کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371490 | 981846 | 2012 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Crystal structure of phosphoethanolamine methyltransferase from Plasmodium falciparum in complex with amodiaquine
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Crystal structure of phosphoethanolamine methyltransferase from Plasmodium falciparum in complex with amodiaquine Crystal structure of phosphoethanolamine methyltransferase from Plasmodium falciparum in complex with amodiaquine](/preview/png/1371490.png)
چکیده انگلیسی
Phosphoethanolamine N-methyltransferase (PMT) is essential for phospholipid biogenesis in the malarial parasite Plasmodium falciparum. PfPMT catalyzes the triple methylation of phosphoethanolamine to produce phosphocholine, which is then used for phosphatidylcholine synthesis. Here we describe the 2.0 Å resolution X-ray crystal structure of PfPMT in complex with amodiaquine. To better characterize inhibition of PfPMT by amodiaquine, we determined the IC50 values of a series of aminoquinolines using a direct radiochemical assay. Both structural and functional analyses provide a possible approach for the development of new small molecule inhibitors of PfPMT.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 15, 1 August 2012, Pages 4990–4993
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 15, 1 August 2012, Pages 4990–4993
نویسندگان
Soon Goo Lee, Tara D. Alpert, Joseph M. Jez,