Results 1 to 10 of about 6,286 (187)

CCR5 receptor antagonists in preclinical to phase II clinical development for treatment of HIV [PDF]

Expert Opinion on Investigational Drugs, 2016
The chemokine receptor CCR5 has garnered significant attention in recent years as a target to treat HIV infection largely due to the approval and success of the drug Maraviroc. The side effects and inefficiencies with other first generation agents led to failed clinical trials, prompting the development of newer CCR5 antagonists.
Lawrence Wilson, Dennis C Liotta, Michelle B Kim   +2 more
exaly   +5 more sources

The Role of the CCR5 Receptor in Neuropathic Pain Modulation: Current Insights and Therapeutic Implications [PDF]

Biomedicines
Neuropathic pain, a chronic condition arising from injury or dysfunction of the somatosensory nervous system, is characterized by persistent hypersensitivity and spontaneous pain.
Mario García-Domínguez
doaj   +2 more sources

Effect of CCR5 receptor antagonists on endocytosis of the human CCR5 receptor in CHO‐K1 cells [PDF]

British Journal of Pharmacology, 2008
Background and purpose:The CCR5 chemokine receptor is a member of the G protein‐coupled receptor (GPCR) family that is expressed by macrophages, memory T‐lymphocytes and dendritic cells and is activated by chemotactic proteins (e.g. MIP‐1α [CCL3], MIP‐1β [CCL4] and RANTES [CCL5]).
Stephen Hill
exaly   +4 more sources

The Discovery of Tropane-derived CCR5 Receptor Antagonists [PDF]

Chemical Biology and Drug Design, 2006
The development of compound 1, a piperidine‐based CCR5 receptor antagonist with Type I CYP2D6 inhibition, into the tropane‐derived analogue 5, is described. This compound, which is devoid of CYP2D6 liabilities, is a highly potent ligand for the CCR5 receptor and has broad‐spectrum activity against a range of clinically relevant HIV isolates.
David Price, Marcel J De Groot
exaly   +3 more sources

Glycogen synthase kinase-3 activation and dysregulation of amyloid transport receptors expression and shedding in HIV-induced Alzheimer’s disease-like pathology: modulatory effects of CCR5 antagonists [PDF]

Acta Neuropathologica Communications
Neurocognitive impairments occur in about 50% of HIV-infected humans and are associated with Alzheimer’s disease (AD)-like brain pathologies, including increased amyloid-beta1-42(Aβ42) and phospho-Tau.
Biju Bhargavan, Narendran Annadurai, Georgette D. Kanmogne   +2 more
doaj   +2 more sources

Preclinical systematic review of CCR5 antagonists as cerebroprotective and stroke recovery enhancing agents [PDF]

eLife
C-C chemokine receptor type 5 (CCR5) antagonists may improve both acute stroke outcome and long-term recovery. Despite their evaluation in ongoing clinical trials, gaps remain in the evidence supporting their use.
Ayni Sharif, Matthew S Jeffers, Dean A Fergusson, Raj Bapuji, Stuart G Nicholls, John Humphrey, Warren Johnston, Ed Mitchell, Mary-Ann Speirs, Laura Stronghill, Michele Vuckovic, Susan Wulf, Risa Shorr, Dar Dowlatshahi, Dale Corbett, Manoj M Lalu   +15 more
doaj   +2 more sources

CXCR4 mediated recognition of HIV envelope spike and inhibition by CXCL12 [PDF]

Nature Communications
CCR5 and CXCR4 both act as HIV co-receptors, though CXCR4 is less explored. CXCR4 binds the chemokine CXCL12 to regulate cellular processes and mediate HIV entry, a process that CXCL12 inhibits.
Zhiying Zhang, Hongwei Zhang, Lyuqin Zheng, Shihua Chen, Shuo Du, Junyu Xiao, Dinshaw J. Patel   +6 more
doaj   +2 more sources

The GHS-R Blocker D-[Lys3] GHRP-6 Serves as CCR5 Chemokine Receptor Antagonist [PDF]

International Journal of Medical Sciences, 2012
[D-Lys3]-Growth Hormone Releasing Peptide-6 (DLS) is widely utilized in vivo and in vitro as a selective ghrelin receptor (GHS-R) antagonist. This antagonist is one of the most common antagonists utilized in vivo to block GHS-R function and activity ...
Kalpesh Patel, Vishwa Deep Dixit, Jun Ho Lee, Jie Wan Kim, Eric M. Schaffer, Dzung Nguyen, Dennis D. Taub
doaj   +3 more sources

Quantifying the relationship between HIV-1 susceptibility to CCR5 antagonists and virus affinity for antagonist-occupied co-receptor

Virology, 2009
Previous studies have demonstrated that HIV-1 develops resistance to CCR5 antagonists by gaining the ability to use drug-occupied co-receptor. However, the effects of CCR5 antagonists on the affinity of virus-co-receptor interactions have been difficult to quantify.
Robert Ralston, Julie Strizki, John A Howe   +2 more
exaly   +3 more sources

Use of maraviroc, the first CCR5 receptor antagonist, in HIV treatment regimens

Терапевтический архив, 2013
The paper gives the results of international trials of and guidelines for the use of maraviroc, the first CCR5 receptor antagonist, in treatment regimens for HIV-infected patients.
A V Kravchenko
doaj   +2 more sources