Rational design of stapled peptides targeting phosphorylated GSK3β for regulating osteoclast differentiation

Glycogen synthase kinase-3β (GSK-3β), has been reported to show essential roles in osteoclast differentiation. Modeled after FRATtide, a peptide derived from a GSK-3 binding protein, here we designed and synthesized a series of stapled peptides targeting phosphorylated GSK3β, and evaluated the corre...

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Detalles Bibliográficos
Autores principales: Liu, Tairong, Cong, Wei, Ye, Lei, Xu, Xike, Liao, Xiufei, Xie, Gang, Cheng, Zhaoxi, Hu, Honggang, Li, Xiang, Liao, Hongli
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2020
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9049898/
https://www.ncbi.nlm.nih.gov/pubmed/35492160
http://dx.doi.org/10.1039/d0ra00008f
Descripción
Sumario:Glycogen synthase kinase-3β (GSK-3β), has been reported to show essential roles in osteoclast differentiation. Modeled after FRATtide, a peptide derived from a GSK-3 binding protein, here we designed and synthesized a series of stapled peptides targeting phosphorylated GSK3β, and evaluated the corresponding biological activities. The results indicated that stapled peptides with better helical contents and proteolytic stability than the linear ones showed improved biological activity in inhibiting osteoclast differentiation. Among them, FRC-2 and FRN-2 showed promising prospects for treating osteoporosis.

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