Form Matters: Stable Helical Foldamers Preferentially Target Human Monocytes and Granulocytes.
ChemMedChem
; 12(4): 337-345, 2017 02 20.
Article
em En
| MEDLINE
| ID: mdl-28067470
ABSTRACT
Some hybrid foldamers of various length, all containing the (4R,5S)-4-carboxy-5-methyloxazolidin-2-one (d-Oxd) moiety alternating with an l-amino acid (l-Val, l-Lys, or l-Ala), were prepared in order to study their preferred conformations and to evaluate their biological activity. Surprisingly, only the longer oligomers containing l-Ala fold into well-established helices, whereas all the other oligomers give partially unfolded turn structures. Nevertheless, they all show good biocompatibility, with no detrimental effects up to 64â
µm. After equipping some selected foldamers with the fluorescent tag rhodamineâ
B, a quantitative analysis was performed by dose- and time-response fluorescence-activated cell sorting (FACS) assays with human HeLa cells and primary blood lymphocytes, granulocytes, and monocytes. Among the cell types analyzed, the oligomers associated with monocytes and granulocytes with greatest efficacy, still visible after 24â
h incubation. This effect is even more pronounced for foldamers that are able to form stable helices.
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Base de dados:
MEDLINE
Assunto principal:
Materiais Biocompatíveis
/
Monócitos
/
Peptoides
/
Granulócitos
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article