Discovery of a Drug Lead Employing a Peptide Library: Inhibition of HIV-1 Tat and Viral Replication by the Tripeptide YPG-NH2

A library of the 8000 tripeptides derivable from coded amino acids was prepared in 20 sets of 400 using solid phase synthesis on a benzhydrylamine resin. The peptide mixtures, as C-terminal amides, were screened for inhibition of secreted alkaline phosphatase expression in a cellular (COS) system wh...

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Published in:Antiviral chemistry & chemotherapy 1994-04, Vol.5 (2), p.128-129
Main Authors: Coffen, D. L., Huang, T.-N., Ramer, S. E., West, R. C., Connell, E. V., Schutt, A. D., Hsu, M.-C.
Format: Article
Language:English
Subjects:
Alkaline phosphatase
Amides
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
CD4 antigen
HIV
Human immunodeficiency virus
Lymphocytes T
Medical sciences
Peptides
Pharmacology. Drug treatments
Replication
Solid phase methods
Tat gene
Tat protein
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container_end_page 129
container_issue 2
container_start_page 128
container_title Antiviral chemistry & chemotherapy
container_volume 5
creator Coffen, D. L.
Huang, T.-N.
Ramer, S. E.
West, R. C.
Connell, E. V.
Schutt, A. D.
Hsu, M.-C.
description A library of the 8000 tripeptides derivable from coded amino acids was prepared in 20 sets of 400 using solid phase synthesis on a benzhydrylamine resin. The peptide mixtures, as C-terminal amides, were screened for inhibition of secreted alkaline phosphatase expression in a cellular (COS) system wherein a transfected SeAP gene construct was under control of the HIV-1 LTR promoter, activated by the product of a cotransfected HIV Tat gene construct. Thus, YPG-NH2 was discovered as an inhibitor of HIV-1 Tat function and then shown to block HIV replication in a CD4+ T-cell line (CEM) with IC50 = 35μM.
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0956-3202
2040-2066
language eng
recordid cdi_proquest_journals_2342379403
source Publicly Available Content (ProQuest); SAGE Journals Online Archive
subjects Alkaline phosphatase
Amides
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
CD4 antigen
HIV
Human immunodeficiency virus
Lymphocytes T
Medical sciences
Peptides
Pharmacology. Drug treatments
Replication
Solid phase methods
Tat gene
Tat protein
title Discovery of a Drug Lead Employing a Peptide Library: Inhibition of HIV-1 Tat and Viral Replication by the Tripeptide YPG-NH2
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