Cargando…
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...
| Autores principales: | , , , , , , , , , |
|---|---|
| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
The Royal Society of Chemistry
2020
|
| Materias: | |
| 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 |
| _version_ | 1784696244225966080 |
|---|---|
| author | Liu, Tairong Cong, Wei Ye, Lei Xu, Xike Liao, Xiufei Xie, Gang Cheng, Zhaoxi Hu, Honggang Li, Xiang Liao, Hongli |
| author_facet | Liu, Tairong Cong, Wei Ye, Lei Xu, Xike Liao, Xiufei Xie, Gang Cheng, Zhaoxi Hu, Honggang Li, Xiang Liao, Hongli |
| author_sort | Liu, Tairong |
| collection | PubMed |
| description | 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. |
| format | Online Article Text |
| id | pubmed-9049898 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2020 |
| publisher | The Royal Society of Chemistry |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-90498982022-04-29 Rational design of stapled peptides targeting phosphorylated GSK3β for regulating osteoclast differentiation Liu, Tairong Cong, Wei Ye, Lei Xu, Xike Liao, Xiufei Xie, Gang Cheng, Zhaoxi Hu, Honggang Li, Xiang Liao, Hongli RSC Adv Chemistry 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. The Royal Society of Chemistry 2020-02-24 /pmc/articles/PMC9049898/ /pubmed/35492160 http://dx.doi.org/10.1039/d0ra00008f Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/ |
| spellingShingle | Chemistry Liu, Tairong Cong, Wei Ye, Lei Xu, Xike Liao, Xiufei Xie, Gang Cheng, Zhaoxi Hu, Honggang Li, Xiang Liao, Hongli Rational design of stapled peptides targeting phosphorylated GSK3β for regulating osteoclast differentiation |
| title | Rational design of stapled peptides targeting phosphorylated GSK3β for regulating osteoclast differentiation |
| title_full | Rational design of stapled peptides targeting phosphorylated GSK3β for regulating osteoclast differentiation |
| title_fullStr | Rational design of stapled peptides targeting phosphorylated GSK3β for regulating osteoclast differentiation |
| title_full_unstemmed | Rational design of stapled peptides targeting phosphorylated GSK3β for regulating osteoclast differentiation |
| title_short | Rational design of stapled peptides targeting phosphorylated GSK3β for regulating osteoclast differentiation |
| title_sort | rational design of stapled peptides targeting phosphorylated gsk3β for regulating osteoclast differentiation |
| topic | Chemistry |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9049898/ https://www.ncbi.nlm.nih.gov/pubmed/35492160 http://dx.doi.org/10.1039/d0ra00008f |
| work_keys_str_mv | AT liutairong rationaldesignofstapledpeptidestargetingphosphorylatedgsk3bforregulatingosteoclastdifferentiation AT congwei rationaldesignofstapledpeptidestargetingphosphorylatedgsk3bforregulatingosteoclastdifferentiation AT yelei rationaldesignofstapledpeptidestargetingphosphorylatedgsk3bforregulatingosteoclastdifferentiation AT xuxike rationaldesignofstapledpeptidestargetingphosphorylatedgsk3bforregulatingosteoclastdifferentiation AT liaoxiufei rationaldesignofstapledpeptidestargetingphosphorylatedgsk3bforregulatingosteoclastdifferentiation AT xiegang rationaldesignofstapledpeptidestargetingphosphorylatedgsk3bforregulatingosteoclastdifferentiation AT chengzhaoxi rationaldesignofstapledpeptidestargetingphosphorylatedgsk3bforregulatingosteoclastdifferentiation AT huhonggang rationaldesignofstapledpeptidestargetingphosphorylatedgsk3bforregulatingosteoclastdifferentiation AT lixiang rationaldesignofstapledpeptidestargetingphosphorylatedgsk3bforregulatingosteoclastdifferentiation AT liaohongli rationaldesignofstapledpeptidestargetingphosphorylatedgsk3bforregulatingosteoclastdifferentiation |