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Integramides A and B, two novel non-ribosomal linear peptides containing nine C(alpha)-methyl amino acids produced by fungal fermentations that are inhibitors of HIV-1 integrase.

Publication ,  Journal Article
Singh, SB; Herath, K; Guan, Z; Zink, DL; Dombrowski, AW; Polishook, JD; Silverman, KC; Lingham, RB; Felock, PJ; Hazuda, DJ
Published in: Org Lett
May 2, 2002

[structure: see text]. Integramides A and B are two novel 16-mer linear peptides rich in C(alpha)-methyl amino acids that were isolated from fungal extracts of Dendrodochium sp. by employing a bioassay-guided isolation procedure using recombinant HIV-1 integrase. The structure and stereochemistry were elucidated by a combination of 2D NMR and ESI- and FAB-MS including MS/MS studies and by Marfey's method. Integramides A and B inhibited the coupled reaction of HIV-1 integrase with IC50 values of 17 and 10 microM, respectively.

Duke Scholars

Published In

Org Lett

DOI

ISSN

1523-7060

Publication Date

May 2, 2002

Volume

4

Issue

9

Start / End Page

1431 / 1434

Location

United States

Related Subject Headings

  • Peptides
  • Organic Chemistry
  • Oligopeptides
  • HIV Integrase Inhibitors
  • HIV Integrase
  • Fungi
  • Fermentation
  • Chromatography, High Pressure Liquid
  • 03 Chemical Sciences
 

Citation

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Singh, S. B., Herath, K., Guan, Z., Zink, D. L., Dombrowski, A. W., Polishook, J. D., … Hazuda, D. J. (2002). Integramides A and B, two novel non-ribosomal linear peptides containing nine C(alpha)-methyl amino acids produced by fungal fermentations that are inhibitors of HIV-1 integrase. Org Lett, 4(9), 1431–1434. https://doi.org/10.1021/ol025540a
Singh, Sheo B., Kithsiri Herath, Ziqiang Guan, Deborah L. Zink, Anne W. Dombrowski, Jon D. Polishook, Keith C. Silverman, Russell B. Lingham, Peter J. Felock, and Daria J. Hazuda. “Integramides A and B, two novel non-ribosomal linear peptides containing nine C(alpha)-methyl amino acids produced by fungal fermentations that are inhibitors of HIV-1 integrase.Org Lett 4, no. 9 (May 2, 2002): 1431–34. https://doi.org/10.1021/ol025540a.
Singh SB, Herath K, Guan Z, Zink DL, Dombrowski AW, Polishook JD, Silverman KC, Lingham RB, Felock PJ, Hazuda DJ. Integramides A and B, two novel non-ribosomal linear peptides containing nine C(alpha)-methyl amino acids produced by fungal fermentations that are inhibitors of HIV-1 integrase. Org Lett. 2002 May 2;4(9):1431–1434.
Journal cover image

Published In

Org Lett

DOI

ISSN

1523-7060

Publication Date

May 2, 2002

Volume

4

Issue

9

Start / End Page

1431 / 1434

Location

United States

Related Subject Headings

  • Peptides
  • Organic Chemistry
  • Oligopeptides
  • HIV Integrase Inhibitors
  • HIV Integrase
  • Fungi
  • Fermentation
  • Chromatography, High Pressure Liquid
  • 03 Chemical Sciences