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Subtilisin and α-chymotrypsin catalyzed synthesis of peptides containing arginine and lysine p-nitroanilides as c-terminal moieties

✍ Scribed by Valentin M. Stepanov; Elena Yu. Terent'eva; Tatiana L. Voyushina; Mikhail Yu. Gololobov


Book ID
103992121
Publisher
Elsevier Science
Year
1995
Tongue
English
Weight
612 KB
Volume
3
Category
Article
ISSN
0968-0896

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✦ Synopsis


Almtract---p-Nitroanilides of N-acylated di-, tri-and tetrapeptides with C-terminal arginine or lysine residues have been obtained, as a rule with good yields, via acylation of arginine or lysine p-nitroanilides by methyl esters of respective N-acylated peptides, catalyzed by subtilisin or ct-ehymotrypsin. The synthesis might be performed by two routes---by reaction in waterorganic solvent mixtures, catalyzed by dissolved enzyme, or by condensation of the components in organic solvents with low water content in the presence of any enzyme distributed over a silica support surface. The second approach seems to be preferable due to suppression of hydrolytic side reactions and improved stability of an enzyme. Subtilisin 72 is especially effective as a catalyst for the acylation of p-nitroanilides by N-protected tripeptide methyl esters---the derivatives capable of occupying the S t, S 2 and S 3 subsites of its extended binding site. Even dipeptide esters with D-amino acids in P2 position can be applied for p-nitroanilide acylation. The efficiency of ¢z-chymotrypsin as a catalyst for peptide synthesis is more limited due to restricted specificity of this enzyme.