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Membranes 2015, 5(2), 228-252;

Drug Trafficking into Macrophages via the Endocytotic Receptor CD163

Institute of Molecular Medicine, University of Southern Denmark, J. B. Winsløws Vej 25, 5000-Odense C, Denmark
Department of Clinical Biochemistry and Pharmacology, Odense University Hospital, 5000-Odense C, Denmark
Author to whom correspondence should be addressed.
Academic Editor: Morten S. Nielsen
Received: 4 May 2015 / Accepted: 11 June 2015 / Published: 23 June 2015
(This article belongs to the Special Issue Trafficking of Membrane Receptors 2015)
View Full-Text   |   Download PDF [271 KB, uploaded 23 June 2015]


In inflammatory diseases, macrophages are a main producer of a range of cytokines regulating the inflammatory state. This also includes inflammation induced by tumor growth, which recruits so-called tumor-associated macrophages supporting tumor growth. Macrophages are therefore relevant targets for cytotoxic or phenotype-modulating drugs in the treatment of inflammatory and cancerous diseases. Such targeting of macrophages has been tried using the natural propensity of macrophages to non-specifically phagocytose circulating foreign particulate material. In addition, the specific targeting of macrophage-expressed receptors has been used in order to obtain a selective uptake in macrophages and reduce adverse effects of off-target delivery of drugs. CD163 is a highly expressed macrophage-specific endocytic receptor that has been studied for intracellular delivery of small molecule drugs to macrophages using targeted liposomes or antibody drug conjugates. This review will focus on the biology of CD163 and its potential role as a target for selective macrophage targeting compared with other macrophage targeting approaches. View Full-Text
Keywords: macrophage; CD163; dexamethasone; antibody drug conjugate; targeting; inflammation; internalization macrophage; CD163; dexamethasone; antibody drug conjugate; targeting; inflammation; internalization
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Graversen, J.H.; Moestrup, S.K. Drug Trafficking into Macrophages via the Endocytotic Receptor CD163. Membranes 2015, 5, 228-252.

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