*Seminar Series: SCMB Chemistry Seminar
*Location: AIBN Seminar Room
*Date: 29/05/2017
*Time: 13:00

Speaker #1 details
*Title of talk: Native State Mass Spectrometry in Fragment Based Drug Discovery
*Speaker's name: Prof. Sally-Ann Poulsen
*Speaker's organisation: Griffith Institute for Drug Discovery
Speaker's city/state/country:
Website: https://www.griffith.edu.au/professional-page/dr-sally-ann-poulsen
Talk Abstract: Fragment based drug discovery (FBDD) is a recently validated approach to identify small molecules as better chemical starting points for drug discovery. Since 2005, fragment screening has resulted in two FDA approved drugs and more than 30 drug candidates in clinical trials. The take-up of FBDD in academia, biotech and pharma is growing owing to this success.

FBDD is contingent on the development of robust analytical methods to identify weak, noncovalent protein−fragment interactions. In contrast to high throughput screening (HTS), where hit compounds are relatively potent (KDs in the nM to µM range), the binding interactions of hit fragments tend to be considerably weaker (KDs in the µM to mM range), so that fragment hits may not be as readily identified in classical biochemical screens as for HTS hits.

A number of biophysical techniques have been used to screen fragment libraries with some of the most popular techniques being NMR, SPR and X-ray crystallography. The use of mass spectrometry (MS) for fragment screening has remained relatively underexplored.[1] This presentation will demonstrate the application of MS as a complementary screening method in fragment-based drug discovery. Specifically we will discuss the discovery of new zinc binding chemotypes by fragment screening and a screening campaign employing SAR by MS.
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Speaker #2 details
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Other Details: Anybody wishing to meet with Prof. Poulsen may contact Elizabeth Krenske.
*Host name: Elizabeth Krenske
Host phone number:
*Host email: e.krenske@uq.edu.au