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1. 发明授权

US07396926B2 Beta-lactamase substrates having phenolic ethers 有权
标题翻译：具有酚醚的β-内酰胺酶底物
公开(公告)号：US07396926B2
公开(公告)日：2008-07-08
申请号：US10044486
申请日：2002-01-11
申请人： Roger Y. Tsien , Jianghong Rao
发明人： Roger Y. Tsien , Jianghong Rao
IPC分类号： C07D501/34 , C07D501/30 , C07D501/28 , C07D501/24 , C07D505/18 , C07D505/20 , C07D519/06 , G01N33/573 , C07D463/22 , C07D463/20 , C07D463/18
CPC分类号： C12Q1/6897 , C07D463/18 , C07D501/00 , C07D505/00 , C07F9/65613 , C12Q1/34
摘要： Provided are fluorescent substrates for β-lactamases having the general formula I: in which R is a benzyl, 2-thienylmethyl, or cyanomethyl group; R′ is selected from the group consisting of H, physiologically acceptable salts or metal, ester groups, ammonium cations, —CHR2OCO(CH2)nCH3, —CHR2OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, β-morpholinoethyl, dialkylaminoethyl, and dialkylaminocarbonyloxymethyl, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z is a donor fluorescent moiety. Also provided are methods of use of the compound of general formula I.
摘要翻译：提供具有通式I的β-内酰胺酶的荧光底物：其中R是苄基，2-噻吩基甲基或氰基甲基; R'选自H，生理上可接受的盐或金属，酯基，铵阳离子，-CHR 2 OCO（CH 2）n，（CH 3）3，酰基硫甲基，酰氧基-α- 苄基，异丙基丁内酰胺，甲氧基羰氧基甲基，苯基，甲基亚磺酰基甲基，β-吗啉代乙基，二烷基氨基乙基和二烷基氨基羰基氧基甲基，其中R 2选自H和低级烷基; A选自S，O，SO，SO 2和CH 2; Z是供体荧光部分。还提供了通式I化合物的使用方法。

2. 发明授权

US07427680B2 Fluorogenic substrates for BETA-lactamase gene expression 失效
标题翻译：荧光底物用于BETA-内酰胺酶基因表达
公开(公告)号：US07427680B2
公开(公告)日：2008-09-23
申请号：US10884019
申请日：2004-07-02
申请人： Roger Y. Tsien , Jianghong Rao
发明人： Roger Y. Tsien , Jianghong Rao
IPC分类号： C07D501/24 , G01N33/573
CPC分类号： C12Q1/6897 , C07D463/18 , C07D463/20 , C07D501/00 , C07D505/00 , C07F9/65613
摘要： Fluorescent substrates for beta-lactamases having the general formula shown above are provided. Z includes a fluorophore or chromophore and includes a group that may link to the lactam-containing group; R1 and R2 are independently selected from H, aliphatic, aromatic, alkyl, and acyl; R4 may be H and lower alkyl; B may be H, physiologically acceptable salts or metal, ester groups, ammonium cations, —CHR5OCO(CH2)nCH3, —CHR5OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benz, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, and dialkylaminocarbonyloxymethyl, in which R5 is selected from the group consisting of H and lower alkyl; n is an integer between 0 and 10, inclusive; and A may be S, O, SO, SO2 or CH2. In embodiments, the beta-lactam ring may be cleaved by a beta-lactamase enzyme effective to free a fluorophore. Methods of assaying beta-lactamase activity and monitoring expression in systems using beta-lactamase as a reporter gene are also disclosed.
摘要翻译：提供了具有上述通式的β-内酰胺酶的荧光底物。 Z包括荧光团或发色团，并且包括可以连接到含内酰胺基团的基团; R 1和R 2独立地选自H，脂族，芳族，烷基和酰基; R 4可以是H和低级烷基; B可以是H，生理上可接受的盐或金属，酯基，铵阳离子，-CHR 5 OCO（CH 2）n CH 2 （CH 3）3，酰基硫甲基，酰氧基-α-苯并三唑，丁内酰脲，甲氧羰基氧基甲基，苯基，甲基亚磺酰基甲基，β-吗啉代乙基，二烷基氨基乙基和二烷基氨基羰基氧基甲基，其中R 5选自H和低级烷基; n是0和10之间的整数，包括0和10; A可以是S，O，SO，SO 2或CH 2。在实施方案中，β-内酰胺环可以被有效释放荧光团的β-内酰胺酶切割。还公开了使用β-内酰胺酶作为报告基因的系统中测定β-内酰胺酶活性和监测表达的方法。

