A photocleavable masked nuclear-receptor ligand enables temporal control of C.â
elegans development.
Angew Chem Int Ed Engl
; 53(8): 2110-3, 2014 Feb 17.
Article
en En
| MEDLINE
| ID: mdl-24453122
ABSTRACT
The development and lifespan of C.â
elegans are controlled by the nuclear hormone receptor DAF-12, an important model for the vertebrate vitaminâ
D and liverâ
X receptors. As with its mammalian homologues, DAF-12 function is regulated by bile acid-like steroidal ligands; however, tools for investigating their biosynthesis and function inâ
vivo are lacking. A flexible synthesis for DAF-12 ligands and masked ligand derivatives that enable precise temporal control of DAF-12 function was developed. For ligand masking, photocleavable amides of 5-methoxy-N-methyl-2-nitroaniline (MMNA) were introduced. MMNA-masked ligands are bioavailable and after incorporation into the worm, brief UV irradiation can be used to trigger the expression of DAF-12 target genes and initiate development from dauer larvae into adults. The inâ
vivo release of DAF-12 ligands and other small-molecule signals by using photocleavable MMNA-masked ligands will enable functional studies with precise spatial and temporal resolution.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Caenorhabditis elegans
/
Receptores Citoplasmáticos y Nucleares
/
Proteínas de Caenorhabditis elegans
/
Amidas
/
Ligandos
Límite:
Animals
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Año:
2014
Tipo del documento:
Article