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Synthesis of homologous peptides using fragment condensation: analogs of an HIV proteinase substrate.

作者信息

Bláha I, Nemec J, Tözsér J, Oroszlan S

机构信息

Laboratory of Molecular Virology and Carcinogenesis, PRI/DynCorp., NCI-Frederick Cancer Research and Development Center, MD.

出版信息

Int J Pept Protein Res. 1991 Nov;38(5):453-8. doi: 10.1111/j.1399-3011.1991.tb01526.x.

DOI:10.1111/j.1399-3011.1991.tb01526.x
PMID:1802863
Abstract

Two protected peptides Boc-Val-Ser(Bzl)-Gln-Asn-Tyr(BrZ)OH and Boc-Val-Ser(Bzl)-Gln-Asn-Tyr(BrZ)-ProOH were synthesized on a resin substituted by 9-(hydroxymethyl)-2-fluoreneacetic acid. After cleavage with piperidine/DMF, desalting, and activation, these peptides were used for the synthesis of 11 analogs of an HIV proteinase nonapeptide substrate Val-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-NH2 using fragment condensation in solid phase. The fragment condensation was made in an ultrasonic bath. Using only 2 equivalents of the activated peptide in a DMF solution, this reaction was complete in 2 h. All nonapeptides were assayed as substrates for HIV-1 and HIV-2 proteinases.

摘要

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