Document Detail

Anti-Tat and anti-HIV activities of trimers of n-alkylglycines.
MedLine Citation:
PMID:  16405868     Owner:  NLM     Status:  MEDLINE    
Transcription of human immunodeficiency virus (HIV-1) is activated by viral Tat protein which regulates HIV-LTR transcription and elongation. In the present report, the evaluation of the anti-Tat activity of a combinatorial library composed of 5120 N-trialkylglycines is reported. The antiviral activity was studied through luciferase-based assays targeting the HIV-1 promoter activation induced by the HIV-1 Tat protein. We identified five peptoids with specific anti-HIV-1 Tat activity; none of these peptoids affected the binding of HIV-1 Tat protein to the viral TAR RNA. Using a recombinant-virus assay in which luciferase activity correlates with the rate of HIV-1 transcription we have detected that one of the five selected peptoids, NC37-37-15C, is a potent inhibitor of HIV-1-LTR transcription in both primary T lymphocytes and transformed cell lines. The inhibitory effect of NC37-37-15C, which is additive with azidothymidine (AZT), correlates with its ability to inhibit CTD phosphorylation and shows a suitable profile for development of novel anti-HIV-1 drugs. Likewise, the structural simplicity of N-alkylglycine oligomers makes these peptidomimetics amenable to structural manipulation, thus facilitating the optimisation of lead molecules for drug-like properties.
Nieves Márquez; Rocío Sancho; Antonio Macho; Alejandra Moure; Isabel Masip; Angel Messeguer; Eduardo Muñoz
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2006-01-06
Journal Detail:
Title:  Biochemical pharmacology     Volume:  71     ISSN:  0006-2952     ISO Abbreviation:  Biochem. Pharmacol.     Publication Date:  2006 Feb 
Date Detail:
Created Date:  2006-01-27     Completed Date:  2006-03-23     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  0101032     Medline TA:  Biochem Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  596-604     Citation Subset:  IM    
Departamento de Biología Celular, Fisiología e Inmunología, Universidad de Córdoba, Facultad de Medicina, Avda. de Menéndez Pidal s/n, E-14004 Córdoba, Spain.
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MeSH Terms
Anti-HIV Agents / pharmacology*
Base Sequence
Combinatorial Chemistry Techniques
DNA Primers
Electrophoretic Mobility Shift Assay
Gene Products, tat / antagonists & inhibitors*
Glycine / analogs & derivatives,  chemistry,  pharmacology*
HIV Long Terminal Repeat
HIV-1 / drug effects
Jurkat Cells
Molecular Structure
Polymers / chemistry,  pharmacology*
tat Gene Products, Human Immunodeficiency Virus
Reg. No./Substance:
0/Anti-HIV Agents; 0/DNA Primers; 0/Gene Products, tat; 0/Polymers; 0/tat Gene Products, Human Immunodeficiency Virus; 56-40-6/Glycine

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