نتایج جستجو برای: peg400
تعداد نتایج: 97 فیلتر نتایج به سال:
We have previously shown that inhibitors of I B kinase (IKK ), including 4(2 -aminoethyl)amino-1,8-dimethylimidazo(1,2a)quinoxaline (BMS-345541), are efficacious against experimental arthritis in rodents. In our efforts to identify an analog as a clinical candidate for the treatment of autoimmune and inflammatory disorders, we have discovered the potent and highly selective IKK inhibitor 2-meth...
The entry of drug payloads into the circulatory system is met by rapid removal by resident macrophages. The almost immediate drop in circulating levels of the therapeutic agent has been identified as a major obstacle for efficient drug delivery. Various physical properties determine the fate of NP-based (NP= nanoparticle) drug-delivery platforms in vivo. Size, surface charge, and surface hydrop...
سیستم های تحویل کلوییدی به طور گسترده در صنایع غذایی و دارویی برای انکپسولاسیون ترکیبات لیپیددوست عملگرا استفاده شده اند (given و همکاران، 2009؛ mcclements و rao، 2011) ترکیبات لیپیددوست انکپسوله شده می توانند شامل انواع گوناگونی از مولکول ها با عملکرد های متفاوت باشند از جمله تری آسیل گلیسرول ها، روغن مرکبات، چربی های ضروری، فیتواسترول ها، کاروتنوئیدها، ویتامین های محلول در چربی و داروهای لیپی...
Endothelial nitric oxide synthase (eNOS), which generates the endogenous vasodilator, nitric oxide (NO), is highly regulated by post-translational modifications and protein interactions. We recently used purified proteins to characterize the mechanisms by which heat shock protein 90 (HSP90) increases eNOS activity at low and high Ca levels (Takahashi, S. and Mendelsohn, M. E., J. Biol. Chem. 27...
The objective of this study was to investigate the transport kinetics of cyclosporin A, a well known substrate for P-glycoprotein (P-gp), across the blood-brain barrier (BBB), and the expression of the transporter in the brain of streptozotocin-induced diabetic rats. The in vivo transport clearance of cyclosporin A was significantly reduced in diabetic rats compared with that in the control. Th...
Previous studies have demonstrated that optimal reversal of 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) resistance requires complete inactivation of the DNA repair protein Omethylguanine DNA methyltransferase (MGMT) for at least 24 h following BCNU administration. In preparation for clinical trials at this institution, this study was undertaken to compare the efficacy of a conventional single-b...
Purpose: The present study was designed to determine biological structure-activity relationships for four newly synthesized analogues of natural compounds (makaluvamines). The compounds, 7-(4-fluorobenzylamino)-1,3,4,8-tetrahydropyrrolo[4,3,2-de] quinolin-8(1H)-one (FBA-TPQ); 7-(phenethylamino)-1,3,4,8-tetrahydropyrrolo[4,3,2-de] quinolin-8(1H)-one (PEA-TPQ); 7-(3,4-methylenedioxyphenethylamino...
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