3. 发明申请

US20160376629A1 Use of Bacterial Beta-Lactamase for In Vitro Diagnostics and In Vivo Imaging, Diagnostics and Therapeutics 审中-公开
标题翻译：使用细菌β-内酰胺酶进行体外诊断和体内成像，诊断和治疗
公开(公告)号：US20160376629A1
公开(公告)日：2016-12-29
申请号：US15262374
申请日：2016-09-12
申请人： Jeffrey D. Cirillo , Jianghong Rao
发明人： Jeffrey D. Cirillo , Jianghong Rao
IPC分类号： C12Q1/18 , G01N21/64 , G01N21/78
CPC分类号： C12Q1/18 , A61K49/0013 , A61K49/0021 , A61K49/0028 , A61K49/0032 , A61K49/0041 , A61K49/0052 , C09B57/02 , C12Q1/04 , C12Q1/34 , C12Q1/66 , G01N21/6408 , G01N21/6428 , G01N21/78 , G01N2021/6417 , G01N2201/061 , G01N2333/986
摘要： Provided herein provided is an assay system for monitoring drug susceptibility of a pathogenic bacteria comprising color-producing substrates for a beta-lactamase of the pathogenic bacteria, an assay device for visibly detecting a product of the beta-lactamase on the substrate thereof and a reader configured to quantify the visibly detected product. Also provided is an in vitro method to determine susceptibility to a drug effective against a pathogenic bacteria, for example, a pathogenic Mycobacteria, that has a beta-lactamase activity. An excitation wavelength is delivered to a biological sample obtained from a subject having an infection from the pathogenic bacteria in the presence of a beta-lactamase substrate. The intensity of a signal, such as a fluorescent, luminescent or colorimetric signal, at an emission wavelength of a product of the beta-lactamase on the subject is correlated to drug susceptibility.
摘要翻译：本文提供了一种用于监测病原细菌的药物敏感性的测定系统，其包括致病细菌的β-内酰胺酶的着色产生底物，用于可见地检测其底物上的β-内酰胺酶的产物和读数器配置为量化可见检测到的产品。还提供了一种体外方法来确定对具有β-内酰胺酶活性的致病细菌例如致病分枝杆菌有效的药物的易感性。在β-内酰胺酶底物的存在下，将激发波长输送到从具有病原菌感染的受试者获得的生物样品。在受试者的β-内酰胺酶的产物的发射波长处的信号强度，例如荧光，发光或比色信号与药物敏感性相关。

4. 发明授权

US08592227B2 Hybrid quantum dot/protein nanostructure, methods of making, and methods of use thereof 失效
标题翻译：杂交量子点/蛋白质纳米结构，制备方法及其使用方法
公开(公告)号：US08592227B2
公开(公告)日：2013-11-26
申请号：US13068174
申请日：2011-05-04
申请人： Nan Ma , Jianghong Rao
发明人： Nan Ma , Jianghong Rao
IPC分类号： H01L21/00
CPC分类号： G01N33/582 , B82Y5/00 , B82Y15/00 , G01N33/588
摘要： Embodiments of the present disclosure include hybrid quantum dot/protein nanostructure, hybrid quantum dot/protein nanostructure systems, methods of using hybrid quantum dot/protein nanostructures, and the like.
摘要翻译：本公开的实施方案包括杂交量子点/蛋白质纳米结构，杂交量子点/蛋白质纳米结构体系，使用混合量子点/蛋白质纳米结构的方法等。

