secErbB4-26/549 antagonizes ligand-induced ErbB4 tyrosine phosphorylation.
ErbB4 is a member of the ErbB family of receptor tyrosine kinases. Because of a paucity of appropriate pharmacologic tools, little is known about ErbB4 functions in vivo. In response to this need, we hypothesized that a recombinant form of the extracellular domain of ErbB4 would antagonize ligand-induced receptor tyrosine phosphorylation and subsequent downstream signaling and could be used to probe ErbB4 function. Indeed, we show here that one such ErbB4 protein, secErbB4-26/549, is a potent inhibitor of ligand-induced ErbB4 tyrosine phosphorylation and of ligand-induced ErbB4 coupling to biological responses. Furthermore, we demonstrate that secErbB4-26/549 antagonizes ligand-induced ErbB4 signaling by acting as a ligand sink. Thus, secErbB4-26/549 is suitable for elucidating the effects of ErbB4 ligand-induced ErbB signaling in a variety of biological contexts.
Gilmore
Jennifer L
JL
Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University School of Pharmacy, West Lafayette, IN 47907-1333, USA.
Riese
David J
DJ
D000818:Animals; D018929:Cell Culture Techniques; D066246:ErbB Receptors / Q000502:physiology*; D007313:Insecta; D008024:Ligands; D010446:Peptide Fragments / Q000494:pharmacology*; D010766:Phosphorylation; D066247:Receptor, ErbB-4; D015398:Signal Transduction; D014443:Tyrosine / Q000378:metabolism*
D008024:Ligands; D010446:Peptide Fragments; D014443:Tyrosine; D066246:ErbB Receptors; D066247:Receptor, ErbB-4; C500229:secErbB4-26-549