کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587816 | 981440 | 2011 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Chemical modifications of resveratrol for improved protein kinase C alpha activity
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کلمات کلیدی
ERK1PDBtPANrf2HEKAMPKSRC12-O-tetradecanoylphorbol-13-acetatePKCPDSSir2Jnk1PKDIkkBSirtuin-1p56LckES-MSC log PNF-κBMALDI-TOFSirt1STAT3COXnuclear magnetic resonance - رزونانس مغناطیسی هستهای3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide - 3- (4،5-dimethylthiazol-2-yl) -2،5-difenyltetrazolium bromideAMP activated protein kinase - AMP پروتئین کیناز فعال شده استBSA - BSAMTT - MTTbovine serum albumin - آلبومین سرم گاوcyclooxygenase - آنزیم سیکلواکسیژنازElectrospray mass spectrometry - اسپکترومتری جرم الکترو اسپریMembrane translocation - انتقال محفظهLOX - اکسیژن مایعNMR - تشدید مغناطیسی هستهای silent information regulator 2 - تنظیم کننده اطلاعات خاموش 2diacylglycerol - دیسیل گلیسیرینResveratrol - رسوراترولDAG - روزNF-E2 related factor 2 - عامل NF-E2 2nuclear factor κB - فاکتور هسته ای κBPhosphatidylserine - فسفاتیدیلسرینActivation - فعال سازیFluorescence - فلورسنسLipooxygenase - لیپوکسینژازsignal transducer and activators of transcription - مبدل سیگنال و فعال کننده های رونویسیProtein Data Bank - پروتئین بانک اطلاعاتیprotein kinase D - پروتئین کیناز DProtein kinase C - پروتئین کیناز سیMolecular docking - پیوندهای بین مولکولیhuman embryonic kidney - کلیه جنین انسانextracellular signal-regulated kinase - کیناز تنظیم شده سیگنال خارج سلولیEpidermal growth factor receptor - گیرنده فاکتور رشد اپیدرمال
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Resveratrol (1) is a naturally occurring phytoalexin that affects a variety of human disease models, including cardio- and neuroprotection, immune regulation, and cancer chemoprevention. One of the possible mechanisms by which resveratrol affects these disease states is by affecting the cellular signaling network involving protein kinase C alpha (PKCα). PKCα is a member of the family of serine/threonine kinases, whose activity is inhibited by resveratrol. To study the structure-activity relationship, several monoalkoxy, dialkoxy and hydroxy analogs of resveratrol have been synthesized, tested for their cytotoxic effects on HEK293 cells, measured their effects on the membrane translocation properties of PKCα in the presence and absence of the PKC activator TPA, and studied their binding with the activator binding domain of PKCα. The analogs showed less cytotoxic effects on HEK293 cells and caused higher membrane translocation (activation) than that of resveratrol. Among all the analogs, 3, 16 and 25 showed significantly higher activation than resveratrol. Resveratrol analogs, however, inhibited phorbol ester-induced membrane translocation, and the inhibition was less than that of resveratrol. Binding studies using steady state fluorescence spectroscopy indicated that resveratrol and the analogs bind to the second cysteine-rich domain of PKCα. The molecular docking studies indicated that resveratrol and the analogs interact with the protein by forming hydrogen bonds through its hydroxyl groups. These results signify that molecules developed on a resveratrol scaffold can attenuate PKCα activity and this strategy can be used to regulate various disease states involving PKCα.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 18, 15 September 2011, Pages 5321-5333
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 18, 15 September 2011, Pages 5321-5333
نویسندگان
Joydip Das, Satyabrata Pany, Anjoy Majhi,