5. 发明授权

US08530178B2 Hydrolase detection system with caged substrates 失效
标题翻译：水解酶检测系统与笼式底物
公开(公告)号：US08530178B2
公开(公告)日：2013-09-10
申请号：US12445378
申请日：2007-10-17
申请人： Daniel Sobek , Jianghong Rao
发明人： Daniel Sobek , Jianghong Rao
IPC分类号： C12Q1/42
CPC分类号： C12Q1/34
摘要： An enzyme detection method includes forming a caged substrate; releasing an uncaged substrate by cleaving a caging molecule from the caged substrate; and emitting a light emission from a Bioluminescence Resonance Energy Transfer luminescent nanocrystal conjugate reacting with the uncaged substrate.
摘要翻译：酶检测方法包括形成笼状基材; 通过从笼形基底切割笼状分子释放未起皮的底物; 并且从与未起始的底物反应的生物发光共振能量转移发光纳米晶体共轭物发射发光。

6. 发明申请

US20120269734A1 Self-Illuminating Dot Systems and Methods of Use Thereof 失效
标题翻译：自发光点系统及其使用方法
公开(公告)号：US20120269734A1
公开(公告)日：2012-10-25
申请号：US13495208
申请日：2012-06-13
申请人： Jianghong Rao , Min-kyung So , Chenjie Xu , Andreas M. Loening , Sanjiv S. Gambhir
发明人： Jianghong Rao , Min-kyung So , Chenjie Xu , Andreas M. Loening , Sanjiv S. Gambhir
IPC分类号： C12N9/96 , A61K38/44 , G01N21/76 , A61K49/00 , B82Y15/00
CPC分类号： G01N33/543 , B82Y15/00 , G01N21/763 , G01N33/588
摘要： Generally, aspects of the present disclosure are directed to conjugate systems, self-illuminating quantum dot conjugates, methods of detecting a target in a host, methods of treating a disease in a host, and the like.
摘要翻译：通常，本公开的方面涉及共轭系统，自发光量子点缀合物，检测宿主中靶标的方法，治疗宿主中的疾病的方法等。

7. 发明申请

US20110278554A1 Hybrid quantum dot/protein nanostructure, methods of making, and methods of use thereof 失效
标题翻译：杂交量子点/蛋白质纳米结构，制备方法及其使用方法
公开(公告)号：US20110278554A1
公开(公告)日：2011-11-17
申请号：US13068174
申请日：2011-05-04
申请人： Nan Ma , Jianghong Rao
发明人： Nan Ma , Jianghong Rao
IPC分类号： H01L51/30 , H01L51/40
CPC分类号： G01N33/582 , B82Y5/00 , B82Y15/00 , G01N33/588
摘要： Embodiments of the present disclosure include hybrid quantum dot/protein nanostructure, hybrid quantum dot/protein nanostructure systems, methods of using hybrid quantum dot/protein nanostructures, and the like.
摘要翻译：本公开的实施方案包括杂交量子点/蛋白质纳米结构，杂交量子点/蛋白质纳米结构体系，使用混合量子点/蛋白质纳米结构的方法等。

8. 发明授权

US08518713B2 Self-illuminating dot systems and methods of use thereof 失效
标题翻译：自发光点系统及其使用方法
公开(公告)号：US08518713B2
公开(公告)日：2013-08-27
申请号：US13495208
申请日：2012-06-13
申请人： Jianghong Rao , Min-kyung So , Chenjie Xu , Andreas M. Loening , Sanjiv S. Gambhir
发明人： Jianghong Rao , Min-kyung So , Chenjie Xu , Andreas M. Loening , Sanjiv S. Gambhir
IPC分类号： G01N33/543
CPC分类号： G01N33/543 , B82Y15/00 , G01N21/763 , G01N33/588
摘要： Generally, conjugate systems, self-illuminating quantum dot conjugates, methods of detecting a target in a host, methods of treating a disease in a host, and the like, are described herein.
摘要翻译：通常，本文描述共轭体系，自发光量子点共轭体，检测宿主中靶标的方法，治疗宿主疾病的方法等。

