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Broad Antiretroviral Activity and Resistance Profile of the Novel Human Immunodeficiency Virus Integrase Inhibitor Elvitegravir (JTK-303/GS-9137)
The antiviral activity and resistance profile in vitro of a novel IN inhibitor, elvitegravir (EVG) (also known as JTK-303/GS-9137), currently being developed for the treatment of HIV-1 infection are described, suggesting that IN inhibitors bind to a conformationally conserved region of various retroviral IN enzymes and are an ideal drug for a range of Retroviral infections.
Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140.
Mutations Conferring Resistance to Human Immunodeficiency Virus Type 1 Fusion Inhibitors Are Restricted by gp41 and Rev-Responsive Element Functions
HIV acquired resistance to C34 by mutations in N-HR, which directly interacted with C34, however, since this region also encoded the RRE, additional mutations were required to maintain viral replication.
Amino Acid Mutation N348I in the Connection Subdomain of Human Immunodeficiency Virus Type 1 Reverse Transcriptase Confers Multiclass Resistance to Nucleoside and Nonnucleoside Reverse Transcriptase…
Molecular modeling analysis shows that residue 348 is proximal to the NNRTI-binding pocket and to a flexible hinge region at the base of the p66 thumb that may be affected by the N348I mutation, which further highlight the role of connection subdomain residues in drug resistance.
Remodeling of gp41-C34 peptide leads to highly effective inhibitors of the fusion of HIV-1 with target cells.
Current research on chronic active Epstein–Barr virus infection in Japan
- S. Fujiwara, H. Kimura, H. Wakiguchi
- Medicine, BiologyPediatrics international : official journal of…
- 1 April 2014
The current understanding of CA EBV is summarized and the recent progress of CAEBV research in Japan is described, which shows that the geographical distribution is markedly uneven and most cases have been reported from Japan and other East Asian countries.
Epigallocatechin Gallate Inhibits the HIV Reverse Transcription Step
EGCG appears to act mainly as an allosteric reverse transcriptase inhibitor with mechanisms different from those of currently approved NNRTIs that directly interact with the NN RTI binding pocket, and is a good candidate for use as an additional or supportive anti-HIV agent derived from natural plants.
Clinical relevance of substitutions in the connection subdomain and RNase H domain of HIV-1 reverse transcriptase from a cohort of antiretroviral treatment-naïve patients.
Antileukemic activity and mechanism of action of cordycepin against terminal deoxynucleotidyl transferase-positive (TdT+) leukemic cells.
Mechanism of Inhibition of HIV-1 Reverse Transcriptase by 4′-Ethynyl-2-fluoro-2′-deoxyadenosine Triphosphate, a Translocation-defective Reverse Transcriptase Inhibitor*
- E. Michailidis, B. Marchand, S. Sarafianos
- Biology, ChemistryThe Journal of Biological Chemistry
- 16 October 2009
4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA), a nucleoside analog that retains a 3′-hydroxyl moiety, inhibited HIV-1 replication in activated peripheral blood mononuclear cells with an EC50 of 0.05 nm, a potency several orders of magnitude better than any of the current clinically used NRTIs.