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 Nε-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 f...

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Main Authors:	Jiajia Liu, Yajun Huang, Weiping Zheng
Format:	Article
Language:	English
Published:	MDPI AG 2016-09-01
Series:	Molecules
Subjects:	sirtuin SIRT5 inhibitor cyclic peptide Nε-carboxyethyl-thiocarbamoyl-lysine
Online Access:	http://www.mdpi.com/1420-3049/21/9/1217

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spelling	doaj-0663821577ce40799b18d4ce4501731c2020-11-24T22:13:52ZengMDPI AGMolecules1420-30492016-09-01219121710.3390/molecules21091217molecules21091217A Selective Cyclic Peptidic Human SIRT5 InhibitorJiajia Liu0Yajun Huang1Weiping Zheng2School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, ChinaSchool of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, ChinaSchool of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, ChinaIn the current study, we discovered that a side chain-to-side chain cyclic pentapeptide harboring a central Nε-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.http://www.mdpi.com/1420-3049/21/9/1217sirtuinSIRT5inhibitorcyclic peptideNε-carboxyethyl-thiocarbamoyl-lysine
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Jiajia Liu Yajun Huang Weiping Zheng
spellingShingle	Jiajia Liu Yajun Huang Weiping Zheng A Selective Cyclic Peptidic Human SIRT5 Inhibitor Molecules sirtuin SIRT5 inhibitor cyclic peptide Nε-carboxyethyl-thiocarbamoyl-lysine
author_facet	Jiajia Liu Yajun Huang Weiping Zheng
author_sort	Jiajia Liu
title	A Selective Cyclic Peptidic Human SIRT5 Inhibitor
title_short	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_sort	selective cyclic peptidic human sirt5 inhibitor
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2016-09-01
description	In the current study, we discovered that a side chain-to-side chain cyclic pentapeptide harboring a central Nε-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.
topic	sirtuin SIRT5 inhibitor cyclic peptide Nε-carboxyethyl-thiocarbamoyl-lysine
url	http://www.mdpi.com/1420-3049/21/9/1217
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A Selective Cyclic Peptidic Human SIRT5 Inhibitor

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