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Cocaine is one of the most addictive drugs without a U.S. Food and Drug Administration (FDA)-approved medication. Enzyme therapy using an efficient cocaine-metabolizing enzyme is recognized as the most promising approach to cocaine overdose treatment. The actual enzyme, known as RBP-8000, under current clinical development for cocaine overdose treatment is our previously designed T172R/G173Q mutant of bacterial cocaine esterase (CocE). The T172R/G173Q mutant is effective in hydrolyzing cocaine but inactive against benzoylecgonine (a major, biologically active metabolite of cocaine). Unlike cocaine itself, benzoylecgonine has an unusually stable zwitterion structure resistant to further hydrolysis in the body and environment. In fact, benzoylecgonine can last in the body for a very long time (a few days) and, thus, is responsible for the long-term toxicity of cocaine and a commonly used marker for drug addiction diagnosis in pre-employment drug tests. Because CocE and its mutants are all active against coc...
| Authors: | Xiabin Chen; Xirong Zheng; Max Zhan; Ziyuan Zhou; Chang-Guo Zhan; Fang Zheng | |
| Journal: | ACS Chemical Biology | |
| Year: | 2016 | |
| DOI: | 10.1021/acschembio.6b00277 | |
| Publication date: | 09-Jun-2016 |
Chemokine receptor CXCR4 plays an important role in cancer cell invasion and metastasis. Recent findings suggest that anti-VEGF therapies upregulate CXCR4 expression, which contributes to resistance to antiangiogenic therapies. Here, we report the development of novel derivatives of polyeth ... more
The molecular structures of three parthenolide analogues, (−)-goyazensolide (1), (−)-15-deoxygoyazensolide (2), and (−)-ereglomerulide (3), isolated from the leaves of Piptocoma rufescens in a previous study were determined by X-ray analysis, and the absolute configuration of (−)-goyazensol ... more
Mutual Impact of Phase Separation/Crystallization and Water Sorption in Amorphous Solid Dispersions
The molecular integration of poorly water soluble active pharmaceutical ingredients (APIs) in a suitable polymeric matrix is a possible approach to enhance the dissolution behavior and solubility of these APIs. Like all newly developed pharmaceutical formulations, these formulations (often ... more
Discovery of a biochemical basis for broccoli's cancer-fighting ability
Scientists are reporting discovery of a potential biochemical basis for the apparent cancer-fighting ability of broccoli and its veggie cousins. They found for the first time that certain substances in the vegetables appear to target and block a defective gene associated with cancer. Their ... more
Faster, more cost-effective DNA test for crime scenes, disease diagnosis
Scientists in Japan are reporting development of a faster, less expensive version of the fabled polymerase chain reaction (PCR) a DNA test widely used in criminal investigations, disease diagnosis, biological research and other applications. The new method could lead to expanded use of PCR ... more
'Nanoshells' simultaneously detect and destroy cancerous cells
Researchers at Rice University in Texas have developed a new approach to fighting cancer, based on nanoscale particles that can both detect and destroy cancerous cells. The report appears in the American Chemical Society's journal Nano Letters. Current molecular imaging approaches only dete ... more
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