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1. 发明申请

US20070238197A9 Fluorescent ligands for GPCR arrays 审中-公开
标题翻译： GPCR阵列的荧光配体
公开(公告)号：US20070238197A9
公开(公告)日：2007-10-11
申请号：US11363400
申请日：2006-02-27
申请人： Ye Fang , Yulong Hong , Jinlin Peng
发明人： Ye Fang , Yulong Hong , Jinlin Peng
IPC分类号： G01N33/543
CPC分类号： G01N33/582 , C07K7/083 , C07K14/63 , G01N33/6845 , G01N33/74 , G01N2333/63 , G01N2333/726
摘要： Microarrays employing a fluorescent ligand including a material having a binding affinity in the range of about 0.01 to about 25 nM, or about 0.1 to about 10 nM; a specificity to its cognate receptor in the range of about 50 to about 99%, or about 65 to about 99%; a cross-activity to other receptors of 0 to about 20%, or 0 to about 10%; a net charge per ligand of about −3 to about +5, or more preferably, about −2 to about +2 or most preferably for small compound ligands about −1 to about +2. The ligand may also have a hydrophobicity in the range of about 3 to about 55 minutes eluting time (as measured under specified eluting conditions). In some embodiments, the ligand includes fluorescently labeled motilin 1-16 labeled with Bodipy-TMR, rhodamine or Cy5-. Other embodiments include fluorescently labeled Cy5-naltrexone, Cy5-neurotensin 2-13, N-terminal labeled neurotensin 2-13 or lys-labeled labeled neurotensin 2-13.
摘要翻译：使用荧光配体的微阵列，其包括具有约0.01至约25nM或约0.1至约10nM范围内的结合亲和力的材料; 在约50至约99％，或约65至约99％的范围内对其同源受体的特异性; 与其他受体的交叉活性为0至约20％，或0至约10％; 每个配体的净电荷为约-3至约+5，或更优选约-2至约+2，或最优选约为-1至约+2的小化合物配体。配体还可以具有约3至约55分钟洗脱时间（在规定的洗脱条件下测量）的疏水性。在一些实施方案中，配体包括用Bodipy-TMR，罗丹明或Cy5-标记的荧光标记的胃动素1-16。其他实施方案包括荧光标记的Cy5-纳曲酮，Cy5-神经丝氨酸2-13，N-末端标记的神经丝氨酸蛋白酶2-13或lys-标记的标记的神经丝氨酸素2-13。

2. 发明申请

US20060148101A1 Fluorescent ligands for GPCR arrays 审中-公开
标题翻译： GPCR阵列的荧光配体
公开(公告)号：US20060148101A1
公开(公告)日：2006-07-06
申请号：US11363400
申请日：2006-02-27
申请人： Ye Fang , Yulong Hong , Jinlin Peng
发明人： Ye Fang , Yulong Hong , Jinlin Peng
IPC分类号： G01N33/543
CPC分类号： G01N33/582 , C07K7/083 , C07K14/63 , G01N33/6845 , G01N33/74 , G01N2333/63 , G01N2333/726
摘要： Microarrays employing a fluorescent ligand including a material having a binding affinity in the range of about 0.01 to about 25 nM, or about 0.1 to about 10 nM; a specificity to its cognate receptor in the range of about 50 to about 99%, or about 65 to about 99%; a cross-activity to other receptors of 0 to about 20%, or 0 to about 10%; a net charge per ligand of about −3 to about +5, or more preferably, about −2 to about +2 or most preferably for small compound ligands about −1 to about +2. The ligand may also have a hydrophobicity in the range of about 3 to about 55 minutes eluting time (as measured under specified eluting conditions). In some embodiments, the ligand includes fluorescently labeled motilin 1-16 labeled with Bodipy-TMR, rhodamine or Cy5-. Other embodiments include fluorescently labeled Cy5-naltrexone, Cy5-neurotensin 2-13, N-terminal labeled neurotensin 2-13 or lys-labeled labeled neurotensin 2-13.
摘要翻译：使用荧光配体的微阵列，其包括具有约0.01至约25nM或约0.1至约10nM范围内的结合亲和力的材料; 在约50至约99％，或约65至约99％的范围内对其同源受体的特异性; 与其他受体的交叉活性为0至约20％，或0至约10％; 每个配体的净电荷为约-3至约+5，或更优选约-2至约+2，或最优选约为-1至约+2的小化合物配体。配体还可以具有约3至约55分钟洗脱时间（在规定的洗脱条件下测量）的疏水性。在一些实施方案中，配体包括用Bodipy-TMR，罗丹明或Cy5-标记的荧光标记的胃动素1-16。其他实施方案包括荧光标记的Cy5-纳曲酮，Cy5-神经丝氨酸2-13，N-末端标记的神经丝氨酸蛋白酶2-13或lys-标记的标记的神经丝氨酸素2-13。

