公开(公告)号：US20070010548A1

公开(公告)日：2007-01-11

申请号：US10560591

申请日：2004-06-14

申请人： Beth Drees ,  Leena Chakravarty ,  Glenn Prestwich ,  Gyorgy Dorman ,  Mariann Kavecz ,  Andras Lukacs ,  Laszlo Urge ,  Ferenc Darvas ,  Piotr Rzepecki ,  Colin Ferguson

发明人： Beth Drees ,  Leena Chakravarty ,  Glenn Prestwich ,  Gyorgy Dorman ,  Mariann Kavecz ,  Andras Lukacs ,  Laszlo Urge ,  Ferenc Darvas ,  Piotr Rzepecki ,  Colin Ferguson

IPC分类号： A61K31/4745 ,  C07D471/02 ,  C12Q1/48

CPC分类号： C07D471/04 ,  C12Q1/485 ,  G01N2500/02

摘要： Compounds inhibiting phosphatidylinositol 3-kinase (PI 3-K) activities and methods of preparing and using thereof in treating diseases are disclosed. Compounds inhibiting PI 3-K activity and methods of using PI 3-K inhibitory compounds to inhibit cancer cell grwoth or to treat disorders of immunity and inflammation, in which PI 3-K plays a role in leukocyte function are also provided.

摘要翻译： 公开了抑制磷脂酰肌醇3-激酶（PI 3-K）活性的化合物及其制备及其在治疗疾病中的应用的方法。 还提供了抑制PI3-K活性的化合物和使用PI 3-K抑制化合物抑制癌细胞凋亡或治疗PI3-K在白细胞功能中起作用的免疫和炎症疾病的方法。

公开(公告)号：US20060240497A1

公开(公告)日：2006-10-26

申请号：US11473573

申请日：2006-06-22

申请人： Beth Drees ,  Glenn Prestwich ,  Paul Neilsen ,  Leena Chakravarty ,  Michael Mostert

发明人： Beth Drees ,  Glenn Prestwich ,  Paul Neilsen ,  Leena Chakravarty ,  Michael Mostert

IPC分类号： G01N33/53

CPC分类号： G01N33/574 ,  G01N33/573 ,  G01N33/92

摘要： Lipid assay method, kit, and apparatus involving exposure of a protein, having a lipid recognition motif that interacts with a target lipid and a competing lipid, to a solution containing the competing lipid, and determining whether the target lipid is present in the solution. The target lipid has a stronger affinity to the lipid recognition motif than does the competing lipid. The lipid recognition motif is preferably a pleckstrin homology (PH) domain, with the target lipid being a phosphoinositide. The assay determines activity of a lipid kinase, the target lipid being a phosphorylation product of a reaction between the lipid kinase and a substrate lipid. The assay can be a cancer screening method for detection of cancer cells, where detection of certain levels of a PI(3,4,5)P3 target lipid is an indicator of a cancer cell.

摘要翻译： 脂质测定方法，试剂盒和装置，其涉及具有与靶脂质和竞争性脂质相互作用的脂质识别基序的蛋白质暴露于含有竞争性脂质的溶液中，以及确定溶液中是否存在目标脂质。 目标脂质对脂质识别基序的亲和力高于竞争脂质。 脂质识别基序优选是pleckstrin同源性（PH）结构域，其中目标脂质是磷酸肌醇。 该测定法确定脂质激酶的活性，目标脂质是脂质激酶和底物脂质之间的反应的磷酸化产物。 该测定可以是用于检测癌细胞的癌症筛选方法，其中检测某些水平的PI（3,4,5）P3靶标脂质是癌细胞的指标。

公开(公告)号：US07067269B2

公开(公告)日：2006-06-27

申请号：US09991933

申请日：2001-11-26

申请人： Beth E. Drees ,  Glenn D. Prestwich ,  Paul O. Neilsen ,  Leena Chakravarty ,  Michael J. Mostert

发明人： Beth E. Drees ,  Glenn D. Prestwich ,  Paul O. Neilsen ,  Leena Chakravarty ,  Michael J. Mostert

IPC分类号： G01N33/53

CPC分类号： G01N33/574 ,  G01N33/573 ,  G01N33/92

摘要： A lipid assay method, kit, and apparatus involving exposure of a protein, having a lipid recognition motif that interacts with a target lipid and a competing lipid, to a solution containing the competing lipid, and determining whether the target lipid is present in the solution. The target lipid has a stronger affinity to the lipid recognition motif than does the competing lipid. The lipid recognition motif is preferably a pleckstrin homology (PH) domain, with the target lipid being a phosphoinositide. The assay determines activity of a lipid kinase, the target lipid being a phosphorylation product of a reaction between the lipid kinase and a substrate lipid. The assay can be a cancer screening method for detection of cancer cells, where detection of certain levels of a PI(3,4,5)P3 target lipid is an indicator of a cancer cell.

摘要翻译： 一种脂质测定方法，试剂盒和装置，其涉及将具有与靶脂质和竞争性脂质相互作用的脂质识别基序的蛋白质暴露于含有竞争性脂质的溶液中，以及确定目标脂质是否存在于溶液中 。 目标脂质对脂质识别基序的亲和力高于竞争脂质。 脂质识别基序优选是pleckstrin同源性（PH）结构域，其中目标脂质是磷酸肌醇。 该测定法确定脂质激酶的活性，目标脂质是脂质激酶和底物脂质之间的反应的磷酸化产物。 该测定可以是用于检测癌细胞的癌症筛选方法，其中检测某些水平的PI（3,4,5）P 3/3靶标脂质是癌细胞的指标。