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Blocking HIV-1 entry by a gp120 surface binding inhibitor.

Publication ,  Journal Article
Tsou, LK; Chen, C-H; Dutschman, GE; Cheng, Y-C; Hamilton, AD
Published in: Bioorg Med Chem Lett
May 1, 2012
Published version (DOI) Link to item

We report the mode of action of a proteomimetic compound that binds to the exterior surface of gp120 and blocks HIV-1 entry into cells. Using a one cycle time-of-addition study and antibody competition binding studies, we have determined that the compound blocks HIV-1 entry through modulation of key protein-protein interactions mediated by gp120. The compound exhibits anti-HIV-1 replication activities against several pseudotype viruses derived from primary isolates and the resistant strains isolated from existing drug candidates with equal potency. Together, these data provide evidence that the proteomimetic compound represents a novel class of HIV-1 viral entry inhibitor that functions through protein surface recognition in analogy to an antibody.

Duke Scholars

Chin-Ho Chen
Author Chin-Ho Chen Surgery, Surgical Sciences

Published In

Bioorg Med Chem Lett

DOI

10.1016/j.bmcl.2012.02.079

EISSN

1464-3405

Publication Date

May 1, 2012

Volume

22

Issue

9

Start / End Page

3358 / 3361

Location

England

Related Subject Headings

  • Virus Replication
  • Virus Internalization
  • Protein Binding
  • Medicinal & Biomolecular Chemistry
  • Humans
  • HIV-1
  • HIV Envelope Protein gp120
  • Binding, Competitive
  • Anti-HIV Agents
  • 3405 Organic chemistry
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Tsou, L. K., Chen, C.-H., Dutschman, G. E., Cheng, Y.-C., & Hamilton, A. D. (2012). Blocking HIV-1 entry by a gp120 surface binding inhibitor. Bioorg Med Chem Lett, 22(9), 3358–3361. https://doi.org/10.1016/j.bmcl.2012.02.079
Tsou, Lun K., Chin-Ho Chen, Ginger E. Dutschman, Yung-Chi Cheng, and Andrew D. Hamilton. “Blocking HIV-1 entry by a gp120 surface binding inhibitor.” Bioorg Med Chem Lett 22, no. 9 (May 1, 2012): 3358–61. https://doi.org/10.1016/j.bmcl.2012.02.079.
Tsou LK, Chen C-H, Dutschman GE, Cheng Y-C, Hamilton AD. Blocking HIV-1 entry by a gp120 surface binding inhibitor. Bioorg Med Chem Lett. 2012 May 1;22(9):3358–61.
Tsou, Lun K., et al. “Blocking HIV-1 entry by a gp120 surface binding inhibitor.” Bioorg Med Chem Lett, vol. 22, no. 9, May 2012, pp. 3358–61. Pubmed, doi:10.1016/j.bmcl.2012.02.079.
Tsou LK, Chen C-H, Dutschman GE, Cheng Y-C, Hamilton AD. Blocking HIV-1 entry by a gp120 surface binding inhibitor. Bioorg Med Chem Lett. 2012 May 1;22(9):3358–3361.
Journal cover image

Published In

Bioorg Med Chem Lett

DOI

10.1016/j.bmcl.2012.02.079

EISSN

1464-3405

Publication Date

May 1, 2012

Volume

22

Issue

9

Start / End Page

3358 / 3361

Location

England

Related Subject Headings

  • Virus Replication
  • Virus Internalization
  • Protein Binding
  • Medicinal & Biomolecular Chemistry
  • Humans
  • HIV-1
  • HIV Envelope Protein gp120
  • Binding, Competitive
  • Anti-HIV Agents
  • 3405 Organic chemistry