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- Butyrylcholinesterase (16)
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- Hydrolysis (14)
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- High activity (10)
- Mutants (10)
- Thereof (10)
- Inhibitors (9)
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Articles 61 - 90 of 193
Full-Text Articles in Pharmacy and Pharmaceutical Sciences
Bis-Quaternary Ammonium Cyclophane Compounds That Interact With Neuronal Nicotinic Acetylcholine Receptors, Peter A. Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Davis D. Allen, Zhenfa Zheng, Paul Lockman
Bis-Quaternary Ammonium Cyclophane Compounds That Interact With Neuronal Nicotinic Acetylcholine Receptors, Peter A. Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Davis D. Allen, Zhenfa Zheng, Paul Lockman
Pharmaceutical Sciences Faculty Patents
Provided are bis-quaternary ammonium cyclophane 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.
Enhancing Transdermal Delivery Of Opioid Antagonists And Agonists Using Codrugs Linked To Bupropion Or Hydroxybupropion, Audra L. Stinchcomb, Peter A. Crooks, Mohamad O. Hamad, Paul K. Kiptoo
Enhancing Transdermal Delivery Of Opioid Antagonists And Agonists Using Codrugs Linked To Bupropion Or Hydroxybupropion, Audra L. Stinchcomb, Peter A. Crooks, Mohamad O. Hamad, Paul K. Kiptoo
Pharmaceutical Sciences Faculty Patents
The present invention is directed to novel codrugs comprising bupropion or hydroxybupropion and an opioid antagonist or an opioid agonist joined together by chemical bonding. The codrugs provide a significant increase in the transdermal flux across human skin, as compared to the basic opioid antagonist or opioid agonist.
Tetrakis-Quaternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acteylcholine Receptors, Peter A. Crooks, Linda P. Dwoskin, Zhnefa Zhang, Marharyta Pivavarchyk
Tetrakis-Quaternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acteylcholine Receptors, Peter A. Crooks, Linda P. Dwoskin, Zhnefa Zhang, Marharyta Pivavarchyk
Pharmaceutical Sciences Faculty Patents
Provided are tetrakis-quaternary 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, 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.
Bis-Pyridino Containing Compounds For The Use In The Treatment Of Cns Pathologies, Peter A. Crooks, Linda P. Dwoskin, Joshua Ayers, Vladimir Grinevich, Sangeetha Sumithran
Bis-Pyridino Containing Compounds For The Use In The Treatment Of Cns Pathologies, Peter A. Crooks, Linda P. Dwoskin, Joshua Ayers, Vladimir Grinevich, Sangeetha Sumithran
Pharmaceutical Sciences Faculty Patents
N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.
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 view this abstract, please download this patent.
Glycosylate Derivatives Of Mithramycin, Method Of Preparation And Uses Thereof, Jürgen Rohr, Irfan Baig, Jose Antonio Salas Fernandez, Alfredo Fernandez Brana, Maria Perez Solares
Glycosylate Derivatives Of Mithramycin, Method Of Preparation And Uses Thereof, Jürgen Rohr, Irfan Baig, Jose Antonio Salas Fernandez, Alfredo Fernandez Brana, Maria Perez Solares
Pharmaceutical Sciences Faculty Patents
The present invention provides compounds characterized by the formula (I), where each of the substituent radicals is described in the specification. The invention also describes the use of said compounds in the treatment of various diseases, including: cancer or tumoral processes in general, Paget's disease, hypercalcaemia, hypercalciuria and neurological diseases (inter alia, Parkinson's, Alzheimer's, Huntington's).
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 W. Landry, Joanne Macdonald, Shi-Xiang Deng, Chang-Guo Zhan, Daquan Gao, James H. Woods, Roger K. Sunahara, Diwahar L. Narasimhan, Victor Yang, Mei-Chuan Holden Ko, John J. Tesmer, Tien-Yi Lee, Young Min Kwon
Anti-Cocaine Compositions And Treatment, Donald W. Landry, Joanne Macdonald, Shi-Xiang Deng, Chang-Guo Zhan, Daquan Gao, James H. Woods, Roger K. Sunahara, Diwahar L. Narasimhan, Victor Yang, Mei-Chuan Holden Ko, John J. Tesmer, Tien-Yi Lee, Young Min Kwon
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.
