| Title: | Novel antagonist to agonist switch in chimeric G protein-coupled alpha-factor peptide receptors |
| Address: | "Department of Cell Biology, Albert Einstein College of Medicine, Bronx, NY 10461" |
| Journal Title: | Biochem Biophys Res Commun |
| ISSN/ISBN: | 0006-291X (Print) 0006-291X (Linking) |
| Abstract: | "The alpha-factor analog desTrp1,Ala3 alpha-factor (dTA-alpha-factor) acts as an antagonist for both the S. cerevisiae alpha-factor receptor (c-alpha-FR) and the S. kluyveri alpha-factor receptor (k-alpha FR). Chimeric alpha-factor receptors in which a portion (residues 250-303) of the seven hydrophobic segments were derived from the k-alpha FR and the rest from c-alpha FR conferred potent activation of cellular responses by dTA-alpha-factor including induction of FUS1 expression without significantly affecting binding. Chimeric receptors with all hydrophobic segments derived from one receptor did not express sensitivity. We propose that dTA-alpha-factor represents an antagonist that that has an activation energy barrier to activating c-alpha FR and k-alpha FR but which retains a latent potential to act as an agonist" |
| Keywords: | "Binding, Competitive Escherichia coli/drug effects/growth & development GTP-Binding Proteins/biosynthesis/*metabolism Kinetics Mating Factor Peptides/drug effects/*pharmacology Pheromones/*pharmacology Receptors, Mating Factor Receptors, Peptide/*agonists;" |
| Notes: | "MedlineSen, M Marsh, L eng GM43365/GM/NIGMS NIH HHS/ P30 CA13330/CA/NCI NIH HHS/ Comparative Study Research Support, U.S. Gov't, P.H.S. 1995/02/15 Biochem Biophys Res Commun. 1995 Feb 15; 207(2):559-64. doi: 10.1006/bbrc.1995.1224" |
