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1. 发明申请

US20120083527A1 Anticancer Agents 有权
标题翻译：抗癌剂
公开(公告)号：US20120083527A1
公开(公告)日：2012-04-05
申请号：US13263141
申请日：2010-04-16
申请人： Michael D. Burkart , James J. La Clair , Minjin Kang , Brian D. Jones , Alexander L. Mandel , Wei-Luen Yu , Justin C. Hammons
发明人： Michael D. Burkart , James J. La Clair , Minjin Kang , Brian D. Jones , Alexander L. Mandel , Wei-Luen Yu , Justin C. Hammons
IPC分类号： A61K31/365 , C12P17/18 , C12N9/96 , G01N33/53 , C07D493/16 , A61P35/00
CPC分类号： C07D493/18
摘要： The present disclosure relates generally to compositions and methods for treating cancer. In some aspects, novel spirohexenolides and methods of using and producing them are described.
摘要翻译：本公开一般涉及用于治疗癌症的组合物和方法。在一些方面，描述了新颖的螺烯烯内酯及其使用和制备方法。

2. 发明授权

US08653283B2 Anticancer agents 有权
标题翻译：抗癌剂
公开(公告)号：US08653283B2
公开(公告)日：2014-02-18
申请号：US13263141
申请日：2010-04-16
申请人： Michael D. Burkart , James J. La Clair , MinJin Kang , Brian D. Jones , Alexander L. Mandel , Wei-Luen Yu , Justin C. Hammons
发明人： Michael D. Burkart , James J. La Clair , MinJin Kang , Brian D. Jones , Alexander L. Mandel , Wei-Luen Yu , Justin C. Hammons
IPC分类号： C07D307/77
CPC分类号： C07D493/18
摘要： The present disclosure relates generally to compositions and methods for treating cancer. In some aspects, novel spirohexenolides and methods of using and producing them are described.
摘要翻译：本公开一般涉及用于治疗癌症的组合物和方法。在一些方面，描述了新颖的螺烯烯内酯及其使用和制备方法。

3. 发明授权

US08119364B2 Methods for generating analogs of coenzyme A 有权
标题翻译：生成辅酶A类似物的方法
公开(公告)号：US08119364B2
公开(公告)日：2012-02-21
申请号：US12789181
申请日：2010-05-27
申请人： Michael D. Burkart , Kristine Clarke , Andrew C. Mercer , James J. LaClair , Jordan Meier
发明人： Michael D. Burkart , Kristine Clarke , Andrew C. Mercer , James J. LaClair , Jordan Meier
IPC分类号： C12Q1/34 , C12P21/06 , C12N9/00 , C07H21/04
CPC分类号： C12P13/02
摘要： Methods to generate analogs of coenzyme A in vivo are disclosed. The methods to generate analogs of coenzyme A in a cell comprise reacting pantetheine or a derivative thereof with a reporter to form labeled pantetheine or a derivative thereof, contacting the cell with the labeled pantetheine or derivative thereof such that the labeled pantetheine or derivative thereof enters the cell, phosphorylating the labeled pantetheine or derivative thereof to form phosphopantetheine or a derivative thereof, adenylating the labeled phosphopantetheine or derivative thereof to form a labeled dephosphoCoenzyme A or derivative thereof, and phosphorylating the 3′-hydroxyl of the labeled dephosphoCoenzyme A or derivative thereof to form a labeled coenzyme A analog or derivative thereof.
摘要翻译：公开了在体内产生辅酶A的类似物的方法。在细胞中产生辅酶A的类似物的方法包括使泛美他啶或其衍生物与报告基团反应以形成标记的泛ant啶或其衍生物，使细胞与标记的泛ant啶或其衍生物接触，使得其标记的泛et啶或其衍生物进入细胞，磷酸化标记的泛曲坦或其衍生物以形成磷酸泛酸或其衍生物，将标记的磷酸泛酸或其衍生物腺苷酸化，形成标记的去磷酸辅酶A或其衍生物，并将标记的脱辅酶A或其衍生物的3'-羟基磷酸化形成标记的辅酶A类似物或其衍生物。

4. 发明授权

US07727738B2 Methods for generating analogs of coenzyme A 有权
标题翻译：生成辅酶A类似物的方法
公开(公告)号：US07727738B2
公开(公告)日：2010-06-01
申请号：US11485247
申请日：2006-07-11
申请人： Michael D. Burkart , Kristine Clarke , Andrew L Mercer , James J. LaClair , Jordan Meier
发明人： Michael D. Burkart , Kristine Clarke , Andrew L Mercer , James J. LaClair , Jordan Meier
IPC分类号： C12Q1/34 , C12P21/06 , C12N9/00 , C07H21/04
CPC分类号： C12P13/02
摘要： Methods to generate analogs of coenzyme A in vitro and in vivo are disclosed. The methods comprise reacting pantetheine or a derivative thereof with a reporter to form labeled pantetheine or a derivative thereof, phosphorylating the labeled pantetheine or derivative thereof to form phosphopantetheine or a derivative thereof, adenylating the labeled phosphopantetheine or derivative thereof to form a labeled dephosphoCoenzyme A or derivative thereof, and phosphorylating the 3′-hydrozyl of the labeled dephosphoCoenzume A or derivative thereof to form a labeled coenzyme A analog or derivative thereof.
摘要翻译：公开了在体外和体内产生辅酶A类似物的方法。所述方法包括使泛美他啶或其衍生物与报告基团反应形成标记的泛麦角苷或其衍生物，磷酸化标记的泛麦角内苷或其衍生物以形成磷酸泛酸或其衍生物，将标记的磷酸泛酸或其衍生物腺苷酸化以形成标记的去磷酸辅酶A或衍生物，并磷酸化标记的去磷酸辅酶A或其衍生物的3'-羟基以形成标记的辅酶A类似物或其衍生物。

