HT23
Background
PROTACs, or degraders, are a new and very promising type of drug that binds to and degrades specific intracellular signaling proteins by activating the body's own selective degradation system 1. The technology allows new target proteins to be reached with high specificity while avoiding the development of resistance in cancer treatment. In the pharmaceutical industry, there is currently a strong interest in developing this therapeutic strategy for a number of indications. However, the molecular properties of PROTACs and in vitro cell permeability data often suggest that they will have low oral absorption and bioavailability, which is not always reflected in vivo, with reports showing that absorption and disposition are more extensive 2. In order to enable effective research and development of this group of substances, it is therefore of utmost importance to understand the relationship between absorption and disposition in vitro versus in vivo.
Aim
The aim is to characterize and describe intestinal absorption and disposition of PROTACs.
Methods
The experimental work that will be carried may include the following
(i) Stability, degradation, solubility and binding of PROTACs
(ii) In vitro permeability and metabolisms of PROTACs
The definitive study plan will be decided together with the student.
Expect 8 h work days at BMC.
Farmaceutisk vetenskap
Biofarmaci
Laborativ studie
Uppsala University
Uppsala
David Dahlgren
david.dahlgren@farmbio.uu.se
Institutionen för farmaceutisk biovetenskap
Apotekarprogrammet
Fördjupningsprojekt i biofarmaci 30 hp - 3FG008
30hp
1