Indole Compounds And Their Use As Radiation Sensitizing Agents And Chemotherapeutic Agents, Peter A. Crooks, Thirupathi R. Yerramreddy, Narsimha Reddy Penthala, Michael L. Freeman, Sekhar R. Konjeti
Indole Compounds And Their Use As Radiation Sensitizing Agents And Chemotherapeutic Agents, Peter A. Crooks, Thirupathi R. Yerramreddy, Narsimha Reddy Penthala, Michael L. Freeman, Sekhar R. Konjeti
Pharmaceutical Sciences Faculty Patents
Indole derivatives that are useful in the treatment of cancer as a chemotherapeutic agent or radiosensitizing agent.
Tris-Quarternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
Tris-Quarternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
Pharmaceutical Sciences Faculty Patents
Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine 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, 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.
Intranasal Opioid Compositions, Daniel Wermeling
Intranasal Opioid Compositions, Daniel Wermeling
Pharmaceutical Sciences Faculty Patents
The present invention relates to pharmaceutical compositions for intranasal administration to a mammal that contain an effective amount of an opioid, a liquid nasal carrier for the opioid, and optionally a sweetener, flavoring agent or masking agent. In some embodiments of the present invention, the pharmaceutical compositions have improved bioavailability. In other embodiments of the present invention, the opioid compositions improve patient compliance.
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, …
Bis-Quaternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Marharyta Pivavarchyk
Bis-Quaternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Marharyta Pivavarchyk
Pharmaceutical Sciences Faculty Patents
Provided are bis-quaternary 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.
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 view this abstract, please download this patent.
Enantioselective Synthesis Of (+) And (–)-2-[1-(2,6-Dichlorophenoxy)-Ethyl]-1,3-Diazacyclopent-2-Ene, Peter A. Crooks, Ashish Pramod Vartak
Enantioselective Synthesis Of (+) And (–)-2-[1-(2,6-Dichlorophenoxy)-Ethyl]-1,3-Diazacyclopent-2-Ene, Peter A. Crooks, Ashish Pramod Vartak
Pharmaceutical Sciences Faculty Patents
Methods for the enantioselective synthesis of (+) and (−) lofexidine or 2-[1-(2,6)-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene involve converting (+) or (−) 1-methyl-1-[2,6-dichlorophenoxy]ethanamide to an (+) or (−) imino-ether intermediate by electrophilic attack of the amide oxygen by a trimethoxonium ion and, without isolation, converting the (+) or (−) imino-ether intermediate to (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene by adding ethylene diamine; and optionally converting the (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene into a pharmaceutically acceptable acid addition salt thereof.
Liposomal, Ring-Opened Camptothecins With Prolonged, Site-Specific Delivery Of Active Drug To Solid Tumors, Bradley D. Anderson, Vijay Joguparthi, Tiang-Xiang Xiang
Liposomal, Ring-Opened Camptothecins With Prolonged, Site-Specific Delivery Of Active Drug To Solid Tumors, Bradley D. Anderson, Vijay Joguparthi, Tiang-Xiang Xiang
Pharmaceutical Sciences Faculty Patents
A method for preparing a stable dispersion of a camptothecin, camptothecin prodrug, or analog thereof for administration to a patient in need thereof includes preparing a solution of the camptothecin, wherein the solution has a pH which places substantially an entirety of that camptothecin in a carboxylate form. The camptothecin may be a neutral camptothecin. The solution is next loaded into a liposome including at least one lipid, which may be a phospholipid. An intraliposomal pH is maintained which preserves substantially an entirety of the camptothecin in the carboxylate form. The liposomal dispersion is administered to an individual in need …
Removing Aluminum From Solution Using Chelating Compounds And Immobilized Tethered Chelators, Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Chang-Guo Zhan
Removing Aluminum From Solution Using Chelating Compounds And Immobilized Tethered Chelators, Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Chang-Guo Zhan
Pharmaceutical Sciences Faculty Patents
Methods are described for removing aluminum from a solution using novel di- and tripodal compounds as chelators.
Methods And Pharmaceutical Compositions For Decorporation Of Radioactive Compounds, Michael Jay, Russell J. Mumper
Methods And Pharmaceutical Compositions For Decorporation Of Radioactive Compounds, Michael Jay, Russell J. Mumper
Pharmaceutical Sciences Faculty Patents
A composition for removing a radioactive element or compound such as systemic transuranic compounds, from mammals comprises a pharmaceutical carrier and a decorporation agent comprising ester and amide derivatives of DTPA. A method of treating a mammal to remove systemic compounds utilizing the DTPA derivatives is also disclosed.
