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Related Experiment Video

Updated: Mar 15, 2026

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A Selective Cyclic Peptidic Human SIRT5 Inhibitor.

Jiajia Liu1, Yajun Huang2, Weiping Zheng3

  • 1School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, China. liujiajia2401@163.com.

Molecules (Basel, Switzerland)
|September 15, 2016
PubMed
Summary

Researchers developed a cyclic peptide that strongly and selectively inhibits human SIRT5, offering improved stability over linear versions. This discovery provides a promising lead for creating more effective SIRT5 inhibitors.

Keywords:
Nε-carboxyethyl-thiocarbamoyl-lysineSIRT5cyclic peptideinhibitorsirtuin

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Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Enzyme Inhibition

Background:

  • Sirtuin 5 (SIRT5) is a key metabolic enzyme involved in deacylation reactions.
  • Developing selective inhibitors for SIRT5 is crucial for therapeutic applications.
  • Existing inhibitors often lack sufficient selectivity or metabolic stability.

Purpose of the Study:

  • To discover and characterize a novel, potent, and selective inhibitor of human SIRT5.
  • To evaluate the stability and potential of this inhibitor as a lead compound.

Main Methods:

  • Synthesis of a cyclic pentapeptide with a unique lysine modification.
  • Enzyme inhibition assays to determine potency and selectivity against human SIRT5 and other sirtuins (SIRT1/2/3/6).
  • Proteolytic stability assays comparing cyclic and linear peptide counterparts.

Main Results:

  • A cyclic pentapeptide containing N(ε)-carboxyethyl-thiocarbamoyl-lysine demonstrated potent and selective inhibition of human SIRT5.
  • The cyclic compound exhibited significantly enhanced proteolytic stability compared to its linear analog.
  • The inhibitor showed strong selectivity against human SIRT1, SIRT2, SIRT3, and SIRT6.

Conclusions:

  • The novel cyclic pentapeptide is a strong and selective inhibitor of human SIRT5.
  • This compound represents a valuable lead for developing improved, metabolically stable, and cell-permeable SIRT5 inhibitors.
  • Further development could lead to new therapeutic strategies targeting SIRT5-related pathways.