کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1391513 | 983301 | 2006 | 12 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: MASPIT: Three-Hybrid Trap for Quantitative Proteome Fingerprinting of Small Molecule-Protein Interactions in Mammalian Cells MASPIT: Three-Hybrid Trap for Quantitative Proteome Fingerprinting of Small Molecule-Protein Interactions in Mammalian Cells](/preview/png/1391513.png)
SummaryOrganic small molecules generally act by perturbing the function of one or more cellular target proteins, the identification of which is essential to an understanding of the molecular basis of drug action. Here we describe the application of methotrexate-linked small molecule ligands to a mammalian three-hybrid interaction trap for proteome-wide identification of small molecule targets, quantification of the targeting potency of unmodified small molecules for such targets in intact cells, and screening for inhibitors of small molecule-protein interactions. During the course of this study we also identified the pyrido[2,3-d]pyrimidine PD173955, a known SRC kinase inhibitor, as a potent inhibitor of several ephrin receptor tyrosine kinases. This finding could perhaps be exploited in the design of inhibitors for this kinase subfamily, members of which have been implicated in the pathogenesis of various diseases, including cancer.
Journal: - Volume 13, Issue 7, July 2006, Pages 711–722