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Full-Text Articles in Pharmacy and Pharmaceutical Sciences

Sesquiterpene Synthase Gene And Protein, Joseph Chappell, Bryan T. Greenhagen Jan 2017

Sesquiterpene Synthase Gene And Protein, Joseph Chappell, Bryan T. Greenhagen

Pharmaceutical Sciences Faculty Patents

The invention relates to sesquiterpene synthases and methods for their production and use. Particularly, the invention provides nucleic acids comprising the nucleotide sequence of citrus valencene synthase (CVS) which codes for at least one CVS. The invention further provides nucleic acids comprising the nucleotide sequence coding for amino acid residues forming the tier 1 and tier 2 domains of CVS. The invention also provides for methods of making and using the nucleic acids and amino acids of the current invention.


Bis-Quaternary Ammonium Salts As Pain Modulating Agents, Joseph R. Holtman, Peter A. Crooks, Linda Phyliss Dwoskin, J. Michael Mcintosh Nov 2016

Bis-Quaternary Ammonium Salts As Pain Modulating Agents, Joseph R. Holtman, Peter A. Crooks, Linda Phyliss Dwoskin, J. Michael Mcintosh

Pharmaceutical Sciences Faculty Patents

Provided are methods for using his-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.


Proteasome Inhibitors, Kyung Bo Kim, Venod Kasam, Wooin Lee, Dong-Eun Kim, Zachary Miller, Chang-Guo Zhan, Do-Min Lee Nov 2016

Proteasome Inhibitors, Kyung Bo Kim, Venod Kasam, Wooin Lee, Dong-Eun Kim, Zachary Miller, Chang-Guo Zhan, Do-Min Lee

Pharmaceutical Sciences Faculty Patents

To see this patent's abstract, please download it.


Method And System For Producing Triterpenes, Joe Chappell, Thomas D. Niehaus, Shigeru Okada, Timothy P. Devarenne, David Watt Nov 2016

Method And System For Producing Triterpenes, Joe Chappell, Thomas D. Niehaus, Shigeru Okada, Timothy P. Devarenne, David Watt

Pharmaceutical Sciences Faculty Patents

A method and system are provided for the production of triterpene including methylated triterpenes. The method and system include isolated nucleic acid sequences encoding triterpene methyltransferases such as triterpene methyltransferases 1, 2, 3. Advantageously, the method and system includes transgenic plant cells via an expression vector for triterpene methyltransferase and optionally various triterpene synthase and prenyltransferase all with tags directing these enzymes to the chloroplast of the transgenic plant cells for using the chloroplast methyl erythritol phosphate (MEP) pathway in the triterpene biogenesis.


Use Of Parthenolide Derivatives As Antileukemic And Cytotoxic Agents, Peter A. Crooks, Craig T. Jordan, Xiaochen Wei Sep 2016

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.


Semi-Synthetic Mithramycin Derivatives With Anti-Cancer Activity, Jürgen Rohr, Daniel Scott, Markos Leggas, Jhong-Min Chen, Oleg V. Tsodikov Sep 2016

Semi-Synthetic Mithramycin Derivatives With Anti-Cancer Activity, Jürgen Rohr, Daniel Scott, Markos Leggas, Jhong-Min Chen, Oleg V. Tsodikov

Pharmaceutical Sciences Faculty Patents

Mithramycin derivatives and their pharmaceutically acceptable salts are disclosed. The mithramycin derivatives can be used in the treatment of Ewing sarcoma or other cancer or neuro-disease associated with an aberrant erythroblast transformation- specific transcription factor.


High Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Wenchao Yang Aug 2016

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.


Sustained Release Of Topical Anesthetics, Michael Jay Jul 2016

Sustained Release Of Topical Anesthetics, Michael Jay

Pharmaceutical Sciences Faculty Patents

A composition and method to alleviate oral mucosal discomfort and irritation in an orthodontic patient. A wax matrix containing less that 15% analgesic/anesthetic agent such as benzocaine and excipients enhanced and extended release of the analgesic/anesthetic agent compared to known art formulations. The composition exhibited desirable aesthetic properties, was easy to apply, and the relatively lower concentration of active agent provided enhanced safety.


High Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Wenchao Yang, Liu Xue, Shurong Hou Jun 2016

High Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Wenchao Yang, Liu 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.


Flow-Through Filter To Remove Aluminum From Medical Solutions, Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Robert Joseph Kuhn, Vasiliy Paul Abramov, Jason Matthew Lone Feb 2016

Flow-Through Filter To Remove Aluminum From Medical Solutions, Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Robert Joseph Kuhn, Vasiliy Paul Abramov, Jason Matthew Lone

Pharmaceutical Sciences Faculty Patents

A flow through filter assembly includes a trivalent and tetravalent metal ion capturing agent and a flow controller providing a predetermined flow rate which allows capture of the trivalent and tetravalent metal ions by the capturing agent.


