کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2131807 | 1086660 | 2009 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The ErbB kinase domain: Structural perspectives into kinase activation and inhibition
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کلمات کلیدی
MIG6Receptor dimerization - dimerization گیرندهRTK, Receptor tyrosine kinase - تیروزین کینازهای گیرنده ایActivation loop - حلقه فعالstructural biology - زیست شناسی ساختاریLung cancer - سرطان ریهTyrosine kinase inhibitor - مهار کننده تیروزین کینازSignal transduction - هدایت سیگنالGrowth factor receptor - گیرنده عامل رشدEpidermal growth factor receptor - گیرنده فاکتور رشد اپیدرمال
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
تحقیقات سرطان
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چکیده انگلیسی
Epidermal growth factor receptor (EGFR) and its family members, ErbB2, ErbB3 and ErbB4, are receptor tyrosine kinases which send signals into the cell to regulate many critical processes including development, tissue homeostasis, and tumorigenesis. Central to the signaling of these receptors is their intracellular kinase domain, which is activated by ligand-induced dimerization of the receptor and phosphorylates several tyrosine residues in the C-terminal tail. The phosphorylated tail then recruits other signaling molecules and relays the signal to downstream pathways. A model of the autoinhibition, activation and feedback inhibition mechanisms for the ErbB kinase domain has emerged from a number of recent structural studies. Meanwhile, recent clinical studies have revealed the relationship between specific ErbB kinase mutations and the responsiveness to kinase inhibitor drugs. We will review these regulation mechanisms of the ErbB kinase domain, and discuss the binding specificity of kinase inhibitors and the effects of kinase domain mutations found in cancer patients from a structural perspective.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Experimental Cell Research - Volume 315, Issue 4, 15 February 2009, Pages 649-658
Journal: Experimental Cell Research - Volume 315, Issue 4, 15 February 2009, Pages 649-658
نویسندگان
Ron Bose, Xuewu Zhang,