DAPTA is a potent CCR5 antagonist, an amidated octapeptide corresponding to an HIV envelope glycoprotein gp120 (gp160)-derived sequence (aa 185-192; the SF-2 isolate) that competes against gp120-CD4 complex for interaction with CCR5 (IC50 = 0.42 nM against gp120CM235 binding to CCR5/CD4 cells, IC50 = 1.5/1.8 nM against gp120BaL/sCD4 or gp120CM235/sCD4 binding to CCR5+/CD4- cells). DAPTA blocks CCR5-dependent HIV host cell entry in cultures and in vivo.
Potent CCR5 antagonist that blocks CCR5-dependent HIV host cell entry in cultures and in vivo.
The chemokine receptor CCR5 plays a crucial role in transmission of HIV isolates, which predominate in the early and middle stages of infection, as well as those, which populate the brain and cause neuro-AIDS. CCR5 is therefore an attractive therapeutic
Chronic neuroinflammation plays a prominent role in the progression of Alzheimer's disease. Reactive microglia and astrocytes are observed within the hippocampus during the early stages of the disease. Epidemiological findings suggest that anti-inflammatory therapies may slow the onset of Alzheimer's
Frontiers in pharmacology, 12, 551839-551839 (2021-05-07)
Background: Cigarette smoke exposure (CSE) is a major cause of chronic obstructive pulmonary disease (COPD). The smoke disrupts cell-cell adhesion by inducing epithelial barrier damage to the tight junction (TJ) proteins. Even though the inflammatory mechanism of chemokine (C-C motif)
European journal of pharmacology, 846, 100-108 (2019-01-19)
Autism spectrum disorder (ASD) is a prevalent neurodevelopmental disorder characterized by deficits in social interaction, communication, and repetitive behaviors. BTBR T+ Itpr3tf/J (BTBR) mice, a preclinical autistic model featuring ASD symptoms as defined by social relations, was used in this
The Journal of investigative dermatology, 110(4), 332-337 (1998-04-16)
In addition to acquired immunodeficiency syndrome (AIDS), persons infected with human immunodeficiency virus often develop cutaneous manifestations, including severe psoriasis. In previous studies, we have established that psoriatic fibroblasts and erythrocytes obtained from psoriatic patients exhibit decreased levels of cyclic
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