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CXCR4-activated astrocyte glutamate release via TNFα: amplification by microglia triggers neurotoxicity
It is demonstrated that altered glial communication has direct neuropathological consequences and that agents interfering with CXCR4-dependent astrocyte–microglia signaling prevent neuronal apoptosis induced by the HIV-1 coat glycoprotein, gp120IIIB.
Inhibition of T-tropic HIV Strains by Selective Antagonization of the Chemokine Receptor CXCR4
- D. Schols, S. Struyf, J. Damme, J. Esté, G. Henson, E. Clercq
- Biology, MedicineThe Journal of experimental medicine
- 20 October 1997
The bicyclams are, to the authors' knowledge, the first low molecular weight anti-HIV agents shown to act as potent and selective CXCR4 antagonists.
Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV.
- E. Clercq
- 1 April 2009
The bicyclam AMD3100 story
- E. Clercq
- BiologyNature Reviews Drug Discovery
- 1 July 2003
The development process ofAMD3100 is described, which began about 15 years ago with the isolation of an impurity, and the basis for the clinical application of AMD3100 and its congeners are described.
Susceptibility of HIV-2, Siv and Shiv to Various Anti-HIV-1 Compounds: Implications for Treatment and Postexposure Prophylaxis
- M. Witvrouw, C. Pannecouque, W. Switzer, T. Folks, E. Clercq, W. Heneine
- Biology, MedicineAntiviral therapy
- 1 January 2004
Findings support the use of NRTIs, tenofovir, but not NN RTIs, for treating HIV-2-infected persons or for prophylaxis against HIV- 2 and SIV, and show co-receptor antagonists such as AMD3100 show promising anti-HIV-2 therapeutic modalities.
Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives
IN the search for compounds active against human immunodeficiency virus (HIV), we have found that members of a novel series of tetrahydro-imidazo[4,5,1-jk][l,4]-benzodiazepin-2(1H)-one and -thione…
Acyclic nucleoside phosphonates: a key class of antiviral drugs
The discovery and development of acyclic nucleoside phosphonates is reviewed, focusing on cidofovir and its potential in the treatment of various herpes-, papilloma-, polyoma-, adeno- and pox-virus infections, and the prevention of HIV infections.
Identification of a Subset of Human Immunodeficiency Virus Type 1 (HIV-1), HIV-2, and Simian Immunodeficiency Virus Strains Able To Exploit an Alternative Coreceptor on Untransformed Human Brain and…
Primary untransformed cell cultures that lack CCR5 and CXCR4 are tested, including astrocytes and brain microvascular endothelial cells (BMVECs), for naturally expressed alternative coreceptors functional for HIV and SIV infection.