Constrained NBMPR analogue synthesis, pharmacophore mapping and 3D-QSAR modeling of equilibrative nucleoside transporter 1 (ENT1) inhibitory activity
نویسندگان
چکیده
منابع مشابه
Targeting the equilibrative nucleoside transporter ENT1 in Huntington disease
Huntington disease (HD) is a neurodegenerative disorder phenotypically characterized by progressive chorea, cognitive impairments and emotional disturbances. The crucial pathological hallmark of the disease is the atrophy of the striatum, with a remarkable loss of projecting medium spiny neurons. Among many disturbances in the homeostasis of the striatum reported in HD, it has been suggested th...
متن کاملEquilibrative nucleoside transporter 1 (ENT1) is critical for pollen germination and vegetative growth in Arabidopsis
ENT1 of Arabidopsis thaliana was the first member of the equilibrative nucleoside transporter (ENT) family to be identified in plants and characterized as a cellular, high-affinity nucleoside importer. Evidence is presented here for a tonoplast localization of ENT1 based on proteome data and Western blot analyses. Increased export of adenosine from reconstituted tonoplast preparations from 35S:...
متن کاملN-linked glycosylation of N48 is required for equilibrative nucleoside transporter 1 (ENT1) function
Human equilibrative nucleoside transporter 1 (hENT1) transports nucleosides and nucleoside analogue drugs across cellular membranes and is necessary for the uptake of many anti-cancer, anti-parasitic and anti-viral drugs. Previous work, and in silico prediction, suggest that hENT1 is glycosylated at Asn(48) in the first extracellular loop of the protein and that glycosylation plays a role in co...
متن کاملExpression of concern. Equilibrative nucleoside transporter 1 (ENT1) regulates postischemic blood flow during acute kidney injury in mice.
A complex biologic network regulates kidney perfusion under physiologic conditions. This system is profoundly perturbed following renal ischemia, a leading cause of acute kidney injury (AKI) - a life-threatening condition that frequently complicates the care of hospitalized patients. Therapeutic approaches to prevent and treat AKI are extremely limited. Better understanding of the molecular pat...
متن کامل3D-QSAR Modeling of Anti-oxidant Activity of some Flavonoids
The anti-oxidant activities for a diverse set of flavonoids as TEAC (Trolox equivalent anti-oxidant capacity), assay were subjected to 3D-QSAR (3 dimensional quantitative structural-activity relationship) studies using CoMFA (comparative molecular field analysis) and CoMSIA (comparative molecular similarity indices analysis). The obtained results indicated superiority of CoMSIA model over CoMFA...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2008
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2008.01.044