Combined Role of Two Tryptophane Residues of α-Factor Pheromone 


Vol. 34,  No. 2, pp. 600-608, Feb.  2013
10.5012/bkcs.2013.34.2.600


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  Abstract

Amide analogs of tridecapeptide α-factor (WHWLQLKPGQPMYCONH2) of Saccharomyces cerevisiae, in which Trp at position 1 and 3 were replaced with other residues, were synthesized to ascertain whether cooperative interactions between two Trp residues occurred upon binding with its receptor. Analogs containing Ala or Aib at position 3 of the peptide [Ala3]α-factor amide (2) and [Aib3]α-factor amide (5) exhibited greater decreases in bioactivity than analogs with same residue at position one [Ala1]α-factor amide (1) and [Aib1]α- factor amide (4), reflecting that Trp3 may plays more important role than Trp1 for agonist activity. Analogs containing Ala or Aib in both position one and three 3, 6 exhibited complete loss of bioactivity, emphasizing both the essential role and the combined role of two indole rings for triggering cell signaling. In contrast, double substituted analog with D-Trp in both positions 9 exhibited greater activity than single substituted analog with D-Trp 8 or deleted analog 7, reflecting the combined contribution of two tryptophane residues of α-factor ligand to activation of Ste2p through interaction with residue Tyr266 and importance of the proper parallel orientation of two indole rings for efficient triggering of signal G protein coupled activation. Among ten amide analogs, [Ala1,3]α-factor amide (3), [Aib1,3]α-factor amide (6), [D-Trp3]α-factor amide (8) and [des-Trp1,Phe3]α-factor amide (10) were found to have antagonistic activity. Analogs 3 and 6 showed greater antagonistic activity than analogs 8 and 10.

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  Cite this article

[IEEE Style]

E. Y. Hong and N. J. Hong, "Combined Role of Two Tryptophane Residues of α-Factor Pheromone," Bulletin of the Korean Chemical Society, vol. 34, no. 2, pp. 600-608, 2013. DOI: 10.5012/bkcs.2013.34.2.600.

[ACM Style]

Eun Young Hong and Nam Joo Hong. 2013. Combined Role of Two Tryptophane Residues of α-Factor Pheromone. Bulletin of the Korean Chemical Society, 34, 2, (2013), 600-608. DOI: 10.5012/bkcs.2013.34.2.600.

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ISSN(Print) 0253-2964
ISSN(Online) 1229-5949