Pankaj Garg

TL;DR: This work used massively diverse combinatorial libraries of ubiquitin variants to develop inhibitors of four deubiquitinases (DUBs) and analyzed the DUB-inhibitor complexes with crystallography to report a method to target the myriad enzymes that govern ubiquitination of protein substrates.

TL;DR: Stabilization of the numerous other weak interactions between ubiquitin and UPS enzymes by small molecules may be a feasible strategy to selectively inhibit different UPS activities.

TL;DR: The study demonstrates the power of ProP‐PD as a complementary approach to uncover interactions of potential biological relevance and profiles syntenin PDZ1‐2 through proteomic peptide phage display (ProP‐ PD) using a library that displays C‐terminal regions of the human proteome.

TL;DR: The results show that alternative core packing and consequent allosteric modulation of binding interfaces could be used to engineer proteins with novel functions.

TL;DR: The findings validate the E2 backside as a target for inhibition and provide structural insights to aid inhibitor design and screening efforts.