公开(公告)号：US20060063721A1

公开(公告)日：2006-03-23

申请号：US11228707

申请日：2005-09-16

申请人： Stephen Miller ,  Karina Xavier ,  Michiko Taga ,  Shawn Campagna ,  Martin Semmelhack ,  Bonnie Bassler ,  Frederick Hughson

发明人： Stephen Miller ,  Karina Xavier ,  Michiko Taga ,  Shawn Campagna ,  Martin Semmelhack ,  Bonnie Bassler ,  Frederick Hughson

IPC分类号： A61K31/70 ,  A61K31/4015 ,  A61K31/381 ,  A61K31/12

CPC分类号： C07H7/02 ,  A61K38/00 ,  C07H3/02 ,  C07K14/255 ,  C07K2299/00 ,  Y02A50/47 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/481 ,  Y02A50/483

摘要： This invention relates to crystals comprising apo-LsrB and holo-LsrB. The structure of holo-LsrB identifies a tetrahydroxytetrahydrofuran derived from 4,5-dihydroxy-2,3-pentanedione (DPD) as the active autoinducer-2 (AI-2) molecule in Salmonella typhimurium. The X-ray crystallographic data can be used in a drug discovery method. Additionally the invention provides AI-2 analogs based on this discovery as well as pharmaceutical compositions containing those analogs.

摘要翻译： 本发明涉及包含apo-LsrB和holo-LsrB的晶体。 全LsrB的结构鉴定了来自4,5-二羟基-2,3-戊二酮（DPD）的四羟基四氢呋喃作为鼠伤寒沙门氏菌中的活性自动诱导剂-2（AI-2）分子。 X射线晶体学数据可用于药物发现方法。 另外本发明提供了基于该发现的AI-2类似物以及含有这些类似物的药物组合物。

公开(公告)号：US20060269951A1

公开(公告)日：2006-11-30

申请号：US11439812

申请日：2006-05-24

申请人： Michiko Taga ,  Bonnie Bassler ,  Douglas McKenzie

发明人： Michiko Taga ,  Bonnie Bassler ,  Douglas McKenzie

IPC分类号： C12Q1/68 ,  C12Q1/18 ,  C12N15/74 ,  C12N1/21 ,  C07K14/28 ,  C07K16/12

CPC分类号： C07K14/255 ,  C07K14/28 ,  G01N33/56911 ,  Y02A50/52

摘要： The present invention relates to the discovery of the lsr operon, the genes therein, and the polypeptides encoded by these genes. The present invention also includes strains with altered expression levels of the polypeptides encoded by the genes and the lsr operon relative to wild type cells. In some embodiments, the strains express a transporter that transports an autoinducer into the cell at a level higher than that of wild type cells. The present invention also includes methods for identifying compounds that modulate the transport of the autoinducer into cells.