Identification of a major co-receptor for primary isolates of HIV-1

Hongkui Deng, Rong Liu, Wilfried Ellmeier, +12

Nature

Primary ImmunodeficiencyHuman RetrovirusImmunologyAntiviral ResponseVirology +4

HIV-1 entry into CD4+ cells is mediated by the chemokine receptor CC-CKR-5

Tatjana Dragic, Virginia Litwin, Graham P. Allaway, +8

Nature

Cd4+ CellsHuman RetrovirusImmunologyAntiviral ResponseImmunologic Mechanism +7

CC CKR5: A RANTES, MIP-1α, MIP-1β Receptor as a Fusion Cofactor for Macrophage-Tropic HIV-1

Ghalib Alkhatib, Christophe Combadière, Christopher C. Broder, +4

Science

Spirodiketopiperazine-Based CCR5 Inhibitor Which Preserves CC-Chemokine/CCR5 Interactions and Exerts Potent Activity against R5 Human Immunodeficiency Virus Type 1 In Vitro

Kenji Maeda, Hirotomo Nakata, Yasuhiro Koh, +9

Journal of Virology

MedicineHuman RetrovirusImmunologyAntiviral ResponseAntiviral Drug Development +11

Novel Low Molecular Weight Spirodiketopiperazine Derivatives Potently Inhibit R5 HIV-1 Infection through Their Antagonistic Effects on CCR5

Kenji Maeda, Kazuhisa Yoshimura, Shiro Shibayama, +7

Journal of Biological Chemistry

Design, Synthesis, and Biological Evaluation of the Combinatorial Library with a New Spirodiketopiperazine Scaffold. Discovery of Novel Potent and Selective Low-Molecular-Weight CCR5 Antagonists

Hiromu Habashita, Masaya Kokubo, Shin-ichi Hamano, +8

Journal of Medicinal Chemistry

Combinatorial ChemistryDrug TargetPharmacotherapyChemical BiologyPharmaceutical Chemistry +16

Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc

David A. Price, Duncan Armour, Marcel de Groot, +5

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyCcr5 Antagonist MaravirocMedicineHerg AffinityImmunology +3

Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite

Rena Nishizawa, Toshihiko Nishiyama, Katsuya Hisaichi, +11

Bioorganic & Medicinal Chemistry Letters

BiochemistryMedicineNatural SciencesRational Drug DesignLead Identification +5

Chloro-Substituted 3-Alkylamino-4<i>H</i>-1,2,4-benzothiadiazine 1,1-Dioxides as ATP-Sensitive Potassium Channel Activators: Impact of the Position of the Chlorine Atom on the Aromatic Ring on Activity and Tissue Selectivity

Bernard Pirotte, Pascal De Tullio, Quynh-Anh Nguyen, +6

Journal of Medicinal Chemistry

Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles

Rena Nishizawa, Toshihiko Nishiyama, Katsuya Hisaichi, +11

Bioorganic & Medicinal Chemistry Letters

MedicineSpirodiketopiperazine-based Ccr5 AntagonistsClinical PharmacologyPharmacotherapyPharmacology +1