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1. 发明授权

US6051386A Methods for identifying chemicals that act as agonists or antagonists for receptors and other proteins involved in signal transduction via pathways that utilize G-proteins 失效
标题翻译：用于鉴定通过利用G蛋白途径参与信号转导的受体和其他蛋白质作为激动剂或拮抗剂的化学物质的方法
公开(公告)号：US6051386A
公开(公告)日：2000-04-18
申请号：US479121
申请日：1995-06-07
申请人： Michael R. Lerner , Ethan A. Lerner
发明人： Michael R. Lerner , Ethan A. Lerner
IPC分类号： C12Q1/02 , C07K14/705 , C12N5/10 , C12N15/09 , C12N15/12 , C12N15/85 , C12Q1/44 , C12Q1/48 , C12R1/91 , G01N33/50 , G01N33/566
CPC分类号： G01N33/5044 , C07K14/705 , C07K14/70571 , C12N15/85 , G01N33/5008 , G01N33/502 , G01N33/5041 , G01N33/566 , G01N2333/726 , G01N2500/10
摘要： A method for identifying a chemical that acts as an agonist for a G-protein coupled cell surface (GPC) receptor. The method comprises introducing to test cells of a pigment cell line capable of dispersing or aggregating their pigment in response to a specific stimulus and expressing an exogenous clone coding for the GPC receptor, a stimulant that sets an initial state of pigment disposition wherein the pigment is aggregated within the test cells if activation of the exogenous GPC receptor induces pigment dispersion, or introducing a stimulant that sets an initial state of pigment disposition wherein the pigment is dispersed within the test cells if activation of the exogenous GPC receptor induces pigment aggregation; contacting the test cells set in an initial state of pigment disposition with the test chemical; and determining whether the pigment disposition in the test cells treated with the chemical is changed from the initial state of pigment disposition, wherein a change in pigment disposition observed in the test cells expressing the exogenous GPC receptor indicates that the chemical is an agonist for the exogenous GPC receptor.
摘要翻译：用于鉴定作为G蛋白偶联细胞表面（GPC）受体的激动剂的化学物质的方法。该方法包括向测试细胞中引入能够响应于特定刺激而分散或聚集其颜料的颜料细胞系，并表达编码GPC受体的外源克隆，其是设置颜料配置的初始状态的刺激剂，其中颜料为如果外源性GPC受体的活化诱导颜料分散，或引入设定颜料配置的初始状态的刺激剂，则在测试细胞内聚集，其中如果外源GPC受体的激活诱导颜料聚集，则颜料分散在测试细胞内; 使初始颜料配置状态下的测试电池与测试化学品接触; 并且确定用化学物质处理的测试细胞中的颜料配置是否从颜料配置的初始状态改变，其中在表达外源GPC受体的测试细胞中观察到的颜料配置的变化表明该化学物质是外源性的激动剂 GPC受体。

2. 发明授权

US5462856A Methods for identifying chemicals that act as agonists or antagonists for receptors and other proteins involved in signal transduction via pathways that utilize G-proteins 失效
公开(公告)号：US5462856A
公开(公告)日：1995-10-31
申请号：US732476
申请日：1991-07-16
申请人： Michael R. Lerner , Ethan A. Lerner
发明人： Michael R. Lerner , Ethan A. Lerner
IPC分类号： C12Q1/02 , C07K14/705 , C12N5/10 , C12N15/09 , C12N15/12 , C12N15/85 , C12Q1/44 , C12Q1/48 , C12R1/91 , G01N33/50 , G01N33/566
CPC分类号： G01N33/5044 , C07K14/705 , C07K14/70571 , C12N15/85 , G01N33/5008 , G01N33/502 , G01N33/5041 , G01N33/566 , G01N2333/726 , G01N2500/10
摘要： A method for identifying a chemical that acts as an agonist for a G-protein coupled cell surface (GPC) receptor. The method comprises introducing to test cells of a pigment cell line capable of dispersing or aggregating their pigment in response to a specific stimulus and expressing an exogenous clone coding for the GPC receptor, a stimulant that sets an initial state of pigment disposition wherein the pigment is aggregated within the test cells if activation of the exogenous GPC receptor induces pigment dispersion, or introducing a stimulant that sets an initial state of pigment disposition wherein the pigment is dispersed within the test cells if activation of the exogenous GPC receptor induces pigment aggregation; contacting the test cells set in an initial state of pigment disposition with the test chemical; and determining whether the pigment disposition in the test cells treated with the chemical is changed from the initial state of pigment disposition, wherein a change in pigment disposition observed in the test cells expressing the exogenous GPC receptor indicates that the chemical is an agonist for the exogenous GPC receptor.