5. 发明授权

US07279304B2 Methods for preparation of macrocyclic molecules and macrocyclic molecules prepared thereby 失效
标题翻译：制备由此制备的大环分子和大环分子的方法
公开(公告)号：US07279304B2
公开(公告)日：2007-10-09
申请号：US10017324
申请日：2001-12-15
申请人： Christopher Thomas Walsh , John W. Trauger , Rahul Manu Kohli , Michael D. Burkart , Mohammed A. Maraheil , Henning Dieter Mootz , Dirk Schwarzer
发明人： Christopher Thomas Walsh , John W. Trauger , Rahul Manu Kohli , Michael D. Burkart , Mohammed A. Maraheil , Henning Dieter Mootz , Dirk Schwarzer
IPC分类号： C12P1/00 , C12P21/06
CPC分类号： C12P17/00 , C07K7/66
摘要： The preparation of macrocyclic molecules from linear, synthetic thioester precursors is disclosed. An excised thioesterase domain isolated from either a polyketide synthases (PKS) or non-ribosomal peptide synthetases (NRPS) multido system catalyzes the cyclization reaction. Thioester substrates also are described that are efficiently cyclized by the method of the present invention. Additionally, macrocyclic molecules, including macrolactones and macrolactams, that are prepared by the macrocyclization methods of the invention are described.
摘要翻译：公开了从线性合成硫酯前体制备大环分子。从聚酮化合物合酶（PKS）或非核糖体肽合成酶（NRPS）多系统分离的切除的硫酯酶结构域催化环化反应。也描述了通过本发明的方法有效环化的硫酯基质。此外，描述了通过本发明的大环化法制备的大环内酯，包括大内酯和大环内酯。

6. 发明申请

US20100304430A1 Methods for Generating Analogs of Coenzyme A 有权
标题翻译：生产辅酶A类似物的方法
公开(公告)号：US20100304430A1
公开(公告)日：2010-12-02
申请号：US12789181
申请日：2010-05-27
申请人： Michael D. Burkart , Kristine Clarke , Andrew C. Mercer , James J. LaClair , Jordan Meier
发明人： Michael D. Burkart , Kristine Clarke , Andrew C. Mercer , James J. LaClair , Jordan Meier
IPC分类号： C12P21/00 , C12P19/32
CPC分类号： C12P13/02
摘要： Methods to generate analogs of coenzyme A in vivo are disclosed. The methods to generate analogs of coenzyme A in a cell comprise reacting pantetheine or a derivative thereof with a reporter to form labeled pantetheine or a derivative thereof, contacting the cell with the labeled pantetheine or derivative thereof such that the labeled pantetheine or derivative thereof enters the cell, phosphorylating the labeled pantetheine or derivative thereof to form phosphopantetheine or a derivative thereof, adenylating the labeled phosphopantetheine or derivative thereof to form a labeled dephosphoCoenzyme A or derivative thereof, and phosphorylating the 3′-hydroxyl of the labeled dephosphoCoenzyme A or derivative thereof to form a labeled coenzyme A analog or derivative thereof.
摘要翻译：公开了在体内产生辅酶A的类似物的方法。在细胞中产生辅酶A的类似物的方法包括使泛美他啶或其衍生物与报告基团反应以形成标记的泛ant啶或其衍生物，使细胞与标记的泛ant啶或其衍生物接触，使得标记的泛et啶或其衍生物进入细胞，磷酸化标记的泛曲坦或其衍生物以形成磷酸泛酸或其衍生物，将标记的磷酸泛酸或其衍生物腺苷酸化，形成标记的去磷酸辅酶A或其衍生物，并将标记的脱辅酶A或其衍生物的3'-羟基磷酸化形成标记的辅酶A类似物或其衍生物。

7. 发明授权

US06255088B1 Enzymatic sulfation of biomolecules 失效
标题翻译：生物分子的酶硫酸化
公开(公告)号：US06255088B1
公开(公告)日：2001-07-03
申请号：US09393013
申请日：1999-09-10
申请人： Chi-Huey Wong , Michael D. Burkart
发明人： Chi-Huey Wong , Michael D. Burkart
IPC分类号： C12P1100
CPC分类号： C12N9/13
摘要： Enzymatic sulfations of biomolecules catalyzed by 3′-phosphoadenosine-5′-phosphosulfate (PAPS) dependent sulfotransferases are enhanced by coupling the sulfation reaction an enzymatic regeneration of PAPS. The PAPS is enzymatically regenerated from its hydrolysis product 3′,5′-diphosphate (PAP) using recombinant aryl sulfotransferase as the catalyst and aryl sulfate as the substrate. Biomolecules capable of enhanced sulfation by this method include carbohydrates, oligosaccharides, peptides, proteins, flavonoids, and steroids. When enzymatic sulfation and substrate regeneration steps are coupled, the desulfated aryl group produced in the regeneration step has a spectroscopic signature that can be employed for monitoring the progress of the sulfation of the biomolecule.
摘要翻译：通过将硫酸化反应与PAPS的酶促再生耦合，增强了由3'-磷酸腺苷-5'-磷酸硫酸酯（PAPS）依赖的磺基转移酶催化的生物分子的酶促硫酸化。使用重组芳基磺基转移酶作为催化剂和芳基硫酸盐作为底物，将PAPS从其水解产物3'，5'-二磷酸（PAP）酶促再生。能够通过该方法增强硫酸化的生物分子包括碳水化合物，寡糖，肽，蛋白质，类黄酮和类固醇。当酶促硫酸化和底物再生步骤偶联时，在再生步骤中产生的脱硫芳基具有可用于监测生物分子的硫酸化进程的光谱特征。

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