / metabolism
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Cell Line, Tumor / pathology
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Cisplatin / pharmacology
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DNA Damage
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DNA Repair / drug effects
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DNA, Neoplasm / genetics*
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DNA, Neoplasm / metabolism
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Drug Resistance, Neoplasm / drug effects
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Drug Resistance, Neoplasm / genetics*
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Gene Expression Regulation, Neoplastic*
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Humans
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Mice
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Protein Processing, Post-Translational
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Respiratory Mucosa / drug effects
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Respiratory Mucosa / metabolism
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Respiratory Mucosa / pathology
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Sequence Alignment
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Sequence Homology, Amino Acid
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Signal Transduction
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Sirtuin 1 / antagonists & inhibitors
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Sirtuin 1 / genetics*
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Sirtuin 1 / metabolism
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Ubiquitination
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X-ray Repair Cross Complementing Protein 1 / genetics*
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X-ray Repair Cross Complementing Protein 1 / metabolism
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beta-Transducin Repeat-Containing Proteins / genetics*
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beta-Transducin Repeat-Containing Proteins / metabolism
Substances
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6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
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Antineoplastic Agents
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Carbazoles
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DNA, Neoplasm
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X-ray Repair Cross Complementing Protein 1
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XRCC1 protein, human
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beta-Transducin Repeat-Containing Proteins
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Sirt1 protein, mouse
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Sirtuin 1
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Cisplatin