3. 发明授权

US5300097A Fiber optic psoriasis treatment device 失效
标题翻译：光纤银屑病治疗装置
公开(公告)号：US5300097A
公开(公告)日：1994-04-05
申请号：US947893
申请日：1992-09-18
申请人： Ethan A. Lerner , R. Rox Anderson , Michael R. Lerner
发明人： Ethan A. Lerner , R. Rox Anderson , Michael R. Lerner
IPC分类号： A61N5/06 , G02B6/10 , G02B6/26 , G02B6/42 , A61M5/06
CPC分类号： A61N5/0617 , G02B6/102 , G02B6/262 , G02B6/4298 , A61N2005/0661 , A61N5/0616
摘要： Disclosed is a therapeutic device including an optical source including means for generating ultraviolet (UV) radiation, and a light delivery apparatus. The light delivery apparatus includes a body member and a plurality of optical fibers extending therefrom. Each of the optical fibers includes a proximal tip affixed to the body member, a distal tip at the end of the fiber opposite the proximal tip, and means for coupling the generated radiation from the proximal tips of the fibers through the fibers, and to the distal tips. The distal tips are characterized by a radius of curvature in the range 0.25 to 2.0 mm. The coupling means includes a flexible central core disposed within a flexible outer cladding. The central core has a diameter in the range of 0.1 mm to 1.0 mm, and the cladding has a refraction less than the index of refraction of the core.
摘要翻译：公开了一种治疗装置，其包括包括用于产生紫外线（UV）辐射的装置的光源和光输送装置。光输送装置包括主体部件和从其延伸的多根光纤。每个光纤包括固定到本体构件的近端，在与近端相反的端部处的远端，以及用于将所产生的辐射从纤维的近端通过纤维耦合的装置，以及远端提示。远端尖端的特征在于曲率半径在0.25至2.0mm的范围内。联接装置包括设置在柔性外包层内的柔性中心芯。中心芯的直径在0.1mm至1.0mm的范围内，并且包层的折射小于芯的折射率。

4. 发明授权

US5294543A Inhibitor of platelet aggregation 失效
标题翻译：抑制血小板聚集
公开(公告)号：US5294543A
公开(公告)日：1994-03-15
申请号：US865166
申请日：1992-04-08
申请人： Ethan A. Lerner , Michael R. Lerner
发明人： Ethan A. Lerner , Michael R. Lerner
IPC分类号： A61K38/00 , C07K14/435 , C12N15/11 , C07K7/10 , C07K15/12 , C12N15/63
CPC分类号： C07K14/43581 , A61K38/00 , Y10S514/822 , Y10S514/824
摘要： Purified DNA comprising a sequence encoding chrysoptin.Chrysoptin can be used to alter the hemodynamic or hemostatic properties of an animal's blood by administering to the animal an effective amount of chrysoptin.
摘要翻译：纯化的DNA，其包含编码chrysoptin的序列。辣根素可用于通过向动物施用有效量的木霉素来改变动物血液的血液动力学或止血性质。

5. 发明授权

US07829298B2 Human G protein-coupled receptors for metabolic-related disorders 有权
标题翻译：人G蛋白偶联受体代谢相关疾病
公开(公告)号：US07829298B2
公开(公告)日：2010-11-09
申请号：US10930662
申请日：2004-08-31
申请人： David J. Unett , Ruoping Chen , Jeremy G. Richman , Daniel T. Connolly , Huong T. Dang , Bryan J. Choi , James N. Leonard , Yaron Hakak , Chen W. Liaw , Dominic P. Behan , Derek T. Chalmers , Michael R. Lerner , Kevin P. Lowitz
发明人： David J. Unett , Ruoping Chen , Jeremy G. Richman , Daniel T. Connolly , Huong T. Dang , Bryan J. Choi , James N. Leonard , Yaron Hakak , Chen W. Liaw , Dominic P. Behan , Derek T. Chalmers , Michael R. Lerner , Kevin P. Lowitz
IPC分类号： G01N33/53
CPC分类号： C07D403/02 , A01K2217/00 , A01K2227/105 , A01K2267/03 , A61K31/4439 , C07K14/705 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
摘要翻译：本发明涉及鉴定候选化合物是G蛋白偶联受体（GPCR）的调节剂的方法。在优选的实施方案中，GPCR是人。在其它优选实施方案中，GPCR与Gi偶联并降低细胞内cAMP的水平。在其它优选实施方案中，GPCR由脂肪细胞内源性表达。在进一步优选的实施方案中，GPCR抑制细胞内脂肪分解。在其它进一步优选的实施方案中，GPCR是烟酸受体。本发明还涉及使用所述GPCR的调节剂的方法。优选的调节剂是激动剂。本发明的激动剂可用作预防或治疗代谢相关疾病，包括血脂异常，动脉粥样硬化，冠心病，中风，胰岛素抵抗和2型糖尿病的治疗剂。

6. 发明授权

US4564597A Anti-Sm hybridoma 失效
标题翻译：抗Sm杂交瘤
公开(公告)号：US4564597A
公开(公告)日：1986-01-14
申请号：US244899
申请日：1981-03-18
申请人： Ethan A. Lerner , Michael R. Lerner
发明人： Ethan A. Lerner , Michael R. Lerner
IPC分类号： G01N33/53 , G01N33/564 , C12N5/00
CPC分类号： G01N33/564 , G01N33/5308 , G01N2800/104 , Y10S435/948 , Y10S436/804 , Y10S436/811 , Y10S436/815 , Y10S530/868
摘要： Anti-Sm antibodies are produced by the hybridoma technique and employed to test for lupus erythematosus in humans.
摘要翻译：抗Sm抗体通过杂交瘤技术产生并用于测试人类的红斑狼疮。

