ReferenceID 6127
Rutin increases alpha-tubulin acetylation via histone deacetylase 6 inhibition
Drug Dev Res
Microtubules are dynamic cytoskeletal filaments composed of alpha- (α) and beta (β)-tubulin proteins. α-tubulin proteins are posttranslationally acetylated, and loss of acetylation is associated with axonal transport def
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Record Fields
Scalar fields from the final reference record.
- Reference Id
- 6127
- Evidence Id
- 22717
- Core Evidence Id
- 22717
- Source Reference Id
- 5518
- Herb2 Reference Id
- HBREF006315
- Subject Paper Key
- HBIN041663_35266183
- Pubmed Id
- 35266183
- Doi
- 10.1002/ddr.21927
- Paper Title
- Rutin increases alpha-tubulin acetylation via histone deacetylase 6 inhibition
- Paper Abstract
- Microtubules are dynamic cytoskeletal filaments composed of alpha- (α) and beta (β)-tubulin proteins. α-tubulin proteins are posttranslationally acetylated, and loss of acetylation is associated with axonal transport defects, a common alteration contributing to the pathomechanisms of several neurodegenerative diseases. Restoring α-tubulin acetylation by pharmacological inhibition of HDAC6, a primary α-tubulin deacetylase, can rescue impaired transport. Therefore, HDAC6 is considered a promising therapeutic target for neurodegenerative diseases, but currently, there is no clinically approved inhibitor for this purpose. In this study, using drug repurposing strategy, we aimed to identify compounds possessing HDAC6 inhibition activity and inducing α-tubulin acetylation. We systematically analyzed the FDA-approved library by utilizing virtual screening and consensus scoring approaches. Inhibition activities of promising compounds were tested using in vitro assays. Motor neuron-like NSC34 cells were treated with the candidate compounds, and α-tubulin acetylation levels were determined by Western blot. Our results demonstrated that rutin, a natural flavonoid, inhibits cellular HDAC6 activity without inducing any toxicity, and it significantly increases α-tubulin acetylation level in motor neuron-like cells.
- Journal
- Drug Dev Res
- Publish Year
- 2022
- Experiment Subject
- Experiment Type
- Cell Experiment
- Phenotype Related
- Axonal Transport Defects; Neurodegenerative Diseases
- Paper Title Cn
- Paper Title En
- Rutin increases alpha-tubulin acetylation via histone deacetylase 6 inhibition
- Bilingual Status
- semi_complete