Autores
Beate Saeger, Hans-Peter Schmitt-Wrede, Markus Dehnhardt, W Peter M Benten, Jürgen Krücken, Achim Harder, Georg von Samson-Himmelstjerna, Herbert Wiegand, Frank Wunderlich
Fecha de publicación
2001/5/1
Revista
The FASEB Journal
Volumen
15
Número
7
Páginas
1332-1334
Editor
Federation of American Societies for Experimental Biology
Descripción
PF1022A belongs to a new class of cyclodepsipeptides with broad anthelmintic activity. Here, we describe a novel target for PF1022A. Using PF1022A ligand immunoscreening of a cDNA library constructed from the parasitic nematode Haemonchus contortus, we identified a 3539 bp cDNA encoding a novel orphan heptahelical transmembrane 110 kDa‐receptor, termed HC110‐ R, similar to the mammalian G‐protein coupled receptor latrophilin. HC110‐R is localized at plasma membranes and in intracellular vesicles of HC110‐R‐transfected HEK‐293 cells. The ligand of latrophilin, a‐latrotoxin (LTX), binds to the extracellular N‐terminal region of HC110‐ R and induces influx of external Ca2+ through Cd2+‐ and nifedipine‐blockable Ca2+ channels. PF1022A also binds to the N‐terminus of HC110‐R and acts as an antagonist to LTX signaling in HC110‐R transfected HEK‐293 cells.
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