Identification of small‐molecule binding sites of a ubiquitin‐conjugating enzyme‐UBE2T through fragment‐based screening
Yong Yao Loh,
Jothi Anantharajan,
Qiwei Huang
et al.
Abstract:UBE2T is an attractive target for drug development due to its linkage with several types of cancers. However, the druggability of ubiquitin‐conjugating E2 (UBE2T) is low because of the lack of a deep and hydrophobic pocket capable of forming strong binding interactions with drug‐like small molecules. Here, we performed fragment screening using 19F‐nuclear magnetic resonance (NMR) and validated the hits with 1H‐15N‐heteronuclear single quantum coherence (HSQC) experiment and X‐ray crystallographic studies. The … Show more
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