Development of new classes of bio-relevant linkers for PROTACs and other conjugates using new technologies

PROTACs are bifunctional molecules that allow the elimination of target proteins in the cells. Despite the advantages of this early field, the area of small molecules PROTACs presents some drawbacks, in particular, the long and tedious syntheses of the central linker. Secondly, the variety of those linkers is quite scarce, as poly-ether or alkyl chains are almost exclusively used. Thirdly, their length variation and effects on the activity of the PROTACs are rarely studied.
The goals of this project are to develop new synthetic routes allowing the easier synthesis of various linkers, develop new categories of linkers, and combine those advances to allow the rapid synthesis of a wide range of linkers that will constitute a toolbox for next generation bioconjugates, including but not limited to PROTACs . These goals will be achieved by the use of new technologies and chemical strategies. TO BE CONT’D

Faculty Supervisor:

André Bernard Charette

Student:

Partner:

NuChem Therapeutics

Discipline:

Life Sciences

Sector:

Professional, scientific and technical services

University:

Université de Montréal

Program: