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