3. 发明申请

US20050009205A1 Fluorescent ligands for GPCR arrays 审中-公开
标题翻译： GPCR阵列的荧光配体
公开(公告)号：US20050009205A1
公开(公告)日：2005-01-13
申请号：US10741213
申请日：2003-12-19
申请人： Ye Fang , Yulong Hong , Jinlin Peng
发明人： Ye Fang , Yulong Hong , Jinlin Peng
IPC分类号： C07K7/08 , C07K14/63 , G01N33/543
CPC分类号： G01N33/582 , C07K7/083 , C07K14/63 , G01N33/6845 , G01N33/74 , G01N2333/63 , G01N2333/726
摘要： A fluorescent ligand includes a material having a binding affinity in the range of about 0.01 to about 25 nM, or about 0.1 to about 10 nM; a specificity to its cognate receptor in the range of about 50 to about 99%, or about 65 to about 99%; a cross-activity to other receptors of 0 to about 20%, or 0 to about 10%; a net charge per ligand of about −3 to about +5, or more preferably, about −2 to about +2 or most preferably for small compound ligands about −1 to about +2. The ligand may also have a hydrophobicity in the range of about 3 to about 55 minutes eluting time (as measured under specified eluting conditions). In some embodiments, the ligand including fluorescently labeled motilin 1-16 labeled with Bodipy-TMR, rhodamine or Cy5-. Other embodiments include fluorescently labeled Cy5-naltrexone, Cy5-neurotensin 2-13, N-terminal labeled neurotensin 2-13 or lys-labeled labeled neurotensin 2-13.
摘要翻译：荧光配体包括具有约0.01至约25nM，或约0.1至约10nM范围内的结合亲和力的材料; 在约50至约99％，或约65至约99％的范围内对其同源受体的特异性; 与其他受体的交叉活性为0至约20％，或0至约10％; 每个配体的净电荷为约-3至约+5，或更优选约-2至约+2，或最优选约为-1至约+2的小化合物配体。配体还可以具有约3至约55分钟洗脱时间（在规定的洗脱条件下测量）的疏水性。在一些实施方案中，配体包括用Bodipy-TMR，罗丹明或Cy5-标记的荧光标记的胃动素1-16。其他实施方案包括荧光标记的Cy5-纳曲酮，Cy5-神经丝氨酸2-13，N-末端标记的神经丝氨酸蛋白酶2-13或lys-标记的标记的神经丝氨酸素2-13。

