Design, synthesis, and activity evaluation of novel erythropoietin mimetic peptides.
Bioorg Med Chem Lett
; 28(18): 3038-3041, 2018 10 01.
Article
em En
| MEDLINE
| ID: mdl-30097369
ABSTRACT
The approval of the erythropoietin (EPO) mimetic peptide drug peginesatide in 2012 was a breakthrough for the treatment of secondary anemia. However, due to severe allergic reactions, peginesatide was recalled a year later. In this study, 12 novel peptides were designed and synthesized by substituting specific amino acids of the monomeric peptide in peginesatide, with the aim of obtaining new EPO mimetic peptides with higher activities and lower side effects than the parent compound. Their cell proliferation activities were evaluated, and the structure-activity relationships were analyzed. Five compounds had equal cell proliferation activity to the control peptide. Among them, one compound showed a higher in vivo activity than the control peptide, with no obvious side effects.
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Base de dados:
MEDLINE
Assunto principal:
Peptídeos
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Desenho de Fármacos
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Eritroblastos
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article