18998634

Source:http://linkedlifedata.com/resource/pubmed/id/18998634

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Predicate	Object
rdf:type	pubmed:Citation
lifeskim:mentions	umls-concept:C0021469, umls-concept:C0027126, umls-concept:C0036576, umls-concept:C0205341, umls-concept:C0303231, umls-concept:C0567416, umls-concept:C0599894, umls-concept:C1414081, umls-concept:C1414085, umls-concept:C1415941, umls-concept:C1533691, umls-concept:C1704675, umls-concept:C1880355, umls-concept:C2931688
pubmed:issue	48
pubmed:dateCreated	2009-2-20
pubmed:abstractText	Myotonic dystrophy type 1 (DM1), the most common form of muscular dystrophy in adults, is an RNA-mediated disease. Dramatically expanded (CUG) repeats accumulate in nuclei and sequester RNA-binding proteins such as the splicing regulator MBNL1. We have employed resin-bound dynamic combinatorial chemistry (RBDCC) to identify the first examples of compounds able to inhibit MBNL1 binding to (CUG) repeat RNA. Screening an RBDCL with a theoretical diversity of 11 325 members yielded several molecules with significant selectivity for binding to (CUG) repeat RNA over other sequences. These compounds were also able to inhibit the interaction of GGG-(CUG)(109)-GGG RNA with MBNL1 in vitro, with K(i) values in the low micromolar range.
pubmed:grant	http://linkedlifedata.com/resource/pubmed/grant/08U54NS048843-05, http://linkedlifedata.com/resource/pubmed/grant/NS58345, http://linkedlifedata.com/resource/pubmed/grant/T32 AR007472-19, http://linkedlifedata.com/resource/pubmed/grant/T32AR007472
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pubmed:language	eng
pubmed:journal	http://linkedlifedata.com/resource/pubmed/journal/7503056
pubmed:citationSubset	IM
pubmed:chemical	http://linkedlifedata.com/resource/pubmed/chemical/Lead, http://linkedlifedata.com/resource/pubmed/chemical/Ligands, http://linkedlifedata.com/resource/pubmed/chemical/RNA, http://linkedlifedata.com/resource/pubmed/chemical/RNA-Binding Proteins
pubmed:status	MEDLINE
pubmed:month	Dec
pubmed:issn	1520-5126
pubmed:author	pubmed-author:GareissPeter CPC, pubmed-author:McNaughtonBrian RBR, pubmed-author:MillerBenjamin LBL, pubmed-author:PaldePrakash BPB, pubmed-author:SobczakKrzysztofK, pubmed-author:ThorntonCharles ACA
pubmed:issnType	Electronic
pubmed:day	3
pubmed:volume	130
pubmed:owner	NLM
pubmed:authorsComplete	Y
pubmed:pagination	16254-61
pubmed:dateRevised	2011-9-26
pubmed:meshHeading	pubmed-meshheading:18998634-Combinatorial Chemistry Techniques, pubmed-meshheading:18998634-Dimerization, pubmed-meshheading:18998634-Lead, pubmed-meshheading:18998634-Ligands, pubmed-meshheading:18998634-Myotonic Dystrophy, pubmed-meshheading:18998634-RNA, pubmed-meshheading:18998634-RNA-Binding Proteins, pubmed-meshheading:18998634-Tandem Repeat Sequences
pubmed:year	2008
pubmed:articleTitle	Dynamic combinatorial selection of molecules capable of inhibiting the (CUG) repeat RNA-MBNL1 interaction in vitro: discovery of lead compounds targeting myotonic dystrophy (DM1).
pubmed:affiliation	Department of Biochemistry and Biophysics, University of Rochester, Rochester, New York 14642, USA.
pubmed:publicationType	Journal Article, Research Support, U.S. Gov't, Non-P.H.S., Research Support, N.I.H., Extramural