7. 发明授权

US06602856B1 Antagonists of alpha-melanocyte stimulating hormone and methods based thereon 失效
标题翻译： α-黑素细胞刺激激素的拮抗剂及其基础
公开(公告)号：US06602856B1
公开(公告)日：2003-08-05
申请号：US08373151
申请日：1995-01-17
申请人： J. Mark Quillan , Channa K. Jayawickreme , Michael R. Lerner
发明人： J. Mark Quillan , Channa K. Jayawickreme , Michael R. Lerner
IPC分类号： A61K3806
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0812 , C07K14/68
摘要： Peptide antagonists of &agr;-melanocyte stimulating hormone are disclosed, together with methods of inhibiting the effects of &agr;-melanocyte stimulating hormone on cells or tissues sensitive to that hormone. In particular, methods for lightening the pigmentation of skin and for treating malignant melanoma, as well as kits for practicing the invention are also disclosed.
摘要翻译：公开了α-黑素细胞刺激激素的肽拮抗剂，以及抑制α-黑素细胞刺激激素对对该激素敏感的细胞或组织的作用的方法。特别地，还公开了减轻皮肤色素沉着和治疗恶性黑素瘤的方法，以及用于实施本发明的试剂盒。

8. 发明授权

US06475733B1 Cell surface receptors for the detection and identification of compounds 失效
标题翻译：用于检测和鉴定化合物的细胞表面受体
公开(公告)号：US06475733B1
公开(公告)日：2002-11-05
申请号：US09647653
申请日：2000-10-04
申请人： Michael R. Lerner
发明人： Michael R. Lerner
IPC分类号： C12Q168
CPC分类号： C12N15/1058 , C12N15/1034 , C12Q1/6811 , G01N33/5005 , G01N33/566 , G01N33/6872 , G01N33/74 , G01N2333/726 , G01N2500/10
摘要： The invention exploits the evolutionary principles responsible for the development of the broad spectrum general odorant detector system, to create a cell-surface receptor based system capable of detecting and discriminating between thousands of chemicals. This is accomplished by subjecting a defined set of cell-surface receptors such as G-protein coupled receptors, tyrosine kinase receptors, and/or ion channels, to the types of evolutionary forces that have created the array of approximately 1,000 natural receptors used in general olfaction by higher animals. This goal is further accomplished by a ‘directed evolution-in-a-test-tube’ method, imposing very high rates of mutation and extremely strict selection criteria to create a sensor. The novel sensor of the present invention is selected using a sensitive melanophore-based functional bioassay.
摘要翻译：本发明利用了广泛的一般加臭剂检测器系统的发展的进化原理，以创建能够检测和区分数千种化学物质的基于细胞表面受体的系统。这是通过使一组限定的细胞表面受体（例如G蛋白偶联受体，酪氨酸激酶受体和/或离子通道）经受一定程度的进化而产生的，这些进化力已经产生了一般使用的大约1,000个天然受体阵列高等动物的嗅觉。该目标通过“定向进化试管”方法进一步完成，施加非常高的突变率和非常严格的选择标准来创建传感器。本发明的新型传感器使用敏感的黑素素的功能生物测定。

9. 发明授权

US5601992A Peptide library formats and methods relating thereto 失效
标题翻译：与其相关的肽文库格式和方法
公开(公告)号：US5601992A
公开(公告)日：1997-02-11
申请号：US303585
申请日：1994-09-09
申请人： Michael R. Lerner , Channa K. Jayawickreme , Ethan A. Lerner
发明人： Michael R. Lerner , Channa K. Jayawickreme , Ethan A. Lerner
IPC分类号： C12Q1/68 , C40B30/04 , G01N33/531 , G01N33/543 , G01N33/68 , G01N33/53
CPC分类号： C40B30/04 , G01N33/531 , G01N33/54353 , G01N33/6845 , G01N33/6878 , G01N2333/5758 , G01N2410/00
摘要： A method for detecting the interaction between an oligomeric molecule and a target is provided. A plurality of beads is applied to a substrate, each bead having associated therewith multiple copies of only a single oligomeric molecule. The beads are substantially spaced-apart from one another and are substantially immobilized on the substrate. Conditions are applied such that a substantial portion of the multiple copies associated with each bead can disassociate from and diffuse into the substrate, the substrate constructed and arranged to permit only substantially localized diffusion. A localized signal occurring as a result of the diffusion is detected. Coated beads and libraries of coated beads also are provided.
摘要翻译：提供了一种用于检测低聚物分子与靶标之间相互作用的方法。将多个珠子施加到基底上，每个珠粒具有仅具有单个寡聚分子的多个拷贝。珠子基本上彼此间隔开并且基本上固定在基底上。施加条件使得与每个珠子相关联的多个拷贝的大部分可以分离和扩散到基底中，所述基底被构造和布置成仅允许基本上局部扩散。检测出作为扩散结果发生的局部化信号。还提供涂覆的珠粒和涂覆的珠粒的文库。

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