کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10594111 | 981818 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H4 and the ion channel serotonin 5-HT3A
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H4 and the ion channel serotonin 5-HT3A Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H4 and the ion channel serotonin 5-HT3A](/preview/png/10594111.png)
چکیده انگلیسی
A fragment library was screened against the G protein-coupled histamine H4 receptor (H4R) and the ligand-gated ion channel serotonin 5-HT3A (5-HT3AR). Interestingly, significant overlap was found between H4R and 5-HT3AR hit sets. The data indicates that dual active H4R and 5 HT3AR fragments have a higher complexity than the selective compounds which has important implications for chemical genomics approaches. The results of our fragment-based library screening study illustrate similarities in ligand recognition between H4R and 5-HT3AR and have important consequences for selectivity profiling in ongoing drug discovery efforts on H4R and 5-HT3AR. The affinity profiles of our fragment screening studies furthermore match the chemical properties of the H4R and 5-HT3AR binding sites and can be used to define molecular interaction fingerprints to guide the in silico prediction of protein-ligand interactions and structure.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 18, 15 September 2011, Pages 5460-5464
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 18, 15 September 2011, Pages 5460-5464
نویسندگان
Mark H.P. Verheij, Chris de Graaf, Gerdien E. de Kloe, Saskia Nijmeijer, Henry F. Vischer, Rogier A. Smits, Obbe P. Zuiderveld, Saskia Hulscher, Linda Silvestri, Andrew J. Thompson, Jacqueline E. van Muijlwijk-Koezen, Sarah C.R. Lummis, Rob Leurs,