Synthesis of a macrocyclic rhodamine 110 enzyme substrate as an intracellular probe for caspase 3 activity

Autor:	John J. Naleway, Rod C. Schutte, Anthony P. Guzikowski, Christina T. Shipp
Rok vydání:	2000
Předmět:	chemistry.chemical_classification Chemistry Organic Chemistry Substrate (chemistry) Caspase 3 Biochemistry Fluorescence law.invention Enzyme Apoptosis law Drug Discovery Recombinant DNA Amine gas treating Intracellular
Zdroj:	Tetrahedron Letters. 41:4733-4735
ISSN:	0040-4039
DOI:	10.1016/s0040-4039(00)00708-5
Popis:	The synthesis of the macrocyclic rhodamine 110 caspase 3 substrate 8 is described. The key step is a high dilution intramolecular cyclization reaction of an in situ generated primary amine with a 4-nitrophenyl ester. Substrate 8 reacts with recombinant caspase 3 to yield a fluorescent signal but virtually no signal is detected in the absence of caspase 3 or in the presence of the caspase 3 inhibitor Ac-DEVD-CHO. Notably, 8 selectively stains live cells that have been induced to undergo apoptosis with etoposide.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::37bbf6e1bae20d505030d3290cab7657 https://doi.org/10.1016/s0040-4039(00)00708-5 Zobrazit plný text záznamu Full Text from ScienceDirect