A customer perspective on hit validation in fragment based drug discovery

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00:00:00 Welcome
00:02:09 Untitled
00:02:55 Sprint Bioscience
00:03:49 Drug Discovery Platform
00:06:19 Fragment screening
00:07:45 Thermal Shift Assays (TSA)
00:09:44 TSA as Primary Fragment Screening Method
00:12:55 Fragment Screening by TSA
00:13:49 Fragment Library Properties
00:16:02 Fragment screening cascade
00:17:23 Untitled
00:19:21 Thermodynamic profiling
00:21:22 Mode of action?
00:22:41 Vps34 Screening Summary
00:25:19 Fragment expansion
00:27:36 Conclusions
00:28:41 Questions?

Guest Presenter: Dr. Martin Andersson, Director Protein Science, Sprint Bioscience, Stockholm, Sweden

Sprint Bioscience have established a fragment-based drug discovery (FBDD) platform with disciplines ranging from protein production, fragment screening, biophysics and x-ray crystallography to computational and medicinal chemistry. In order to drive projects in an efficient manner they identified the need for a set of screening technologies that were generic, could be rapidly established for new targets and efficiently could identify fragment hits from their fragment library. Furthermore, technologies for follow-up after primary screening are important to allow for elimination of false positives and fragments with undesirable modes of action. 

In this webinar, learn how:

  • Orthogonal use of biophysical techniques and combination of target-based and phenotypic approaches enables selection of most promising fragment series and leads.
  • Isothermal Titration Calorimetry (ITC) can be used as a secondary screening tool in hit validation for proteins demonstrating limited stability in other orthogonal assays
  • ITC is a good predictor of successful determination of protein-ligand co-crystal structures