Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)

0502055 - ÚEB 2019 RIV GB eng J - Journal Article
Krajčovičová, S. - Jorda, Radek - Hendrychová, Denisa - Kryštof, Vladimír - Soural, M.
Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC).
Chemical Communications. Roč. 55, č. 7 (2019), s. 929-932. ISSN 1359-7345. E-ISSN 1364-548X
R&D Projects: GA MŠMT(CZ) LO1304
Institutional support: RVO:61389030
Keywords : INDUCED PROTEIN-DEGRADATION * DESIGN * kinase inhibitor
OECD category: Biochemistry and molecular biology
Impact factor: 5.996, year: 2019

A preloaded resin consisting of a thalidomide moiety and an ethylene-oxy linker allows the simple and fast formation of PROTACs. The feasibility of the procedure was illustrated by conjugating different protein kinase inhibitors. The biological functionality of an ibrutinib-like conjugate was then confirmed by a cellular experiment.
Permanent Link: http://hdl.handle.net/11104/0294002