A Selective Cyclic Peptidic Human SIRT5 Inhibitor

In the current study, we discovered that a side chain-to-side chain cyclic pentapeptide harboring a central N(ε)-carboxyethyl-thiocarbamoyl-lysine residue behaved as a strong and selective (versus human SIRT1/2/3/6) inhibitor against human SIRT5-catalyzed deacylation reaction. This compound was also...

Descripción completa

Detalles Bibliográficos
Autores principales: Liu, Jiajia, Huang, Yajun, Zheng, Weiping
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272981/
https://www.ncbi.nlm.nih.gov/pubmed/27626398
http://dx.doi.org/10.3390/molecules21091217
_version_ 1783377279093571584
author Liu, Jiajia
Huang, Yajun
Zheng, Weiping
author_facet Liu, Jiajia
Huang, Yajun
Zheng, Weiping
author_sort Liu, Jiajia
collection PubMed
description In the current study, we discovered that a side chain-to-side chain cyclic pentapeptide harboring a central N(ε)-carboxyethyl-thiocarbamoyl-lysine residue behaved as a strong and selective (versus human SIRT1/2/3/6) inhibitor against human SIRT5-catalyzed deacylation reaction. This compound was also found to be proteolytically much more stable than its linear counterpart. This compound could be a valuable lead for developing stronger, selective, metabolically stable, and cell permeable human SIRT5 inhibitors.
format Online
Article
Text
id pubmed-6272981
institution National Center for Biotechnology Information
language English
publishDate 2016
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-62729812018-12-28 A Selective Cyclic Peptidic Human SIRT5 Inhibitor Liu, Jiajia Huang, Yajun Zheng, Weiping Molecules Communication In the current study, we discovered that a side chain-to-side chain cyclic pentapeptide harboring a central N(ε)-carboxyethyl-thiocarbamoyl-lysine residue behaved as a strong and selective (versus human SIRT1/2/3/6) inhibitor against human SIRT5-catalyzed deacylation reaction. This compound was also found to be proteolytically much more stable than its linear counterpart. This compound could be a valuable lead for developing stronger, selective, metabolically stable, and cell permeable human SIRT5 inhibitors. MDPI 2016-09-10 /pmc/articles/PMC6272981/ /pubmed/27626398 http://dx.doi.org/10.3390/molecules21091217 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Communication
Liu, Jiajia
Huang, Yajun
Zheng, Weiping
A Selective Cyclic Peptidic Human SIRT5 Inhibitor
title A Selective Cyclic Peptidic Human SIRT5 Inhibitor
title_full A Selective Cyclic Peptidic Human SIRT5 Inhibitor
title_fullStr A Selective Cyclic Peptidic Human SIRT5 Inhibitor
title_full_unstemmed A Selective Cyclic Peptidic Human SIRT5 Inhibitor
title_short A Selective Cyclic Peptidic Human SIRT5 Inhibitor
title_sort selective cyclic peptidic human sirt5 inhibitor
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272981/
https://www.ncbi.nlm.nih.gov/pubmed/27626398
http://dx.doi.org/10.3390/molecules21091217
work_keys_str_mv AT liujiajia aselectivecyclicpeptidichumansirt5inhibitor
AT huangyajun aselectivecyclicpeptidichumansirt5inhibitor
AT zhengweiping aselectivecyclicpeptidichumansirt5inhibitor
AT liujiajia selectivecyclicpeptidichumansirt5inhibitor
AT huangyajun selectivecyclicpeptidichumansirt5inhibitor
AT zhengweiping selectivecyclicpeptidichumansirt5inhibitor

Ejemplares similares