Datum der Aufzeichnung: 04 December 2014

Duration: 52 minutes 08 seconds

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
Table of contents
1. Welcome
02:09
2. Untitled
00:46
3. Sprint Bioscience
00:54
4. Drug Discovery Platform
02:30
5. Fragment screening
01:26
6. Thermal Shift Assays (TSA)
01:59
7. TSA as Primary Fragment Screening Method
03:11
8. Fragment Screening by TSA
00:54
9. Fragment Library Properties
02:13
10. Fragment screening cascade
01:21
11. Untitled
01:58
12. Thermodynamic profiling
02:01
13. Mode of action?
01:19
14. Vps34 Screening Summary
02:38
15. Fragment expansion
02:17
16. Conclusions
01:05
17. Questions?
23:27