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Durhamycin A, a potent inhibitor of HIV Tat transactivation.

Publication ,  Journal Article
Jayasuriya, H; Lingham, RB; Graham, P; Quamina, D; Herranz, L; Genilloud, O; Gagliardi, M; Danzeisen, R; Tomassini, JE; Zink, DL; Guan, Z; Singh, SB
Published in: J Nat Prod
August 2002

Tat is a small HIV protein essential for both viral replication and the progression of HIV disease. In our efforts to discover Tat inhibitors from natural product screening of microbial fermentation extracts, we discovered durhamycin A (1) as a potent inhibitor (IC(50) = 4.8 nM) of Tat transactivation. Detailed NMR and MS/MS studies were utilized to elucidate the structure of 1 as a new member of the aureolic acid family of antibiotics. It consists of tetrasaccharide and disaccharide moieties attached to the aglycone, which is hitherto unknown in the aureolic acid family. Three other novel analogues, durhamycin B (2), compound (3), and the aglycone (4), were also discovered or chemically prepared that were less potent than durhamycin A.

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Published In

J Nat Prod

DOI

ISSN

0163-3864

Publication Date

August 2002

Volume

65

Issue

8

Start / End Page

1091 / 1095

Location

United States

Related Subject Headings

  • tat Gene Products, Human Immunodeficiency Virus
  • Substrate Specificity
  • Structure-Activity Relationship
  • Protein Binding
  • Plicamycin
  • Molecular Structure
  • Medicinal & Biomolecular Chemistry
  • Mass Spectrometry
  • Magnetic Resonance Spectroscopy
  • Inhibitory Concentration 50
 

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Jayasuriya, H., Lingham, R. B., Graham, P., Quamina, D., Herranz, L., Genilloud, O., … Singh, S. B. (2002). Durhamycin A, a potent inhibitor of HIV Tat transactivation. J Nat Prod, 65(8), 1091–1095. https://doi.org/10.1021/np010642f
Jayasuriya, Hiranthi, Russell B. Lingham, Pia Graham, Donette Quamina, Lucia Herranz, Olga Genilloud, Magda Gagliardi, et al. “Durhamycin A, a potent inhibitor of HIV Tat transactivation.J Nat Prod 65, no. 8 (August 2002): 1091–95. https://doi.org/10.1021/np010642f.
Jayasuriya H, Lingham RB, Graham P, Quamina D, Herranz L, Genilloud O, et al. Durhamycin A, a potent inhibitor of HIV Tat transactivation. J Nat Prod. 2002 Aug;65(8):1091–5.
Jayasuriya, Hiranthi, et al. “Durhamycin A, a potent inhibitor of HIV Tat transactivation.J Nat Prod, vol. 65, no. 8, Aug. 2002, pp. 1091–95. Pubmed, doi:10.1021/np010642f.
Jayasuriya H, Lingham RB, Graham P, Quamina D, Herranz L, Genilloud O, Gagliardi M, Danzeisen R, Tomassini JE, Zink DL, Guan Z, Singh SB. Durhamycin A, a potent inhibitor of HIV Tat transactivation. J Nat Prod. 2002 Aug;65(8):1091–1095.
Journal cover image

Published In

J Nat Prod

DOI

ISSN

0163-3864

Publication Date

August 2002

Volume

65

Issue

8

Start / End Page

1091 / 1095

Location

United States

Related Subject Headings

  • tat Gene Products, Human Immunodeficiency Virus
  • Substrate Specificity
  • Structure-Activity Relationship
  • Protein Binding
  • Plicamycin
  • Molecular Structure
  • Medicinal & Biomolecular Chemistry
  • Mass Spectrometry
  • Magnetic Resonance Spectroscopy
  • Inhibitory Concentration 50