Results 201 to 210 of about 82,628 (226)

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, François, Nuninger, Marc, Schaefer, Kayhan G, Akyel, Rainer, Albert, Christian, Beerli, Christian, Bruns, Eric, Francotte, Marcel, Luyten, Duncan, MacKenzie, Lukas, Oberer, Markus B, Streiff, Trixie, Wagner, Hansrudolf, Walter, Gisbert, Weckbecker, Hans-Guenter, Zerwes   +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, S C, Berk, K G, Rosauer, S, Degrado, K T, Chapman, S L, Gould, M S, Springer, L, Malkowitz, W A, Schleif, D, Hazuda, M, Miller, J, Kessler, R, Danzeisen, K, Holmes, J, Lineberger, A, Carella, G, Carver, E A, Emini   +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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CCR5 promoter polymorphisms, CCR5 59029A and CCR5 59353C, are under represented in HIV-1-infected long-term non-progressors

AIDS, 2000
Objective To determine the influence of CCR5 promoter polymorphisms on HIV-1 progression to AIDS and to evaluate the interaction between CCR5 structural polymorphisms and those occurring in the regulatory region of the same gene. Participants Seventy-one HIV-1-infected long-term non-progressors with a CD4+ T cell count of > 500 x 10(6)/I more than 8
Alison O. Clegg, Lesley J. Ashton, Robyn A. Biti, Prerna Badhwar, Peter Williamson, John M. Kaldor, Graeme J. Stewart   +6 more
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Recent advances of CCR5 antagonists

Current Opinion in HIV and AIDS, 2006
The interaction of the beta-chemokine receptor CCR5 with the HIV-1 envelope glycoprotein gp120 is critical for viral entry. Therefore, CCR5 seems to be a promising target for inhibition of HIV-1 replication. A number of attempts have been made to identify small-molecule CCR5 antagonists as novel antiretroviral agents.
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???????????????? ???????????????????? ?? ???????????? ???????????????????????????? ?????????????????? ???? ???????????????? ????????-?????????????????????????? ???????? CCR5 del32

2021
Five Ukrainian populations have been genotyped for a deletion polymorphism del32 in CCR5 gene. It has been shown that frequency of this allele in Ukrainians is similar to that of the other Slavic populations.
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CCR5 inhibitors: emergence, success, and challenges

Expert Opinion on Emerging Drugs, 2012
The discovery of CC-chemokine receptor 5 (CCR5) as a human immunodeficiency virus type 1 (HIV-1) coreceptor opened a new avenue to exploit CCR5 as a potential target for the intervention of HIV-1's cellular entry.Various small-molecule CCR5 inhibitors were identified in the last decade; however, maraviroc (MVC) is the only CCR5 inhibitor currently used
Kenji, Maeda, Debananda, Das, Hirotomo, Nakata, Hiroaki, Mitsuya   +3 more
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Maraviroc: A Ccr5 Antagonist

Future HIV Therapy, 2008
HIV requires binding to both the CD4 molecule and a coreceptor to enable entry into the cell. CCR5 is a chemokine receptor that is utilized as a coreceptor by the majority of virus in early asymptomatic HIV infection. Maraviroc is a novel small molecule CCR5 antagonist which, in Phase IIb/III clinical trials up to 48 weeks, has been shown to be ...
LKK Tan, M Nelson
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