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1. 发明申请

US20120004254A1 G PROTEIN-COUPLED RECEPTOR ANTAGONIST AND ITS USE FOR PREVENTING AND TREATING ALZHEIMER'S DISEASE 审中-公开
标题翻译： G蛋白偶联受体拮抗剂及其用于预防和治疗阿尔茨海默病的用途
公开(公告)号：US20120004254A1
公开(公告)日：2012-01-05
申请号：US13214907
申请日：2011-08-22
申请人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
发明人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
IPC分类号： A61K31/485 , A61K31/137 , A61P25/00 , C12Q1/37 , G01N33/566 , A61P25/28 , A61K31/138 , C12Q1/02
CPC分类号： G01N33/5035 , G01N2333/726 , G01N2500/10 , G01N2800/2821
摘要： The invention discloses methods for screening a reagent for treating or preventing Alzheimer's disease or related neurological pathology. A method according to the invention includes the steps of: (a) activating a receptor and determining a first extent of endocytosis of the receptor, wherein the receptor is a G-protein coupled receptor that associates with presenilin-1; (b) activating the receptor under the same conditions as in step (a), in the presence of a candidate reagent, and determining a second extent of endocytosis of the receptor; (c) determining a difference between the first extent of endocytosis and the second extent of endocytosis; and (d) repeating steps (a)-(c), if the difference is less than a threshold. The invention also disclose uses of receptor antagonists for manufacturing medicaments for treating or preventing Alzheimer's disease or related neurological pathology, wherein the receptor antagonists inhibit endocytosis of a G-protein coupled receptor that associates with presenilin-1 during endocytosis.
摘要翻译：本发明公开了用于筛选用于治疗或预防阿尔茨海默病或相关神经病理学的试剂的方法。根据本发明的方法包括以下步骤：（a）激活受体并确定受体的第一内吞程度，其中该受体是与早老素-1相关的G蛋白偶联受体; （b）在与候选试剂的存在下在与步骤（a）相同的条件下活化受体，并确定受体的第二程度的胞吞作用; （c）确定第一内吞程度与第二内吞程度之间的差异; 和（d）如果差值小于阈值，则重复步骤（a） - （c）。本发明还公开了受体拮抗剂用于制备用于治疗或预防阿尔茨海默病或相关神经病理学的药物的用途，其中所述受体拮抗剂抑制内吞作用期间与早老蛋白-1相关的G蛋白偶联受体的内吞作用。

2. 发明授权

US08026073B2 Screening G protein-coupled receptor antagonists for methods of treating Alzheimer's disease 有权
标题翻译：筛选G蛋白偶联受体拮抗剂治疗阿尔茨海默病的方法
公开(公告)号：US08026073B2
公开(公告)日：2011-09-27
申请号：US12159183
申请日：2006-12-26
申请人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
发明人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
IPC分类号： G01N33/53
CPC分类号： G01N33/5035 , G01N2333/726 , G01N2500/10 , G01N2800/2821
摘要： A method for screening a reagent for treating or preventing Alzheimer's disease or related neurological pathology includes the steps of: (a) activating a receptor and determining a first extent of endocytosis of the receptor, wherein the receptor is a G-protein coupled receptor that associates with presenilin-1; (b) activating the receptor under the same conditions as in step (a), in the presence of a candidate reagent, and determining a second extent of endocytosis of the receptor; (c) determining a difference between the first extent of endocytosis and the second extent of endocytosis; and (d) repeating steps (a)-(c), if the difference is less than a threshold. Uses of receptor antagonists for manufacturing medicaments for treating or preventing Alzheimer's disease or related neurological pathology, wherein the receptor antagonists inhibit endocytosis of a G-protein coupled receptor that associates with presenilin-1 during endocytosis.
摘要翻译：用于筛选用于治疗或预防阿尔茨海默病或相关神经病理学的试剂的方法包括以下步骤：（a）激活受体并测定受体的第一内吞程度，其中所述受体是G蛋白偶联受体，与早老素-1; （b）在与候选试剂的存在下在与步骤（a）相同的条件下活化受体，并确定受体的第二程度的胞吞作用; （c）确定第一内吞程度与第二内吞程度之间的差异; 和（d）如果差值小于阈值，则重复步骤（a） - （c）。用于制备用于治疗或预防阿尔茨海默病或相关神经病理学的药物的受体拮抗剂的用途，其中所述受体拮抗剂抑制内吞作用期间与早老蛋白-1相关的G蛋白偶联受体的内吞。

3. 发明申请

US20080312332A1 G Protein-Coupled Receptor Antagonist and Its Use for Preventing and Treating Alzheimer's Disease 有权
标题翻译： G蛋白偶联受体拮抗剂及其用于预防和治疗阿尔茨海默病的用途
公开(公告)号：US20080312332A1
公开(公告)日：2008-12-18
申请号：US12159183
申请日：2006-12-26
申请人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
发明人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
IPC分类号： A61K31/138 , G01N33/566 , A61P25/28
CPC分类号： G01N33/5035 , G01N2333/726 , G01N2500/10 , G01N2800/2821
摘要： A method for screening a reagent for treating or preventing Alzheimer's disease or related neurological pathology includes the steps of: (a) activating a receptor and determining a first extent of endocytosis of the receptor, wherein the receptor is a G-protein coupled receptor that associates with presenilin-1; (b) activating the receptor under the same conditions as in step (a), in the presence of a candidate reagent, and determining a second extent of endocytosis of the receptor; (c) determining a difference between the first extent of endocytosis and the second extent of endocytosis; and (d) repeating steps (a)-(c), if the difference is less than a threshold. Uses of receptor antagonists for manufacturing medicaments for treating or preventing Alzheimer's disease or related neurological pathology, wherein the receptor antagonists inhibit endocytosis of a G-protein coupled receptor that associates with presenilin-1 during endocytosis.
摘要翻译：用于筛选用于治疗或预防阿尔茨海默病或相关神经病理学的试剂的方法包括以下步骤：（a）激活受体并测定受体的第一内吞程度，其中所述受体是G蛋白偶联受体，与早老素-1; （b）在与候选试剂的存在下在与步骤（a）相同的条件下活化受体，并确定受体的第二程度的胞吞作用; （c）确定第一内吞程度与第二内吞程度之间的差异; 和（d）如果差值小于阈值，则重复步骤（a） - （c）。用于制备用于治疗或预防阿尔茨海默病或相关神经病理学的药物的受体拮抗剂的用途，其中所述受体拮抗剂抑制内吞作用期间与早老蛋白-1相关的G蛋白偶联受体的内吞。

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