Open Access. Powered by Scholars. Published by Universities.®

Pharmacy and Pharmaceutical Sciences Commons

Open Access. Powered by Scholars. Published by Universities.®

Articles 1 - 13 of 13

Full-Text Articles in Pharmacy and Pharmaceutical Sciences

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.


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 Feb 2014

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 Feb 2014

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 Jan 2014

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.