Targeted protein degradation: A promise for undruggable proteins

KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Targeted Protein Degradation (TPD) strategies have also been explored to target previously
undruggable proteins… of the proteins targeted by PROTACs and the biological effects of their …

Targeted protein degradation: mechanisms, strategies and application

L Zhao, J Zhao, K Zhong, A Tong, D Jia - … transduction and targeted …, 2022 - nature.com
expanding the range of substrates. In this review, we first provide a simple introduction of
protein degradation … , will not only provide powerful tools for biomedical research, but hold great …

Expanding the arsenal of E3 ubiquitin ligases for proximity-induced protein degradation

A Kannt, I Đikić - Cell chemical biology, 2021 - cell.com
… be hijacked for targeted protein degradation—is still … protein degradation and approaches
used to identify or design E3 ligands, and highlight challenges and opportunities for targeting

Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs

SB Alabi, CM Crews - Journal of Biological Chemistry, 2021 - ASBMB
Of late, targeted protein degradation (TPD) has surfaced as a novel and innovative chemical
tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates …

Prey for the proteasome: targeted protein degradation—a medicinal chemist's perspective

LM Luh, U Scheib, K Juenemann… - Angewandte Chemie …, 2020 - Wiley Online Library
… biology tools as well as therapeutic approaches inducing targeted protein degradation and
… and proteolysis targeting chimeras (PROTACs) paving the way to expand the druggable …

Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - Nature Reviews …, 2021 - nature.com
… of the target protein. The broad … that target oncoproteins with tissue, tumour and subcellular
selectivity. In this Review, we first discuss the molecular basis of targeted protein degradation

Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation

MJ Bond, CM Crews - RSC chemical biology, 2021 - pubs.rsc.org
… To expand the reach of TPD to degrade other “hard to drug” … synthesis, and molecular
biology, tools now exist to identify ligands for almost any protein. This is underscored by the recent …

Discovery of a covalent FEM1B recruiter for targeted protein degradation applications

NJ Henning, AG Manford, JN Spradlin… - Journal of the …, 2022 - ACS Publications
… the degradation of BRD4 and BCR-ABL, respectively. Our study showcases a covalent ligand
that targets … in expanding the arsenal of E3 ligase recruiters suitable for TPD applications. …

Improved Accuracy for Modeling PROTAC-Mediated Ternary Complex Formation and Targeted Protein Degradation via New In Silico Methodologies

ML Drummond, A Henry, H Li… - Journal of Chemical …, 2020 - ACS Publications
… In this current work, we extend upon our initial publication (41… Using these two new methods,
we then extend the test set … Figure 4 do suggest that the modeling tools of this work can …

PROTAC: an effective targeted protein degradation strategy for cancer therapy

SM Qi, J Dong, ZY Xu, XD Cheng, WD Zhang… - Frontiers in …, 2021 - frontiersin.org
… future to achieve the desired degradation results. In this paper, … degradation strategies for
different target proteins (Table 1). … PROTACs can extend the "target space" to the PPI target. It …