High-Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis And Method Of Generating The Same, Chang-Guo Zhan, Hoon Cho, Hsin-Hsiung Tai Dec 2015

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 Dec 2015

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 Nov 2015

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 Oct 2015

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 Sep 2015

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 Jul 2015

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 Jul 2015

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 Jun 2015

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 Apr 2015

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 Feb 2015

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.


Melampomagnolide B Derivatives As Antileukemic And Cytotoxic Agents, Peter A. Crooks, Craig T. Jordan, Shanshan Pei, Shama Nasim Nov 2014

Melampomagnolide B Derivatives As Antileukemic And Cytotoxic Agents, Peter A. Crooks, Craig T. Jordan, Shanshan Pei, Shama Nasim

Pharmaceutical Sciences Faculty Patents

Melampomagnolide B is disclosed as a new antileukemic sesquiterpene. A biotin-conjugated derivative of melampomagnolide B was prepared to elucidate its mechanism of action. Prodrugs of Melampomagnolide B are disclosed.


Ph-Sensitive Mucoadhesive Film-Forming Gels And Wax-Film Composites Suitable For Topical And Mucosal Delivery Of Molecules, Russell J. Mumper, Michael Jay Oct 2014

Ph-Sensitive Mucoadhesive Film-Forming Gels And Wax-Film Composites Suitable For Topical And Mucosal Delivery Of Molecules, Russell J. Mumper, Michael Jay

Pharmaceutical Sciences Faculty Patents

The present invention relates to pH-sensitive mucoadhesive film-forming gels and wax-film composites suitable for topical and mucosal delivery of molecules of interest, namely active pharmaceuticals. The gels comprise a pharmaceutically acceptable pH-sensitive polymer that responds to a lowering of pH by precipitating into films when in contact with the skin or mucosal surface. The films also comprise an adhesive polymer that allows the film to remain in contact with the tissue for an extended period of time. The wax-film composites comprise a bi-layer film having both the said pH-sensitive mucoadhesive layer to promote strong adherence to the skin and mucosal …


Methods To Impair Hematologic Cancer Progenitor Cells And Compounds Related Thereto, Craig T. Jordan Oct 2014

Methods To Impair Hematologic Cancer Progenitor Cells And Compounds Related Thereto, Craig T. Jordan

Pharmaceutical Sciences Faculty Patents

Primitive or progenitor hematologic cancer cells have been implicated in the early stages and development of leukemia and malignant lymphoproliferative disorders, including acute myelogenous leukemia (AML), chronic myelogenous leuke mia (CML) and chronic lymphoid leukemia (CLL). Interleu kin-3 receptor alpha chain (IL-3Ra or CD123) is strongly expressed on progenitor hematologic cancer cells, but is vir tually undetectable on normal bone marrow cells. The present invention provides methods of impairing progenitor hemato logic cancer (e.g., leukemia and lymphomic) cells by selec tively targeting cells expressing CD123. These methods are useful in the detection and treatment of leukemias and malig nant lymphoproliferative …


High Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Wenchao Yang Sep 2014

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.


Mono Quaternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter A. Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Zhenfa Zheng Sep 2014

Mono Quaternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter A. Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Zhenfa Zheng

Pharmaceutical Sciences Faculty Patents

Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.


High-Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis And Method Of Generating The Same, Chang-Guo Zhan, Hoon Cho, Hsin-Hsiung Tai Sep 2014

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, …


Use Of Parthenolide Derivatives As Antileukemic And Cytotoxic Agents, Peter A. Crooks, Craig T. Jordan, Xiaochen Wei May 2014

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.


Opioid-Ketamine And Norketamine Codrug Combinations For Pain Management, Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty Apr 2014

Opioid-Ketamine And Norketamine Codrug Combinations For Pain Management, Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty

Pharmaceutical Sciences Faculty Patents

The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and ketamine or norketamine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain.


Opioid-Nornicotine Codrugs Combinations For Pain Management, Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty Apr 2014

Opioid-Nornicotine Codrugs Combinations For Pain Management, Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty

Pharmaceutical Sciences Faculty Patents

The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and nornicotine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain.


Compositions And Methods For Selectively Targeting Cancer Cells Using A Thiaminase Compound, Jeffrey A. Moscow, Shuqian Liu, Younsoo Bae Mar 2014

Compositions And Methods For Selectively Targeting Cancer Cells Using A Thiaminase Compound, Jeffrey A. Moscow, Shuqian Liu, Younsoo Bae

Pharmaceutical Sciences Faculty Patents

Compositions and methods of treating cancer using a thiaminase compound are described. The presently-disclosed subject matter includes a method of treating cancer by administering a thiaminase compound and a thiamine-dependent enzyme inhibitor.