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CCR5 and HIV Infection

Receptors and Channels, 2002
Chemokines and chemokine receptors play a crucial role in the trafficking of leukocyte populations across the body, and are involved in the development of a large variety of human diseases. CCR5 is the main coreceptor used by macrophage (M)-tropic strains of human immunodeficiency virus type 1 (HIV-1) and HIV-2, which are responsible for viral ...
Blanpain, Cédric   +3 more
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The chemokine receptor, CCR5

The International Journal of Biochemistry & Cell Biology, 2004
The chemokine receptor, CCR5, is a G protein coupled receptor responsible for some of the effects of the chemokines CCL3, CCL4 and CCL5. It is also one of the co-receptors for the entry of human immunodeficiency virus-1 (HIV-1) into cells. Regulation of CCR5 number on cells is, therefore, important for determining the infection rate by HIV-1.
Mueller, A., Strange, P. G.
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CCR5-Maraviroc Structure

Science, 2013
The crystal structure of the HIV co-receptor CCR5 bound to the HIV drug maraviroc provides insight into how HIV enters cells.
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CCR5 and inflammatory storm

Ageing Research Reviews
Chemokines and their corresponding receptors play crucial roles in orchestrating inflammatory and immune responses, particularly in the context of pathological conditions disrupting the internal environment. Among these receptors, CCR5 has garnered considerable attention due to its significant involvement in the inflammatory cascade, serving as a ...
Yuting Lin   +19 more
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Lymphocyte adhesion to CCR5 ligands is reduced by anti-CCR5 gene delivery

Journal of the Neurological Sciences, 2011
Immune-mediated damage to the central nervous system (CNS) is an important contributor to many CNS diseases, including epilepsy. Chemokines play a role in leukocyte recruitment to, and migration across, the blood-brain barrier (BBB) during many such processes. We previously investigated the role of the chemokine receptor CCR5 in a rat model of epilepsy
Elena, Marusich   +3 more
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Orally Bioavailable Competitive CCR5 Antagonists

Journal of Medicinal Chemistry, 2004
The chemokine receptor CCR5 plays an important role in inflammatory and autoimmune disorders as well as in transplant rejection by affecting the trafficking of effector T cells and monocytes to diseased tissues. Antagonists of CCR5 are believed to be of potential therapeutic value for the disorders mentioned above and HIV infection.
Gebhard, Thoma   +15 more
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Combinatorial synthesis of CCR5 antagonists

Bioorganic & Medicinal Chemistry Letters, 2001
Herein we report the preparation of a combinatorial library of compounds with potent CCR5 binding affinity. The library design was aided by SAR generated in a traditional medicinal chemistry effort. Compounds with novel combinations of subunits were discovered that have high binding affinity for the CCR5 receptor.
C A, Willoughby   +17 more
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Maraviroc: a new CCR5 antagonist

Expert Review of Anti-infective Therapy, 2009
Maraviroc is a small molecule and a member of a new class of antiretroviral compounds known as CCR5 antagonists, which block R5-tropic HIV entry into CD4 cells. HIV entry into the cell requires binding to a CD4 molecule and, in the majority of cases, to a coreceptor, either chemokine coreceptor 4 (CXCR4) or 5 (CCR5). In August 2007, the US FDA approved
Shilpa, Sayana, Homayoon, Khanlou
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Middle management of CCR5

Nature Reviews Immunology, 2019
Levels of CCR5 expression by CD4+ T cells, which influence the outcome of HIV-1 infection, are modulated by polymorphism of a non-coding RNA that affects mRNA stability.
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Resistance to CCR5 antagonists

Current Opinion in HIV and AIDS, 2007
CCR5 antagonists disrupt crucial interactions between HIV envelope glycoprotein gp120 and CCR5, preventing virus binding and entry. Current antiretroviral agents target viral proteins, whereas CCR5 antagonists bind to the host cell. This novel mechanism of action is posing new challenges to our understanding of drug resistance.Possible mechanisms of ...
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