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J Pept Res

Title:		Position one analogs of the Saccharomyces cerevisiae tridecapeptide pheromone
Author(s):		Zhang YL; Lu HF; Becker JM; Naider F;
Address:		"Department of Chemistry, College of Staten Island of the City University of New York, USA"
Journal Title:		J Pept Res
Year:		1997
Volume:		50
Issue:		5
Page Number:		319 - 328
DOI:		10.1111/j.1399-3011.1997.tb01190.x
ISSN/ISBN:		1397-002X (Print) 1397-002X (Linking)
Abstract:		"Analogs of the Saccharomyces cerevisiae alpha-mating factor [WHWLQLKPGQPMY], in which a variety of residues replaced Trp1 were synthesized and assayed for biological activity and receptor affinity. Analogs containing Gly or Leu or many different aromatic residues in position 1 of the peptide exhibited bioactivity in a growth arrest assay slightly greater than, or equal to, that of the parent pheromone, whereas the Glu1 and Lys1 analogs exhibited significantly lower bioactivity. Analogs with an aromatic replacement at position 1 had 3- to 6-fold lower receptor affinity than the parent peptide, whereas analogs with a hydrophilic residue at the N-terminus exhibited large reductions in receptor affinity with the peptide with Glu in position 1 showing a 120-fold reduction. N alpha-Acetylation had little effect on bioactivity but lowered receptor affinity by 20- to 40-fold. Amidation of the carboxyl terminus resulted in a 10-fold decrease in activity and a 160-fold decrease in receptor affinity. These results indicate that the alpha-factor receptor has a large hydrophobic binding pocket, possibly containing a negatively charged side-chain, which interacts with the N-terminus of alpha-factor. The lack of correlation between activity and binding and several analogs suggests that small residues near the N-terminus of alpha-factor may be very efficient in triggering isomerization of the receptor to its activated state in the first step of the signal transduction pathway"
Keywords:		Gene Expression Mating Factor Peptides/*chemistry/genetics Pheromones/*chemistry/genetics Saccharomyces cerevisiae/*genetics Signal Transduction/physiology;
Notes:		"MedlineZhang, Y L Lu, H F Becker, J M Naider, F eng GM 22086/GM/NIGMS NIH HHS/ GM 22087/GM/NIGMS NIH HHS/ Research Support, U.S. Gov't, P.H.S. Denmark 1997/12/24 J Pept Res. 1997 Nov; 50(5):319-28. doi: 10.1111/j.1399-3011.1997.tb01190.x"