کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2572540 1129305 2015 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Assay strategies for identification of therapeutic leads that target protein trafficking
ترجمه فارسی عنوان
استراتژیهای تشخیصی برای شناسایی منابعی درمانی که قاچاق پروتئین را هدف قرار می دهند
موضوعات مرتبط
علوم زیستی و بیوفناوری علم عصب شناسی علوم اعصاب سلولی و مولکولی
چکیده انگلیسی


• This article describes a novel approach for drug development by targeting the trafficking of receptor and enzyme proteins.
• Strategies are described for the development of high throughput assays for the identification of this class of drugs.

Receptors, enzymes, and ion channels are traditional targets of therapeutic development. A common strategy is to target these proteins with agents that either activate or suppress their activity with ligands or substrates that occupy orthosteric sites or have allosteric interactions. An alternative approach involves regulation of protein trafficking. In principle, this approach enables ‘rescue’ of misfolded and misrouted mutant proteins to restore function, ‘shipwrecking’ of undesirable proteins by targeting them for destruction, and regulation of levels of partially expressed wild type (WT) proteins at their functional sites of action. Here, we present drug discovery strategies that identify ‘pharmacoperones’, which are small molecules that serve as molecular templates and cause otherwise misfolded mutant proteins to fold and route correctly.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: - Volume 36, Issue 8, August 2015, Pages 498–505
نویسندگان
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