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Design and modular parallel synthesis of a MCR derived alpha-helix mimetic protein-protein interaction inhibitor scaffold
Authors:Antuch Walfrido  Menon Sanjay  Chen Quin-Zene  Lu Yingchun  Sakamuri Sukumar  Beck Barbara  Schauer-Vukasinović Vesna  Agarwal Seema  Hess Sibylle  Dömling Alexander
Affiliation:ABC Pharma, Franckensteinstrasse 9a, 81243 München, Germany.
Abstract:
A terphenyl alpha-helix mimetic scaffold recognized to be capable of disrupting protein-protein interactions was structurally morphed into an easily amenable and versatile multicomponent reaction (MCR) backbone. The design, modular in-parallel library synthesis, initial cell based biological data, and preliminary in vitro screening for the disruption of the Bcl-w/Bak protein-protein interaction by representatives of the MCR derived scaffold are presented.
Keywords:
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