4. 发明申请

US20030118586A1 G protein coupled receptor protein, production and use thereof 审中-公开
标题翻译： G蛋白偶联受体蛋白，其生产和使用
公开(公告)号：US20030118586A1
公开(公告)日：2003-06-26
申请号：US10184426
申请日：2002-06-28
发明人： Shuji Hinuma , Ryo Fujii , Yuji Kawamata
IPC分类号： A61K039/395 , G01N033/53 , C07H021/04 , C12P021/02 , C12N005/06
CPC分类号： C07K14/705 , A01K2217/05 , A01K2217/075 , G01N2333/5757 , G01N2333/595 , G01N2333/63 , G01N2333/645 , G01N2333/655 , G01N2333/726 , G01N2500/02 , G01N2500/04
摘要： Rabbit gastropyrolic part smooth muscle-derived G protein coupled receptor proteins, partial peptides thereof; and DNAs containing said protein or partial peptide-encoding DNA are provided. The receptor protein and the DNA coding for said protein can be used for {circle over (1)} determination of ligands; {circle over (2)} acquisition of antibody and antiserum; {circle over (3)} construction of expression system for of a recombinant type receptor protein; {circle over (4)} development of the receptor binding assay system using said expression system and screening of the candidate compounds for pharmaceuticals; {circle over (5)} conducting a drug design based upon a comparison with structurally analogous ligands and receptors; {circle over (6)} preparation of probes and PCR primers for a gene diagnosis; {circle over (7)} preparation of transgenic animals; and {circle over (8)} preparation of model patient animals deficient in the receptor protein DNA. Elucidation of the structure and property of the G protein coupled receptor is particularly related to the development of unique pharmaceuticals which act on such a system.
摘要翻译：兔子胃部分平滑肌衍生的G蛋白偶联受体蛋白，其部分肽; 并提供含有所述蛋白质或部分肽编码DNA的DNA。受体蛋白和编码所述蛋白质的DNA可以用于（循环（1个配体的测定; {循环（2次获得抗体和抗血清; {circle over（3构建重组型受体蛋白质的表达系统 ;（循环（使用所述表达系统的受体结合测定系统的4个开发和用于药物的候选化合物的筛选）;循环（5个基于与结构上类似的配体和受体的比较进行药物设计; 6制备用于基因诊断的探针和PCR引物;（循环（7个转基因动物的制备）和{循环（8个缺陷受体蛋白DNA的模型患者动物的制备），阐明G蛋白的结构和性质偶联受体与作用于这种系统的独特药物的开发特别相关。

5. 发明申请

WO2005066633A2 FLUORESCENT LIGANDS FOR GPCR ARRAYS 审中-公开
标题翻译：用于GPCR阵列的荧光配体
公开(公告)号：WO2005066633A2
公开(公告)日：2005-07-21
申请号：PCT/US2004/041935
申请日：2004-12-13
申请人： CORNING INCORPORATED , FANG, Ye , HONG, Yulong , PENG, Jinlin
发明人： FANG, Ye , HONG, Yulong , PENG, Jinlin
IPC分类号： G01N33/543
CPC分类号： G01N33/582 , C07K7/083 , C07K14/63 , G01N33/6845 , G01N33/74 , G01N2333/63 , G01N2333/726
摘要： A fluorescent ligand includes a material having a binding affinity in the range of about 0.01 to about 25 nM, or about 0.1 to about 10 nM; a specificity to its cognate receptor in the range of about 50 to about 99%, or about 65 to about 99%; a cross-activity to other receptors of 0 to about 20%, or 0 to about 10%; a net charge per ligand of about -3 to about +5, or more preferably, about -2 to about +2 or most preferably for small compound ligands about -1 to about +2. The ligand may also have a hydrophobicity in the range of about 3 to about 55 minutes eluting time (as measured under specified eluting conditions) . In some embodiments, the ligand including fluorescently labeled motilin 1-16 labeled with Bodipy-TMR, rhodamine or Cy5-. Other embodiments include fluorescently labeled Cy5-naltrexone, Cy5-neurotensin 2-13, N-terminal labeled neurotensin 2-13 or lys-labeled labeled neurotensin 2-13.
摘要翻译：荧光配体包括具有约0.01至约25nM，或约0.1至约10nM范围内的结合亲和力的材料; 在约50至约99％，或约65至约99％的范围内对其同源受体的特异性; 与其他受体的交叉活性为0至约20％，或0至约10％; 每个配体的净电荷为约-3至约+5，或更优选约-2至约+2，或最优选约为-1至约+2的小化合物配体。配体还可以具有约3至约55分钟洗脱时间（在规定的洗脱条件下测量）的疏水性。在一些实施方案中，配体包括用Bodipy-TMR，罗丹明或Cy5-标记的荧光标记的胃动素1-16。其他实施方案包括荧光标记的Cy5-纳曲酮，Cy5-神经丝氨酸2-13，N-末端标记的神经丝氨酸蛋白酶2-13或lys-标记的标记的神经丝氨酸素2-13。

