Alanine scan of endothelin: Importance of aromatic residues

  title={Alanine scan of endothelin: Importance of aromatic residues},
  author={James P Tam and Wen Liu and J Jillian Zhang and Mauro Galantino and Roberto de Castiglione},
A systematic approach to map the functional important determinants of endothelin-1 (ET) by an alanine scan is described. Studies on the in vitro receptor binding affinity and on the agonist contracting activity defined that residues Asp8, Tyr13, Phe14, Leu17, and Trp21 were of major biological significance. A striking observation was that four out of these five sites were hydrophobic amino acids. Ala analogues of the aromatic residues at position 13, 14, and 21 displayed sharply reduced… CONTINUE READING