Given the current uncertain climate of pharmaceutical industry, with FDA
approved NCEs continue to stagger, antibacterial discovery faces unprecedented
challenges, however, huge opportunities exist because the well recognized medical
need for new agents to fi ght MDR bacterial infections, such as conditions caused by
MRSA and VRE, and also a strong industrial appeal for incentives to invest in this area
with orphan drug status, for instance, be granted to novel therapeutics. Here we use
one AstraZeneca discovery program to illustrate the challenges and opportunities. Th e
inhibition of essential cell-wall targets, such as Glutamate Racemase (MurI), provides
a great opportunity to design the next generation of antibacterials. Th is talk will be
focused on the recent eff orts of discovering MurI inhibitors in Gram-positive bacteria
and Gram-negative Helicobacter Pylori. Th e entire discovery process from High
Th roughput Screening, Lead Identifi cation and Lead Optimization will be presented.
Emphasis will be given to the demonstration of the power of HTS to discover allosteric
enzyme inhibitors and Structural Activity Relationship development employing
Structure-Based Drug Design approach.
Dr. Xiaoyan Jiang is a Senior Scientist in the Terry Fox Laboratory of the BC Cancer Agency,
an Associate Professor in the Department of Medical Genetics and an Associate Member in the
Department of Medicine at the University of British Columbia. She is also an Adjunct Professor
at the Shanghai Institute of Medical Genetics of the Shanghai Jiao Tong University. She serves
as an Editorial Board Member of 10 reputed journals, an external (ad hoc) reviewer for more
than 20 journals and a research grant reviewer in Canada and the USA. She has published 45
peers-reviewed publications and 75 Abstracts.
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