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1. 发明申请

WO0110386A3 ANTI-BACTERIAL COMPOUNDS DIRECTED AGAINST PILUS BIOGENESIS, ADHESION AND ACTIVITY; CO-CRYSTALS OF PILUS SUBUNITS AND METHODS OF USE THEREOF 审中-公开
标题翻译：抗细菌化合物指导PILUS生物发生，粘附和活性; PILUS亚基的共晶体及其使用方法
公开(公告)号：WO0110386A3
公开(公告)日：2001-08-02
申请号：PCT/US0022087
申请日：2000-08-11
申请人： UNIV WASHINGTON , HULTGREN SCOTT J , SAUER FREDERIC G , WAKSMAN GABRIEL , FUETTERER KLAUS , CHOUDHURY DEVAPRIY , KNIGHT STEFAN D , BARNHARDT MICHELLE
发明人： HULTGREN SCOTT J , SAUER FREDERIC G , WAKSMAN GABRIEL , FUETTERER KLAUS , CHOUDHURY DEVAPRIY , KNIGHT STEFAN D , BARNHARDT MICHELLE
IPC分类号： A61K38/00 , C07K14/245 , G01N33/569 , G01N33/68 , C07K14/195 , A61P31/04 , C07H3/02 , G06F17/50
CPC分类号： C07K14/245 , A61K38/00 , C07K2299/00 , G01N33/56911 , G01N33/6803 , G01N2500/00
摘要： Many Gram-negative pathogens assemble adhesive structures on their surfaces that allow them to colonize host tissues and cause disease. Novel compositions for the prevention or inhibition of pilus assembly in Gram-negative pathogens are disclosed. Interacting with the binding site of pili subunits will negatively affect the chaperone/usher pathway which is one molecular mechanism by which Gram-negative bacteria assemble adhesive pili structures and thus prevent or inhibit pilus assembly. Additionally, novel compounds and compositions for interfering or preventing adhesion of piliated bacteria to host tissues are provided. Such compounds and compositions prevent or inhibit pili adhesion to host tissues by interacting with the mannose-binding domains on pilus adhesin subunits. Also provided are methods for the treatment or prevention of diseases caused by tissue-adhering pilus-forming bacteria by interaction with the binding between pilus subunits; the binding between pilus subunits and periplasmic chaperones; and the binding of a pilus adhesin to the host epithelial tissue. Also provided are pharmaceutical preparations capable of interacting with the binding between pilus subunits, between pilus subunits and periplasmic chaperones and between the pilus adhesin. The present invention further relates to co-crystals of pilus chaperone-subunit co-ccomplexes, detailed three dimensional structural information illustrating the interaction between pilus subunits and/or between a pilus subunit and a chaperone for a pilus chaperone-subunit co-complex and methods of utilizing the X-ray crystallographic data from such co-crystals to design, identify and screen for compounds that exhibit antibacterial activity. The present invention also relates to machine readable media embedded with the three-dimensional atomic structure coordinates of pilus chaperone-subunit co-complex and subsets thereof.
摘要翻译：许多革兰氏阴性病原体在其表面上装配粘合剂结构，使它们能够在宿主组织中定殖并引起疾病。公开了用于预防或抑制革兰氏阴性病原体中菌毛组装的新型组合物。与菌毛亚基的结合位点相互作用会对伴侣/引导通路产生不利影响，这是革兰氏阴性菌组装粘性菌毛结构从而阻止或抑制菌毛组装的分子机制之一。另外，提供了用于干扰或防止纤毛细菌粘附到宿主组织的新型化合物和组合物。此类化合物和组合物通过与菌毛粘附素亚基上的甘露糖结合结构域相互作用来阻止或抑制菌毛粘附到宿主组织。还提供了通过与菌毛亚基之间的结合相互作用来治疗或预防由组织粘附的菌毛形成细菌引起的疾病的方法; 菌毛亚基和周质伴侣之间的结合; 和菌毛粘附素与宿主上皮组织的结合。还提供了能够与菌毛亚单位之间，菌毛亚单位和周质伴侣之间以及菌毛粘附素之间的结合相互作用的药物制剂。本发明进一步涉及菌毛伴侣 - 亚基共同复合物的共晶体，详细的三维结构信息，说明菌毛伴侣 - 亚基共复合体中菌毛亚基之间和/或菌毛亚基与伴侣蛋白之间的相互作用和方法利用来自这种共晶体的X射线晶体学数据来设计，鉴定和筛选具有抗菌活性的化合物。本发明还涉及嵌入有菌毛伴侣 - 亚基共同复合物及其子集的三维原子结构坐标的机器可读介质。

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