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Influence of Acyclic Nucleoside Phosphonate Antivirals on Gene Expression of Chemokine Receptors CCR5 and CXCR4
- 1.0443963 - ÚOCHB 2016 RIV CZ eng J - Journal Article
Potměšil, P. - Holý, Antonín - Zídek, Zdeněk
Influence of Acyclic Nucleoside Phosphonate Antivirals on Gene Expression of Chemokine Receptors CCR5 and CXCR4.
Folia Biologica. Roč. 61, č. 1 (2015), s. 1-7. ISSN 0015-5500. E-ISSN 0015-5500
R&D Projects: GA ČR GA305/03/1470; GA MŠMT 1M0508
Institutional support: RVO:61388963 ; RVO:68378041
Keywords : acyclic nucleoside phosphonate * HIV * CCR5 * CXCR4 * cytokine * RT-PCR
Subject RIV: CC - Organic Chemistry; FR - Pharmacology ; Medidal Chemistry (UEM-P)
Impact factor: 0.833, year: 2015
Acyclic nucleoside phosphonates (ANPs) are potent antiviral agents effective against replication of DNA viruses and retroviruses including human immunodeficiency virus (HIV). Prototype compound 9-(R)-[2-(phosphonomethoxy)propyl]adenine (tenofovir) is a principal component of drugs widely used in the treatment of HIV infection (Viread, Truvada). Besides their antimetabolic mode of action, ANPs possess immunomodulatory properties. A number of them have been previously found to stimulate secretion of cytokines and anti-HIV effective chemokines. In the present pilot experiments we analysed the in vitro effects of ANPs on the expression of chemokine receptors CCR5 and CXCR4 that are co-receptors of HIV-1 entry in cells. The impact of ANPs was investigated at the level of gene transcription of mRNA in mouse lymphocytes and macrophages using the RT-PCR method. The following compounds were included in the study: 9-(R)-[2-(phosphonomethoxy)propyl]adenine (tenofovir), N-6-cyclopropyl-(R)-9-[2-(phosphonomethoxy)-propyl]2,6-diaminopurine, N-6-cyclopentyl-(R)-9-[2-(phosphonomethoxy)propyl]2,6-diaminopurine, N-6-dimethylaminoethyl-(R)-9-[2-(phosphonomethoxy)propyl]2,6-diaminopurine, N-6-cyclopentyl-9-[2-(phosphonomethoxy)ethyl]2,6-diaminopurine, N-6-isobutyl-9-[2-(phosphonomethoxy)ethyl]2,6-diaminopurine. Gene transcription of chemokine receptors CCR5 and CXCR4 was not affected after application of these acyclic nucleoside phosphonate antivirals.
Permanent Link: http://hdl.handle.net/11104/0246598
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