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Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo.

Thoma, Gebhard and Streiff, Markus and Kovarik, Jiri and Glickman, Fraser and Wagner, Beatrix and Beerli, Christian and Zerwes, Hans-Guenter (2008) Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo. Journal of Medicinal Chemistry, 51 (24). pp. 7915-7920. ISSN 1520-4804

Abstract

The interaction of the chemokine receptor CXCR4 with its ligand CXCL12 is involved in many biological processes such as hematopoesis, migration of immune cells, as well as in cancer metastasis. CXCR4 also mediates the infection of T-cells with X4-tropic HIV functioning as a coreceptor for the viral envelope protein gp120. Here, we describe highly potent, selective CXCR4 inhibitors that block CXCR4/CXCL12 interactions in vitro and in vivo as well as the infection of target cells by X4-tropic HIV.

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Date Deposited: 14 Dec 2009 13:48
Last Modified: 31 Jan 2013 00:53
URI: https://oak.novartis.com/id/eprint/1509

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