Vilanterol (GW642444) is a potent, orally active and long-acting β2-AR (β2-adrenergic receptor) agonist with inherent 24-hour activity. The pEC50s for β2-AR, β1-AR and β3-AR are 10.37, 6.98 and 7.36, respectively.…
The orexin receptors (hypocretin receptors) are a family of G protein-coupled receptors and consist of orexin receptor 1 (OX1R) and orexin receptor 2 (OX2R) subtypes. Orexin receptors play important roles…
AAlzheimer's disease (AD) is a neurodegenerative disease, characterized by progressive memory loss. In AD patients' brain, the Aβ-containing plaques and tau-containing neurofibrillary tangles exhibit significant accumulation. Aβ is primarily generated…
The proteasome is part of the main mechanism by which cells regulate specific protein concentration and degrade misfolded proteins. Specifically, ubiquitin is a key molecule known to cooperate with proteasome.…
CYP2C9 is an enzyme protein. The enzyme participates in the metabolism of exogenous substances (including drugs) and endogenous compounds (including fatty acids) through oxidation. Importantly, CYP2C9 is the most abundant…
Methionine aminopeptidase 2 (MetAP2), a member of the dimetallohydrolase family, is a cytosolic metalloenzyme that catalyzes the hydrolytic removal of N-terminal methionine residues from nascent proteins. Importantly, MetAP2 is found…
Purpurogallin is a flavinol obtainable from oak nutgalls. It can inhibit xanthine oxidase, glutathione S-transferase, catechol O-methyltransferase activities, and effectively protects several cell types, also has anti-inflammatory and anti-cancer activities. In…
Voltage-gated calcium channels (VGCC) are a group of voltage-gated ion channels in the membrane of excitable cells. Specifically, they have permeability to calcium ion Ca2+. This channel is a key…
Dipeptidyl Peptidases are widely distributed exopeptidases that possess central role in proteolysis. The dipeptidyl peptidase family, including DPP-4 DPP-7, DPP-8, DPP-9, and fibroblast activation protein. Among them, DPP-4 (CD26) is…
Aplaviroc (AK 602), an SDP derivative, is a potent CCR5 antagonist. Additionally, the IC50s are 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW. In vitro, Aplaviroc exerts potent activity against HIV-1 strains.…