MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells. Export

@article{citeulike:965148, abstract = {Organic 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.}, address = {GPC Biotech Incorporated, Waltham, Massachusetts 02451, USA.}, author = {Caligiuri, M. and Molz, L. and Liu, Q. and Kaplan, F. and Xu, J. P. and Majeti, J. Z. and Ramos-Kelsey, R. and Murthi, K. and Lievens, S. and Tavernier, J. and Kley, N.}, citeulike-article-id = {965148}, citeulike-linkout-0 = {http://dx.doi.org/10.1016/j.chembiol.2006.05.008}, citeulike-linkout-1 = {http://view.ncbi.nlm.nih.gov/pubmed/16873019}, citeulike-linkout-2 = {http://www.hubmed.org/display.cgi?uids=16873019}, doi = {10.1016/j.chembiol.2006.05.008}, issn = {1074-5521}, journal = {Chem Biol}, keywords = {interaction, mappit, maspit, molecule, protein, small}, month = {July}, number = {7}, pages = {711--722}, posted-at = {2006-11-28 11:09:30}, priority = {2}, title = {MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.}, url = {http://dx.doi.org/10.1016/j.chembiol.2006.05.008}, volume = {13}, year = {2006} }

TY - JOUR ID - citeulike:965148 L3 - citeulike-article-id:965148 N2 - Organic 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. IS - 7 JF - Chem Biol SN - 1074-5521 AD - GPC Biotech Incorporated, Waltham, Massachusetts 02451, USA. EP - 722 TI - MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells. VL - 13 SP - 711 KW - interaction KW - mappit KW - maspit KW - molecule KW - protein KW - small AU - Caligiuri, M AU - Molz, L AU - Liu, Q AU - Kaplan, F AU - Xu, JP AU - Majeti, JZ AU - Ramos-Kelsey, R AU - Murthi, K AU - Lievens, S AU - Tavernier, J AU - Kley, N PY - 2006/07// UR - http://dx.doi.org/10.1016/j.chembiol.2006.05.008 ER -