6. 发明申请

WO2004057328A3 DIAGNOSTICS AND THERAPEUTICS FOR DISEASES ASSOCIATED WITH G-PROTEIN-COUPLED RECEPTOR 38 (GPR38) 审中-公开
标题翻译：与G蛋白偶联受体38相关的疾病的诊断和治疗（GPR38）
公开(公告)号：WO2004057328A3
公开(公告)日：2004-10-07
申请号：PCT/EP0314052
申请日：2003-12-11
申请人： BAYER HEALTHCARE AG , GOLZ STEFAN , BRUEGGEMEIER ULF , SUMMER HOLGER
发明人： GOLZ STEFAN , BRUEGGEMEIER ULF , SUMMER HOLGER
IPC分类号： G01N33/74 , A61K38/00 , C07K16/00 , C12N15/11
CPC分类号： G01N33/74 , G01N2333/63 , G01N2500/10 , G01N2500/20
摘要： The invention provides a human GPR38 which is associated with the disorders of the peripheral and central nervous system, urology diseases and cardiovascular diseases. The invention also provides assays for the identification of compounds useful in the treatment or prevention of disorders of the peripheral and central nervous system, urology diseases and cardiovascular diseases. The invention also features compounds which bind to and/or activate or inhibit the activity of GPR38 as well as pharmaceutical compositions comprising such compounds.
摘要翻译：本发明提供了与外周和中枢神经系统疾病，泌尿科疾病和心血管疾病相关的人类GPR38。本发明还提供了用于鉴定可用于治疗或预防外周和中枢神经系统疾病，泌尿科疾病和心血管疾病的化合物的测定。本发明还涉及结合和/或活化或抑制GPR38的活性的化合物以及包含这些化合物的药物组合物。

7. 发明申请

WO2005066633A3 FLUORESCENT LIGANDS FOR GPCR ARRAYS 审中-公开
标题翻译：用于GPCR阵列的荧光配体
公开(公告)号：WO2005066633A3
公开(公告)日：2006-02-16
申请号：PCT/US2004041935
申请日：2004-12-13
申请人： CORNING INC , FANG YE , HONG YULONG , PENG JINLIN
发明人： FANG YE , HONG YULONG , PENG JINLIN
IPC分类号： C07K7/08 , C07K14/63 , G01N33/543 , G01N33/68 , C07K7/00 , G01N33/50
CPC分类号： G01N33/582 , C07K7/083 , C07K14/63 , G01N33/6845 , G01N33/74 , G01N2333/63 , G01N2333/726
摘要： A fluorescent ligand includes a material having a binding affinity in the range of about 0.01 to about 25 nM, or about 0.1 to about 10 nM; a specificity to its cognate receptor in the range of about 50 to about 99%, or about 65 to about 99%; a cross-activity to other receptors of 0 to about 20%, or 0 to about 10%; a net charge per ligand of about -3 to about +5, or more preferably, about -2 to about +2 or most preferably for small compound ligands about -1 to about +2. The ligand may also have a hydrophobicity in the range of about 3 to about 55 minutes eluting time (as measured under specified eluting conditions) . In some embodiments, the ligand including fluorescently labeled motilin 1-16 labeled with Bodipy-TMR, rhodamine or Cy5-. Other embodiments include fluorescently labeled Cy5-naltrexone, Cy5-neurotensin 2-13, N-terminal labeled neurotensin 2-13 or lys-labeled labeled neurotensin 2-13.
摘要翻译：荧光配体包括具有约0.01至约25nM，或约0.1至约10nM范围内的结合亲和力的材料; 在约50至约99％，或约65至约99％的范围内对其同源受体的特异性; 与其他受体的交叉活性为0至约20％，或0至约10％; 每个配体的净电荷为约-3至约+5，或更优选约-2至约+2，或最优选约为-1至约+2的小化合物配体。配体还可以具有约3至约55分钟洗脱时间（在规定的洗脱条件下测量）的疏水性。在一些实施方案中，配体包括用Bodipy-TMR，罗丹明或Cy5-标记的荧光标记的胃动素1-16。其他实施方案包括荧光标记的Cy5-纳曲酮，Cy5-神经丝氨酸2-13，N-末端标记的神经丝氨酸蛋白酶2-13或lys-标记的标记的神经丝氨酸素2-13。

