alexa Natural Products Based FXR Antagonists: From Plant Constituents To In Vivo Active Molecules | 66703
ISSN: 2329-6836

Natural Products Chemistry & Research
Open Access

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)

2nd International Conference and Exhibition on Marine Drugs and Natural Products

Weishuo Fang
Institute of Materia Medica, China
ScientificTracks Abstracts: Nat Prod Chem Res
DOI: 10.4172/2329-6836-C1-013
Abstract
Farnesoid X Receptor (FXR), belonging to the nuclear receptor superfamily, has emerged as a key player in the control of multiple metabolic pathways. In May 2016, a steroidal FXR agonist obeticholic acid was approved by FDA for the treatment of Primary Biliary Cholangitis (PBC) in combination with Urso Deoxy Cholic Acid (UDCA) in adults with an inadequate response to UDCA, or as a single therapy in adults unable to tolerate UDCA, validating the utility of FXR interacting agents in human. Extensive studies on the discovery of FXR ligands in the past 1-2 decades has resulted in the report of some steroidal (natural ligand like) and non-steroidal FXR ligands. However, serious side effects were encountered during the application of FXR full agonists to animals and patients with diabetes and liver steatosis, so FXR partial agonists and antagonists have been actively pursued as alternatives to full agonists, although their number and structural diversity are still limited. Most of reported FXR antagonists to date are still steroidal molecules, including the first known antagonist guggulsterone, in addition to a few synthetic non-steroidal ones. In the pursuit of new chemo type of FXR interacting agents from natural products, we found some chalcones and pentacyclic triterpenes as FXR antagonists or co-activators. Further chemical manipulations were applied to optimize their Pharmacodynamics (PD) and Pharmacokinetics (PK) properties. Some benzopyrenes (Ia), benzoxepines (Ib), and substituted triterpenoids (II) were found as potent FXR antagonists, demonstrating hypolipidemic activity and hepatic protection ability in diabetic KKAy mice. These studies demonstrated natural products derived FXR antagonists could exert pharmacological activity in mice safely, which are of potential for the metabolic disease treatment.
Biography

Weishuo Fang has graduated from Peking Union Medical College and was awarded PhD degree in 1997. After two years' of Post-doctoral study in Florida State University, USA, he started his independent career in Institute of Materia Medica, Chinese Academy of Medical Sciences as a Professor. The major theme of his research lab is medicinal chemistry and chemical biology of bioactive natural products. Two research directions have been actively pursued by him in the past decade: Drug discovery against three distinct targets, including microtubule (protein-protein interaction), beta-secretase (enzyme) and farnesoid X receptor (nuclear receptor), to pursue therapeutic agents with new chemo types and/or with superior activity; and construction of a natural product-inspired library based on the privileged structure concept and its application to drug discovery to improve the efficiency of hit/lead 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 2018-19
 
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

Agri & Aquaculture Journals

Dr. Krish

[email protected]

+1-702-714-7001Extn: 9040

Biochemistry Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Business & Management Journals

Ronald

[email protected]

1-702-714-7001Extn: 9042

Chemistry Journals

Gabriel Shaw

[email protected]

1-702-714-7001Extn: 9040

Clinical Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Engineering Journals

James Franklin

[email protected]

1-702-714-7001Extn: 9042

Food & Nutrition Journals

Katie Wilson

[email protected]

1-702-714-7001Extn: 9042

General Science

Andrea Jason

[email protected]

1-702-714-7001Extn: 9043

Genetics & Molecular Biology Journals

Anna Melissa

[email protected]

1-702-714-7001Extn: 9006

Immunology & Microbiology Journals

David Gorantl

[email protected]

1-702-714-7001Extn: 9014

Materials Science Journals

Rachle Green

[email protected]

1-702-714-7001Extn: 9039

Nursing & Health Care Journals

Stephanie Skinner

[email protected]

1-702-714-7001Extn: 9039

Medical Journals

Nimmi Anna

[email protected]

1-702-714-7001Extn: 9038

Neuroscience & Psychology Journals

Nathan T

[email protected]

1-702-714-7001Extn: 9041

Pharmaceutical Sciences Journals

Ann Jose

[email protected]

1-702-714-7001Extn: 9007

Social & Political Science Journals

Steve Harry

[email protected]

1-702-714-7001Extn: 9042

 
© 2008- 2018 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version
Leave Your Message 24x7