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- Treatment (4)
- Butyrylcholinesterase (3)
- Cocaine (3)
- High activity (3)
- Hydrolysis (3)
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- Mutants (3)
- Cancer (2)
- Agents (1)
- Ammonium (1)
- Analogs (1)
- Anti-cocaine (1)
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- Applications (1)
- Bioimaging (1)
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- Cytotoxic Agents (1)
- Design (1)
- Discovery (1)
- Disease (1)
- Drug (1)
- Hybrid nanocrystals (1)
- Methods (1)
- Microcystins (1)
- Modeling (1)
- Modulating agents (1)
- Mpges-1 (1)
- Pain (1)
- Parthenolide Derivatives (1)
- Salts (1)
- Stilbene (1)
Articles 1 - 10 of 10
Full-Text Articles in Pharmacy and Pharmaceutical Sciences
High-Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis And Method Of Generating The Same, Chang-Guo Zhan, Hoon Cho, Hsin-Hsiung Tai
High-Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis And Method Of Generating The Same, Chang-Guo Zhan, Hoon Cho, Hsin-Hsiung Tai
Pharmaceutical Sciences Faculty Patents
A novel computational method and generation of mutant butyrylcholinesterase for cocaine hydrolysis is provided. The method includes molecular modeling a possible BChE mutant and conducting molecular dynamics simulations and hybrid quantum mechanical/molecular mechanical calculations thereby providing a screening method of possible BChE mutants by predicting which mutant will lead to a more stable transition state for a rate determining step. Site-directed mutagenesis, protein expression, and protein activity is conducted for mutants determined computationally as being good candidates for possible BChE mutants, i.e., ones predicted to have higher catalytic efficiency as compared with wild-type BChE. In addition, mutants A199S/A328W/Y332G, A199S/F227A/A328W/Y332G, A199S/S287G/A328W/Y332G, …
Anti-Cocaine Compositions And Treatment, Donald Landry, Chang-Guo Zhan, James H. Woods, Roger Sunahara, Diwahar L. Narasimhan, Joanne Macdonald, Victor Yang, Mei-Chuan Holden Ko, Shi-Xian Deng, John J. Tesmer, Tien-Yi Lee, Young Min Kwon, Daquan Gao
Anti-Cocaine Compositions And Treatment, Donald Landry, Chang-Guo Zhan, James H. Woods, Roger Sunahara, Diwahar L. Narasimhan, Joanne Macdonald, Victor Yang, Mei-Chuan Holden Ko, Shi-Xian Deng, John J. Tesmer, Tien-Yi Lee, Young Min Kwon, Daquan Gao
Pharmaceutical Sciences Faculty Patents
Embodiments of the invention disclosed herein generally relate to anti-cocaine therapeutics. Specifically, some embodiments of the invention relate to highly efficient, thermostable, and long-lasting cocaine esterase (CocE) mutants that can protect against the toxic and reinforcing effects of cocaine in subjects. Provided herein are mutant CocE polypeptides displaying thermostable esterase activity. Also provided are methods of treating cocaine-induced conditions in a subject in need via administration of mutant CocE as well as methods for high-throughput screening of candidate esterase polypeptides.
High Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Wenchao Yang
High Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Wenchao Yang
Pharmaceutical Sciences Faculty Patents
Butyrylcholinesterase (BChE) polypeptide variants of the presently-disclosed subject matter have enhanced catalytic efficiency for (-)-cocaine, as compared to wild-type BChE. Pharmaceutical compositions of the presently-disclosed subject matter include a BChE polypeptide variant having an enhanced catalytic efficiency for (-)-cocaine. A method of the presently-disclosed subject matter for treating a cocaine-induced condition includes administering to an individual an effective amount of a BChE polypeptide variant, as disclosed herein, to lower blood cocaine concentration.
Use Of Tris-Quaternary Ammonium Salts As Pain Modulating Agents, Joseph R. Holtman, Peter Anthony Crooks, Linda P. Dwoskin, J. Michael Mcintosh
Use Of Tris-Quaternary Ammonium Salts As Pain Modulating Agents, Joseph R. Holtman, Peter Anthony Crooks, Linda P. Dwoskin, J. Michael Mcintosh
Pharmaceutical Sciences Faculty Patents
Provided are tris-quatemary ammonium compounds which are modulators of nociception and pain.
Stilbene Analogs And Methods Of Treating Cancer, David Watt, Chunming Liu, Vitaliy M. Sviripa, Wen Zhang
Stilbene Analogs And Methods Of Treating Cancer, David Watt, Chunming Liu, Vitaliy M. Sviripa, Wen Zhang
Pharmaceutical Sciences Faculty Patents
Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.
Hybrid Nanocrystals For Treatment And Bioimaging Of Disease, Tonglei Li
Hybrid Nanocrystals For Treatment And Bioimaging Of Disease, Tonglei Li
Pharmaceutical Sciences Faculty Patents
Hybrid nanocrystals able to reach specific targets in the body for treatment and biological imaging are provided, as well as methods of making and administering same for treatment of disease conditions and for bioimaging and radiotherapy. The hybrid nanocrystals and methods can be used alone or in combination with other treatment and imaging modalities.
Modeling Of Mpges-1 Three-Dimensional Structures: Applications In Drug Design And Discovery, Chang-Guo Zhan, Xiaoqin Huang, Adel Hamza
Modeling Of Mpges-1 Three-Dimensional Structures: Applications In Drug Design And Discovery, Chang-Guo Zhan, Xiaoqin Huang, Adel Hamza
Pharmaceutical Sciences Faculty Patents
This invention relates to representations of prostaglandin synthase three-dimensional structures. Such representations are suitable for designing agents that modulate the activity of the enzyme by binding to the substrate binding domain.
Use Of Parthenolide Derivatives As Antileukemic And Cytotoxic Agents, Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
Use Of Parthenolide Derivatives As Antileukemic And Cytotoxic Agents, Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
Pharmaceutical Sciences Faculty Patents
To read this abstract, please download this patent.
Microcystins As Agents For Treatment Of Cancer, Noel R. Monks, Shuqian Liu, Jeffrey A. Moscow
Microcystins As Agents For Treatment Of Cancer, Noel R. Monks, Shuqian Liu, Jeffrey A. Moscow
Pharmaceutical Sciences Faculty Patents
This invention relates to the use of microcystins as agents for treatment of cancer. Also provided are methods of screening for microcystins with improved cytotoxicity.
High Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Wenchao Yang, Lin Xue, Shurong Hou
High Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Wenchao Yang, Lin Xue, Shurong Hou
Pharmaceutical Sciences Faculty Patents
Butyrylcholinesterase (BChE) polypeptide variants of the presently-disclosed subject matter have enhanced catalytic efficiency for (−)-cocaine, as compared to wild-type BChE. Pharmaceutical compositions of the presently-disclosed subject matter include a BChE polypeptide variant having an enhanced catalytic efficiency for (−)-cocaine. A method of the presently-disclosed subject matter for treating a cocaine-induced condition includes administering to an individual an effective amount of a BChE polypeptide variant, as disclosed herein, to lower blood cocaine concentration.