Autophagy inducing cyclic peptides constructed by methionine alkylation

Qin, Xuan; Shi, Xiaodong; Tu, Licheng; Zhou, Ziyuan; Zhao, Rongtong; Zhan, Mei-Miao; Yin, Feng; Li, Zigang

doi:10.1039/c9cc01027k

Cited by 5 publications

(1 citation statement)

References 31 publications

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“…The first strategy involves diversity-oriented stapling, where two cysteines are introduced to the Beclin 1 peptide sequence and cross-linked by thiol bis-alkylation to produce a stapled active peptide DD5-o ( Peraro et al, 2017 ), or three methionine are introduced to the sequence and cross-linked by methionine bis-alkylation to produce a bicyclic active peptide 7f ( Qin et al, 2019 ). Interestingly, although Tat-BECN1 shows as a random coil in circular dichroism, the structure of DD5-o and the activity of retro-inverso variants of Tat-BECN1 suggest helical conformations may be adopted upon action ( Peraro et al, 2017 ).…”

Section: Optimization and Developmentmentioning

confidence: 99%

Development of an autophagy activator from Class III PI3K complexes, Tat-BECN1 peptide: Mechanisms and applications

Lu²,

Zhao³

2022

Front. Cell Dev. Biol.

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Impairment or dysregulation of autophagy has been implicated in many human pathologies ranging from neurodegenerative diseases, infectious diseases, cardiovascular diseases, metabolic diseases, to malignancies. Efforts have been made to explore the therapeutic potential of pharmacological autophagy activators, as beneficial health effects from caloric restriction or physical exercise are linked to autophagy activation. However, the lack of specificity remains the major challenge to the development and clinical use of autophagy activators. One candidate of specific autophagy activators is Tat-BECN1 peptide, derived from Beclin 1 subunit of Class III PI3K complexes. Here, we summarize the molecular mechanisms by which Tat-BECN1 peptide activates autophagy, the strategies for optimization and development, and the applications of Tat-BECN1 peptide in cellular and organismal models of physiology and pathology.

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Section: Optimization and Developmentmentioning

confidence: 99%