Evaluation of a Covalent Library of Diverse Warheads (CovLib) Binding to JNK3, USP7, or p53.

Theresa Klett Martin Schwer Larissa N Ernst Marc U Engelhardt Simon J Jaag Benedikt MasbergCornelius KnappeMichael Lämmerhofer Alexander Titz Frank M Boeckler

Published in: Drug design, development and therapy (2024)

The screening and target evaluation of the CovLib revealed first interesting hits. The highly cysteine-reactive fragments VS004, SN001, SN006, and SN007 covalently modify several target proteins and showed distinct shifts in the melting temperatures up to +5.1 °C and -9.1 °C.

Keyphrases

high resolution
signaling pathway
cell death
induced apoptosis
mass spectrometry