Synthesis and Biological Evaluation of Fluorescent Bryostatin Analogues.
Chembiochem
; 19(8): 877-889, 2018 04 16.
Article
em En
| MEDLINE
| ID: mdl-29424951
ABSTRACT
To investigate the cellular distribution of tumor-promoting vs. non-tumor-promoting bryostatin analogues, we synthesized fluorescently labeled variants of two bryostatin derivatives that have previously shown either phorbol ester-like or bryostatin-like biological activity in U937 leukemia cells. These new fluorescent analogues both displayed high affinity for protein kinaseâ
C (PKC) binding and retained the basic properties of the parent unlabeled compounds in U937 assays. The fluorescent compounds showed similar patterns of intracellular distribution in cells, however; this argues against an existing hypothesis that various patterns of intracellular distribution are responsible for differences in biological activity. Upon further characterization, the fluorescent compounds revealed a slow rate of cellular uptake; correspondingly, they showed reduced activity for cellular responses that were only transient upon treatment with phorbol ester or bryostatinâ
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Base de dados:
MEDLINE
Assunto principal:
Briostatinas
/
Corantes Fluorescentes
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article