9. 发明申请

US20130164221A1 USE OF BACTERIAL BETA-LACTAMASE FOR IN VITRO DIAGNOSTICS AND IN VIVO IMAGING, DIAGNOSTICS AND THERAPEUTICS 有权
标题翻译：用于体外诊断和体内成像，诊断和治疗的细菌β-乳糖酶的使用
公开(公告)号：US20130164221A1
公开(公告)日：2013-06-27
申请号：US13693706
申请日：2012-12-04
申请人： Jeffrey D. Cirillo , James C. Sacchettini , Jianghong Rao , Hexin Xie
发明人： Jeffrey D. Cirillo , James C. Sacchettini , Jianghong Rao , Hexin Xie
IPC分类号： A61K49/00 , G01N21/64
CPC分类号： A61K49/0021 , A61K49/0013 , A61K49/0028 , A61K49/0032 , A61K49/0041 , A61K49/0052 , C09B57/02 , C12Q1/04 , C12Q1/34 , G01N21/6486 , G01N2333/986
摘要： Provided herein are methods for detecting, quantifying, differentiating, diagnosing and imaging pathogenic bacteria or condition associated therewith using substrates for bacterial enzymes. Fluorescent, luminescent or colorimetric signals emitted by substrates or enzyme products in the presence of the bacteria are compared to controls to detect and locate the pathogenic bacteria. Provided is a method for screening therapeutic agents to treat the pathophysiological conditions by measuring a signal emitted from the substrates or products in the presence and absence of the potential therapeutic agent and a diagnostic method for detecting a mycobacterial infection in a subject by contacting biological samples with a substrate and imaging for signals emitted from a mycobacterial beta-lactamase product. Also provided are fluorogenic substrates or substrates comprising a colored dye or a chemical reagent effective to induce a color or pH change.
摘要翻译：本文提供了用于细菌酶底物检测，定量，鉴别，诊断和成像病原菌或与其相关的病症的方法。将在细菌存在下由底物或酶产物发射的荧光，发光或比色信号与对照物进行比较以检测和定位病原菌。本发明提供了一种用于筛选治疗剂以治疗病理生理状况的方法，该方法是通过在存在和不存在潜在治疗剂的情况下测量从底物或产物发出的信号，以及用于通过使生物样品与生物样品接触来检测受试者中的分枝杆菌感染的诊断方法底物和成像从分枝杆菌β-内酰胺酶产物发射的信号。还提供了含有色素或有效诱导颜色或pH变化的化学试剂的荧光底物或底物。

10. 发明申请

US20110201781A1 CYSTEINE LABELING SYSTEM AND METHOD OF USE THEREOF 审中-公开
标题翻译： CYSTEINE标记系统及其使用方法
公开(公告)号：US20110201781A1
公开(公告)日：2011-08-18
申请号：US12998105
申请日：2009-09-16
申请人： Jianghong Rao , Hongjun Ren
发明人： Jianghong Rao , Hongjun Ren
IPC分类号： C07K1/107 , C07C63/04 , C07K14/00 , C07K2/00
CPC分类号： C07D277/68 , A61K47/545 , A61K47/64
摘要： A method of use of a cysteine labeling system includes: providing a 2-cyano benzothial core with a covalently-linked biomolecule X in a reaction environment; and reacting the 2-cyano benzothial core to an N-terminal cystenine.
摘要翻译：半胱氨酸标记系统的使用方法包括：在反应环境中提供具有共价连接的生物分子X的2-氰基苯并核心; 并使2-氰基苯并核心与N-末端胱氨酸反应。

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