scholarly journals Inhibitory effect of a lichen polysaccharide sulfate, GE-3-S, on the replication of human immunodeficiency virus(HIV) in vitro.

1989 ◽  
Vol 37 (9) ◽  
pp. 2410-2412 ◽  
Author(s):  
Kazuhiro HIRABAYASHI ◽  
Susumu IWATA ◽  
Masahiko ITO ◽  
Shirou SHIGETA ◽  
Takao NARUI ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Inhibitory Effect ◽  
Immunodeficiency Virus

scholarly journals Inhibitory effect of new antibiotic, pradimicin A on infectivity, cytopathic effect and replication of human immunodeficiency virus in vitro.

1988 ◽  
Vol 41 (11) ◽  
pp. 1708-1710 ◽  
Author(s):  
AKIKO TANABE ◽  
HIDEKI NAKASHIMA ◽  
OSAMU YOSHIDA ◽  
NAOKI YAMAMOTO ◽  
OSAMU TENMYO ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Cytopathic Effect ◽  
Inhibitory Effect ◽  
Immunodeficiency Virus

Anti-Human Immunodeficiency Virus (HIV) Activity of the Novel Antiviral Antibiotic Quartromicins which Enhance Inhibitory Effect of 3′-azido-2′,3′-dideoxythymidine (AZT) in vitro

1992 ◽  
Vol 3 (6) ◽  
pp. 345-349 ◽  
Author(s):  
A. Tanabe-Tochikura ◽  
H. Nakashima ◽  
T. Murakami ◽  
O. Tenmyo ◽  
T. Oki ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Specific Antigen ◽  
Antigen Expression ◽  
Antiviral Effect ◽  
Inhibitory Effect ◽  
Reverse Transcriptase Activity ◽  
The Novel ◽  
Avian Myeloblastosis Virus ◽  
Immunodeficiency Virus

Novel antiviral antibiotic quartromicins A1 and D1, isolated from Amycolatopsis orientalis, significantly inhibited human immunodeficiency virus (HIV)-induced cytopathic effect and virus specific antigen expression at concentrations of 25–100 μg ml−1 In MT-4 cells infected with HTLV-IIIB. The reverse transcriptase activity of disrupted HTLV-IIIB particles, recombinant HIV-1 enzyme, and purified avian myeloblastosis virus (AMV) enzyme were also significantly inhibited by quartromicins A1 and D1. The combined antiviral effect of quartromicin A1 and AZT on the replication of HIV in MT-4 cells was also examined. Quartromicin A1 synergistically enhanced the inhibitory effect of AZT as revealed by HIV-specific antigen expression.

scholarly journals TAK-652 Inhibits CCR5-Mediated Human Immunodeficiency Virus Type 1 Infection In Vitro and Has Favorable Pharmacokinetics in Humans

2005 ◽  
Vol 49 (11) ◽  
pp. 4584-4591 ◽  
Author(s):  
Masanori Baba ◽  
Katsunori Takashima ◽  
Hiroshi Miyake ◽  
Naoyuki Kanzaki ◽  
Koichiro Teshima ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Chemokine Receptors ◽  
Inhibitory Effect ◽  
Immunodeficiency Virus ◽  
Orally Bioavailable ◽  
Anti Hiv ◽  
Hiv 1

ABSTRACT The first small-molecule CCR5 antagonist, TAK-779, could not be developed as an anti-human immunodeficiency virus type (anti-HIV-1) agent because of its poor oral bioavailability. TAK-652 is an orally bioavailable TAK-779 derivative with potent anti-HIV-1 activity. TAK-652 inhibited the binding of RANTES (regulated on activation, normal T-cell expressed and secreted), macrophage inflammatory protein 1α (MIP-1α), and MIP-1β to CCR5-expressing cells at nanomolar concentrations. TAK-652 could also suppress the binding of monocyte chemotactic protein 1 (MCP-1) to CCR2b-expressing cells. However, its inhibitory effect on ligand binding to other chemokine receptors was limited. TAK-652 was active against CCR5-using (R5) HIV-1 but totally inactive against CXCR4-using (X4) HIV-1. The compound was active against R5 HIV-1 clinical isolates containing reverse transcriptase and protease inhibitor-resistant mutations, with a mean 50% effective concentration (EC50) and EC90 of 0.061 and 0.25 nM, respectively. In addition, recombinant R5 viruses carrying different subtype (A to G) envelope proteins were equally susceptible to TAK-652. A single oral administration of TAK-652 up to 100 mg was safe and well tolerated in humans. The compound displayed favorable pharmacokinetics, and its plasma concentration was 7.2 ng/ml (9.1 nM) even 24 h after the administration of 25 mg. Thus, TAK-652 is a promising candidate as a novel entry inhibitor of HIV-1.

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