Camptothecin Analogs And Methods Of Preparation Thereof, Dennis P. Curran, David Bom, Thomas Burke
Camptothecin Analogs And Methods Of Preparation Thereof, Dennis P. Curran, David Bom, Thomas Burke
Pharmaceutical Sciences Faculty Patents
To read this abstract, please download this patent.
Berry Preparations And Extracts, Russell J. Mumper, Jin Dai, Vincent S. Gallicchio
Berry Preparations And Extracts, Russell J. Mumper, Jin Dai, Vincent S. Gallicchio
Pharmaceutical Sciences Faculty Patents
A method for deriving compositions having antioxidant and anti-inflammatory activity from berries is provided. The method results in a berry extract compositions having stable anthocyanin content. In one aspect, the method comprises exposing a berry to a solvent composition having a pH of from about 1 to about 4.5, and recovering a berry extract having a stabilized anthocyanin content. The berry may be a blackberry. A cryoprotectant may be added, to further stabilize the anthocyanin content. Compositions comprising the berry extract of the present invention, formulated for oral and/or topical administration, are provided also, including nutritional supplements, capsules, enteric-coated capsules, …
Chelating Compounds And Immobilized Tethered Chelators, Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Chang-Guo Zhan
Chelating Compounds And Immobilized Tethered Chelators, Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Chang-Guo Zhan
Pharmaceutical Sciences Faculty Patents
Novel di- and tripodal compounds useful as chelators, intermediates for their production and a method for treating an aqueous solution to remove trivalent metal ions are presented.
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, …
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.
Agmatine And Agmatine Analogs In The Treatment Of Epilepsy, Seizure, And Electroconvulsive Disorders, Peter A. Crooks, Aimee K. Bence, David R. Worthen
Agmatine And Agmatine Analogs In The Treatment Of Epilepsy, Seizure, And Electroconvulsive Disorders, Peter A. Crooks, Aimee K. Bence, David R. Worthen
Pharmaceutical Sciences Faculty Patents
Pharmaceutical preparations containing of agmatine, congeners, analogs or derivatives thereof for use in preventing or treating epilepsy, seizures and other electroconvulsive disorders are provided. Embodiments include administering an effective amount of agmatine, an agmatine analog or a pharmaceutically acceptable salt thereof to a human subject in need of treatment or prevention of epilepsy, seizure or other electroconvulsive disorder to treat, reduce, or prevent the disorder in the subject.
Ph-Sensitive Mucoadhesive Film-Forming Gels And Wax-Film Composites Suitable For Topical And Mucosal Delivery Of Molecules, Russell J. Mumper, Michael Jay
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 …
Gilvocarcin Gene Cluster, Recombinant Production And Use Thereof, Jürgen Rohr, Carsten Fischer
Gilvocarcin Gene Cluster, Recombinant Production And Use Thereof, Jürgen Rohr, Carsten Fischer
Pharmaceutical Sciences Faculty Patents
A nucleic acid molecule encoding the gilvocarcin V gene cluster and subunits thereof. Recombinant vectors and host cells comprising a nucleic acid compound encoding the gilvocarcin V gene cluster or subunits thereof. Host cells comprising recombinant vectors encoding the gilvocarcin polyketide synthase and gilvocarcin post-PKS modifying enzymes from Streptomyces griseoflavus can be used to produce gilvocarcin and functional gilvocarcin mutants, analogs and derivatives thereof with application as antibiotics, anticancer agents, immunosuppressants, antivirals, and neuroprotective agents.
Bioactive Peptide-Based Probes, Clair D. Hicks, Peter A. Crooks
Bioactive Peptide-Based Probes, Clair D. Hicks, Peter A. Crooks
Pharmaceutical Sciences Faculty Patents
A method for preparing a site-specific peptide probe, wherein the peptide is specific to a receptor, includes modifying a marker to include a tether molecule and covalently binding the tether molecule to the peptide. The present invention also provides a labeled probe, comprising a peptide specific for a receptor and a marker. The marker is modified to include a tether molecule capable of covalently binding to the peptide. The peptide is typically derived from a bacteriophage or is a synthetic analog or derivative of the peptide. The receptor will typically be found on a surface of a bacterial cell. The …
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.