8. 发明申请

WO2004057328A2 DIAGNOSTICS AND THERAPEUTICS FOR DISEASES ASSOCIATED WITH G-PROTEIN-COUPLED RECEPTOR 38 (GPR38) 审中-公开
标题翻译： G蛋白偶联受体38（GPR38）相关疾病的诊断和治疗
公开(公告)号：WO2004057328A2
公开(公告)日：2004-07-08
申请号：PCT/EP2003/014052
申请日：2003-12-11
申请人： BAYER HEALTHCARE AG , GOLZ, Stefan , BRÜGGEMEIER, Ulf , SUMMER, Holger
发明人： GOLZ, Stefan , BRÜGGEMEIER, Ulf , SUMMER, Holger
IPC分类号： G01N33/48
CPC分类号： G01N33/74 , G01N2333/63 , G01N2500/10 , G01N2500/20
摘要： The invention provides a human GPR38 which is associated with the disorders of the peripheral and central nervous system, urology diseases and cardiovascular diseases. The invention also provides assays for the identification of compounds useful in the treatment or prevention of disorders of the peripheral and central nervous system, urology diseases and cardiovascular diseases. The invention also features compounds which bind to and/or activate or inhibit the activity of GPR38 as well as pharmaceutical compositions comprising such compounds.
摘要翻译：本发明提供了与外周和中枢神经系统疾病，泌尿科疾病和心血管疾病相关的人GPR38。本发明还提供用于鉴定可用于治疗或预防外周和中枢神经系统疾病，泌尿科疾病和心血管疾病的化合物的测定法。本发明还涉及结合和/或激活或抑制GPR38活性的化合物以及包含此类化合物的药物组合物。

9. 发明专利

TW200533917A G-蛋白連結受納體陣列之螢光配位體 FLUORESCENT LIGANDS FOR GPCR ARRAYS 审中-公开
简体标题： G-蛋白链接受纳体数组之萤光配位体 FLUORESCENT LIGANDS FOR GPCR ARRAYS
公开(公告)号：TW200533917A
公开(公告)日：2005-10-16
申请号：TW093139104
申请日：2004-12-15
申请人：康寧公司 CORNING INCORPORATED
发明人：范業 YE FANG , 洪裕隆 YULONG HONG , 彭吉寧 JINLIN PENG
IPC分类号： G01N
CPC分类号： G01N33/582 , C07K7/083 , C07K14/63 , G01N33/6845 , G01N33/74 , G01N2333/63 , G01N2333/726
摘要：螢光配位體包含一種材料，其鍵結親合力在0.01至25nM範圍內，或0.1至10nM範圍內，對其同類受納體明確度在50％至99％範圍內，或65％至99％範圍內，對其他受納體交叉活性為0至20％，或0至10％；以及每一配位體之淨電荷為–3至＋5，優先地為–2至＋2，對於小化合物配位體最優先地為–1至＋2。配位體疏水性在特定洗提條件下之洗提時間在3至55分鐘範圍內。在一些實施例中，配位體包含螢光標定之motilin 1–16，其以Bodipy–TMR，若丹明或Cy5–標定。其他實施例包含螢光標定Cy5–麻醉藥拮抗劑，Cy5–神經加壓素2–13，N–終端標定神經加壓素2–13或1ys–標定神經加壓素2–13。
简体摘要：萤光配位体包含一种材料，其键结亲合力在0.01至25nM范围内，或0.1至10nM范围内，对其同类受纳体明确度在50％至99％范围内，或65％至99％范围内，对其他受纳体交叉活性为0至20％，或0至10％；以及每一配位体之净电荷为–3至＋5，优先地为–2至＋2，对于小化合物配位体最优先地为–1至＋2。配位体疏水性在特定洗提条件下之洗提时间在3至55分钟范围内。在一些实施例中，配位体包含萤光标定之motilin 1–16，其以Bodipy–TMR，若丹明或Cy5–标定。其他实施例包含萤光标定Cy5–麻醉药拮抗剂，Cy5–神经加压素2–13，N–终端标定神经加压素2–13或1ys–标定神经加压素2–13。

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