Tak-779
Title | Journal |
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Chemokine receptor antagonists. | Journal of medicinal chemistry 20121126 |
The blocking of CXCR3 and CCR5 suppresses the infiltration of T lymphocytes in rat renal ischemia reperfusion. | Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association 20121001 |
Structure activity relationship studies of natural product chemokine receptor CCR5 antagonist anibamine toward the development of novel anti prostate cancer agents. | European journal of medicinal chemistry 20120901 |
CCR5 antagonist TD-0680 uses a novel mechanism for enhanced potency against HIV-1 entry, cell-mediated infection, and a resistant variant. | The Journal of biological chemistry 20120511 |
Baseline susceptibility of primary HIV-2 to entry inhibitors. | Antiviral therapy 20120101 |
Allosteric and orthosteric sites in CC chemokine receptor (CCR5), a chimeric receptor approach. | The Journal of biological chemistry 20111028 |
Effects of a calcineurin inhibitor, FK506, and a CCR5/CXCR3 antagonist, TAK-779, in a rat small intestinal transplantation model. | Transplant immunology 20110701 |
Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist. | Bioorganic & medicinal chemistry 20110701 |
CCL5 neutralization restricts cancer growth and potentiates the targeting of PDGFRβ in colorectal carcinoma. | PloS one 20110101 |
C-C chemokine receptor type 5 (CCR5) utilization of transmitted and early founder human immunodeficiency virus type 1 envelopes and sensitivity to small-molecule CCR5 inhibitors. | The Journal of general virology 20101201 |
Evolution of CCR5 antagonist resistance in an HIV-1 subtype C clinical isolate. | Journal of acquired immune deficiency syndromes (1999) 20101201 |
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents. | European journal of medicinal chemistry 20100901 |
Different selection patterns of resistance and cross-resistance to HIV-1 agents targeting CCR5. | The Journal of antimicrobial chemotherapy 20100301 |
Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells. | Antimicrobial agents and chemotherapy 20100201 |
The chemokine receptor antagonist, TAK-779, decreased experimental autoimmune encephalomyelitis by reducing inflammatory cell migration into the central nervous system, without affecting T cell function. | British journal of pharmacology 20091201 |
Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5. | Molecular pharmacology 20090601 |
Design, synthesis, and structure-activity relationship of novel CCR2 antagonists. | Bioorganic & medicinal chemistry letters 20090315 |
[Viral entry as therapeutic target. Current situation of entry inhibitors]. | Enfermedades infecciosas y microbiologia clinica 20081001 |
Inhibition of HIV fusion with multivalent gold nanoparticles. | Journal of the American Chemical Society 20080604 |
Molecular interactions of CCR5 with major classes of small-molecule anti-HIV CCR5 antagonists. | Molecular pharmacology 20080301 |
HIV-1 escape to CCR5 coreceptor antagonism through selection of CXCR4-using variants in vitro. | AIDS (London, England) 20080102 |
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1. | Antimicrobial agents and chemotherapy 20080101 |
Species selectivity of small-molecular antagonists for the CCR5 chemokine receptor. | International immunopharmacology 20071205 |
Synergistic inhibition of HIV-1 infection by combinations of soluble polyanions with other potential microbicides. | Antiviral research 20070901 |
Isolation and characterization of human immunodeficiency virus type 1 resistant to the small-molecule CCR5 antagonist TAK-652. | Antimicrobial agents and chemotherapy 20070201 |
An anti-CCR5 monoclonal antibody and small molecule CCR5 antagonists synergize by inhibiting different stages of human immunodeficiency virus type 1 entry. | Virology 20060901 |
Interaction of small molecule inhibitors of HIV-1 entry with CCR5. | Virology 20060525 |
Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety. | Journal of medicinal chemistry 20060323 |
T-cell line for HIV drug screening using EGFP as a quantitative marker of HIV-1 replication. | BioTechniques 20060101 |
Role of CCR1 and CCR5 in homing and growth of multiple myeloma and in the development of osteolytic lesions: a study in the 5TMM model. | Clinical & experimental metastasis 20060101 |
HIV entry inhibitor TAK-779 attenuates atherogenesis in low-density lipoprotein receptor-deficient mice. | Arteriosclerosis, thrombosis, and vascular biology 20051201 |
Replicative fitness of historical and recent HIV-1 isolates suggests HIV-1 attenuation over time. | AIDS (London, England) 20051014 |
Selection of human immunodeficiency virus type 1 R5 variants with augmented replicative capacity and reduced sensitivity to entry inhibitors during severe immunodeficiency. | The Journal of general virology 20051001 |
The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor. | Molecular pharmacology 20050401 |
Kinetic factors control efficiencies of cell entry, efficacies of entry inhibitors, and mechanisms of adaptation of human immunodeficiency virus. | Journal of virology 20050401 |
Variants of human immunodeficiency virus type 1 that efficiently use CCR5 lacking the tyrosine-sulfated amino terminus have adaptive mutations in gp120, including loss of a functional N-glycan. | Journal of virology 20050401 |
CCR5 antagonists: host-targeted antivirals for the treatment of HIV infection. | Antiviral chemistry & chemotherapy 20050101 |
Impact of mutations in the coreceptor binding site on human immunodeficiency virus type 1 fusion, infection, and entry inhibitor sensitivity. | Journal of virology 20040501 |
Resistance to HIV-1 entry inhibitors. | Current drug targets. Infectious disorders 20031201 |
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. | Journal of medicinal chemistry 20030911 |
Rapamycin causes down-regulation of CCR5 and accumulation of anti-HIV beta-chemokines: an approach to suppress R5 strains of HIV-1. | Proceedings of the National Academy of Sciences of the United States of America 20030902 |
Development of a novel high-throughput surrogate assay to measure HIV envelope/CCR5/CD4-mediated viral/cell fusion using BacMam baculovirus technology. | Journal of biomolecular screening 20030801 |
Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: a molecular modeling-guided mutagenesis study of the binding pocket. | Biochemistry 20030218 |
Sensitivity of HIV-1 to entry inhibitors correlates with envelope/coreceptor affinity, receptor density, and fusion kinetics. | Proceedings of the National Academy of Sciences of the United States of America 20021210 |
Inhibitory effects of small-molecule CCR5 antagonists on human immunodeficiency virus type 1 envelope-mediated membrane fusion and viral replication. | Antimicrobial agents and chemotherapy 20011201 |
Potent, broad-spectrum inhibition of human immunodeficiency virus type 1 by the CCR5 monoclonal antibody PRO 140. | Journal of virology 20010101 |
Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. | Journal of medicinal chemistry 20000518 |
A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5. | Proceedings of the National Academy of Sciences of the United States of America 20000509 |
A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. | Proceedings of the National Academy of Sciences of the United States of America 19990511 |