alexa Development Of Bacterial β-glucuronidase Specific Inhibitors To Reduce Chemo-induced Intestinal Toxicity And Diarrhea
ISSN: 1948-5956

Journal of Cancer Science & Therapy
Open Access

Like us on:
OMICS International organises 3000+ Global Conferenceseries Events every year across USA, Europe & Asia with support from 1000 more scientific Societies and Publishes 700+ Open Access Journals which contains over 50000 eminent personalities, reputed scientists as editorial board members.

Open Access Journals gaining more Readers and Citations

700 Journals and 15,000,000 Readers Each Journal is getting 25,000+ Readers

This Readership is 10 times more when compared to other Subscription Journals (Source: Google Analytics)

Share This Page

Additional Info

Loading Please wait..

Global Summit on Oncology & Cancer
May 25-27, 2017 Osaka, Japan

Kai-Wen Cheng
National Sun Yat-Sen University, Taiwan
Posters & Accepted Abstracts: J Cancer Sci Ther
DOI: 10.4172/1948-5956-C1-100
The direct inhibition of bacterial β-glucuronidase (βG) activity is expected to reduce the reactivation of glucuronide-conjugated drugs in the intestine, thereby limiting drug toxicity. In this study, we report on the effects of pyrazolo[4,3-c]quinoline derivatives acting as bacterial βG-specific inhibitors. These inhibitors exhibited potent inhibition of E. coli βG (eβG), but not human βG (hβG). The binding modes revealed that the inhibitors bound in the active site of eβG and formed a hydrogen bound relatively strong and stable interaction compared to hβG. Notably, the inhibitors acted effectively against endogenous βG in E. coli, and also had low cytotoxicity to the bacterial cells. The oral administration of one inhibitor, TCH-3511, reduced intestinal βG activity in mice in general, in addition to suppressing intestinal morphology damage in chemotherapeutic CPT-11-treated mice. Finally, CPT-11 treatment combined with the administration of TCH-3511 alleviated diarrhea while maintaining the anti-tumor efficacy in tumorbearing mice. These results suggest a novel and potent bacterial βG-specific inhibitor, TCH-3511, that would allow this inhibitor to be used for the purpose of reducing drug toxicity.

Kai-Wen Cheng received her BS degree in 2007 from Kaohsiung Medical University, Taiwan, with a major in Biomedical Science and Environmental Biology and MSc degree in 2009 from the Graduate Institute of Oral Biology at National Taiwan University. In 2011, she received the Master of Science degree in Cancer Immunology and Biotechnology from the University of Nottingham, UK. She is currently a PhD student at the Institute of Biomedical Sciences in National Sun Yat-Sen University, working in the laboratory of Prof. Tian-Lu Cheng for development of bacterial β-glucuronidase specific inhibitor. Her research interest is Antibody Therapy and Drug Discovery.

Email: [email protected]

image PDF   |   image HTML

Relevant Topics

Peer Reviewed Journals
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2017-18
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

© 2008-2017 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version