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- Butyrylcholinesterase (2)
- Cocaine (2)
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- Epilepsy (1)
- Epoxyketone (1)
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- Gene (1)
- Gilvocarcin (1)
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- Immunoproteasome (1)
Articles 1 - 10 of 10
Full-Text Articles in Pharmacy and Pharmaceutical Sciences
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.
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, …
Methods And Compositions For Optimizing Blood And Tissue Stability Of Camptothecin And Other Albumin-Binding Therapeutic Compounds, Thomas G. Burke, Daniel C. Carter
Methods And Compositions For Optimizing Blood And Tissue Stability Of Camptothecin And Other Albumin-Binding Therapeutic Compounds, Thomas G. Burke, Daniel C. Carter
Pharmaceutical Sciences Faculty Patents
The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves methodologies and formulations that limit human serum albumin-mediated reduction of the anti-cancer and anti-HIV effects of the camptothecins, and the methods and formulations provide combination therapies in which binding of the camptothecin agent to human serum albumin can be modulated by the administration of a competing agent that also binds human serum albumin. Reduced camptothecin drug binding to human serum albumin can result in elevated camptothecin free drug levels …
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.
Methods To Impair Hematologic Cancer Progenitor Cells And Compounds Related Thereto, Craig Jordan
Methods To Impair Hematologic Cancer Progenitor Cells And Compounds Related Thereto, Craig 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 leukemia (CML) and chronic lymphoid leukemia (CLL). Interleukin-3 receptor alpha chain (IL-3Rα or CD123) is strongly expressed on progenitor hematologic cancer cells, but is virtually undetectable on normal bone marrow cells. The present invention provides methods of impairing progenitor hematologic cancer (e.g., leukemia and lymphomic) cells by selectively targeting cells expressing CD123. These methods are useful in the detection and treatment of leukemias and malignant lymphoproliferative disorders. Also provided are compounds useful …
Epoxyketone-Based Immunoproteasome Inhibitors, Kyung Bo Kim, Yik Khuan Ho
Epoxyketone-Based Immunoproteasome Inhibitors, Kyung Bo Kim, Yik Khuan Ho
Pharmaceutical Sciences Faculty Patents
An efficient new route for the preparation of dihydroeponemycin, an active eponemycin derivative, is provided, which includes the synthesis of the intermediate compound, a hydroxymethyl-substituted enone. In addition, a method is provided for synthesizing inhibitors, which includes PI′-modified analogues. These analogues selectively bind to a major immunoproteasome catalytic subunit LMP2 and inactivate its proteolytic activity in a method of treating diseases, including myeloma and other cancers, Huntington's disease and Alzheimer's disease.