Activity and structural analysis of GRL-117C: a novel small molecule CCR5 inhibitor active against R5-tropic HIV-1s

CCR5 is a member of the G-protein coupled receptor family that serves as an essential co-receptor for cellular entry of R5-tropic HIV-1, and is a validated target for therapeutics against HIV-1 infections. In the present study, we designed and synthesized a series of novel small CCR5 inhibitors and...

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Veröffentlicht in:	Scientific reports 2019-03, Vol.9 (1), p.4828, Article 4828
Hauptverfasser:	Nakata, Hirotomo, Maeda, Kenji, Das, Debananda, Chang, Simon B., Matsuda, Kouki, Rao, Kalapala Venkateswara, Harada, Shigeyoshi, Yoshimura, Kazuhisa, Ghosh, Arun K., Mitsuya, Hiroaki
Format:	Artikel
Sprache:	eng
Schlagworte:	13 38/22 38/23 42/70 45 631/326/596/1296 631/45/535/1267 64 82 Amino acids Animals Anti-HIV Agents - chemistry Anti-HIV Agents - pharmacology Anti-HIV Agents - therapeutic use Antiretroviral drugs Antiviral activity Binding Sites - drug effects Blood Buffy Coat - cytology CCR5 protein CCR5 Receptor Antagonists - chemistry CCR5 Receptor Antagonists - pharmacology CCR5 Receptor Antagonists - therapeutic use CD4-Positive T-Lymphocytes - metabolism CD4-Positive T-Lymphocytes - virology Cell Line Chemokines CHO Cells Cloning Cricetulus Cross-resistance Drug Resistance, Viral G protein-coupled receptors HeLa Cells HIV HIV Infections - drug therapy HIV Infections - virology HIV-1 - drug effects HIV-1 - physiology Human immunodeficiency virus Humanities and Social Sciences Humans Hydrophobic and Hydrophilic Interactions - drug effects Hydrophobicity Immunology Infectious diseases Inhibitors Inhibitory Concentration 50 Latency Maraviroc - pharmacology Maraviroc - therapeutic use Molecular Docking Simulation multidisciplinary Primary Cell Culture Receptors, CCR5 - metabolism Receptors, CCR5 - ultrastructure Science Science (multidisciplinary) Structural analysis Virus Latency - drug effects Virus Replication - drug effects Viruses
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