Jul 5, 2021 · This review provides an in-depth analysis of synthetic entries to functionalized ligands for the most relevant E3 ligase ligands, i.e. CRBN, VHL, IAP, and MDM2. Less …

The advent of nonpeptidic small-molecule E3 ligase ligands, notably for von Hippel-Lindau (VHL) and cereblon (CRBN), revolutionized the field and ushered in the design of drug-like …

Here, we briefly review how traditional E3 ligase ligands were discovered, and then outline approaches and ligands that have been recently used to discover new E3 ligases for PROTACs.

Jan 1, 2022 · In the search for alternative E3 ligases for TPD, two primary strategies have been pursued: “ligand first” and “ligase first.” In the first strategy, an E3 ligase is recruited via its …

Using the well-established E3 ligand VH032 and its derivative VH032-OH, we synthesized a set of structurally diverse PROTACs by combining distinct structural features in a modular fashion.

Oct 16, 2023 · One fundamental element in the degradation process is the E3 ligase. However, less than 2% amongst hundreds of E3 ligases in the human genome have been engaged in …

Aug 5, 2023 · To eliminate differences between in vitro binding assays and cell-based assays and rapidly obtain a cellular response E3 ligand, a practical cell-based target engagement assay …

E3 ubiquitin ligases regulate the last step of the enzymatic cascade, which also consists of ubiquitin activating enzymes (E1s) and ubiquitin conjugating enzymes (E2s). E3 ligases can …

most compelling and suited strategies to find new E3 ligase ligands for PROTACs, including applications of structure-based ligand design, DNA-encoded libraries (DELs), dis-play …

2 days ago · Enhancing the arsenal of E3 ligases is important for PROTACs development. Here, the authors identify a non-inhibitory aptameric ligand to CRL2ZYG11B E3 ligase, and develop …