Studies on the total synthesis of an A7,B7-dicarbainsulin. III. Assembly of segments and generation of biological activity |
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Authors: | G Videnov K Büttner M Casaretto J F?hles H G Gattner S Stoev D Brandenburg |
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Institution: | Institute of Molecular Biology, Bulgarian Academy of Sciences, Sofia. |
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Abstract: | As a further contribution to the synthesis of an insulin analogue with a stable A7-B7 interchain bond, the synthesis of A(8-21) by solution methods, and of B(9-25) as well as 7-(2,7-diaminosuberic acid)]B(1-8) by solid phase methods is described. In the latter compound, the amino group of the diaminosuberic acid residue was acylated with A(1-6), and the resulting "U-peptide" sequentially elongated with the C-terminal A- and finally B-chain sequences. The conversion of the product into the disulfide moiety gave a mixture which could not be resolved by currently available methods. However, the low biological activity of the crude product indicates that the A7-B7 disulfide bond is not crucially important for the activity of insulin. |
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