[PDF][PDF] Target protein localization and its impact on PROTAC-mediated degradation

LM Simpson, L Glennie, A Brewer, JF Zhao… - Cell Chemical …, 2022 - cell.com
Proteolysis-targeting chimeras (PROTACs) bring a protein of interest (POI) into spatial
proximity of an E3 ubiquitin ligase, promoting POI ubiquitylation and proteasomal …

Targeted protein degradation: elements of PROTAC design

SL Paiva, CM Crews - Current opinion in chemical biology, 2019 - Elsevier
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …

Native mass spectrometry can effectively predict PROTAC efficacy

R Beveridge, D Kessler, K Rumpel… - ACS Central …, 2020 - ACS Publications
Protein degraders, also known as proteolysis targeting chimeras (PROTACs), are
bifunctional small molecules that promote cellular degradation of a protein of interest (POI) …

Recent developments in PROTAC‐mediated protein degradation: from bench to clinic

Z Hu, CM Crews - ChemBioChem, 2022 - Wiley Online Library
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …

PROTACs: past, present and future

K Li, CM Crews - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …

[HTML][HTML] Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

BE Smith, SL Wang, S Jaime-Figueroa, A Harbin… - Nature …, 2019 - nature.com
Abstract PROteolysis-TArgeting Chimeras (PROTACs) are hetero-bifunctional molecules
that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted …

The present and future of novel protein degradation technology

L Xia, W Liu, Y Song, H Zhu… - Current Topics in …, 2019 - ingentaconnect.com
Proteolysis targeting chimeras (PROTACs), as a novel therapeutic modality, play a vital role
in drug discovery. Each PROTAC contains three key parts; a protein-of-interest (POI) ligand …

Frontiers in PROTACs

GR Hughes, AP Dudey, AM Hemmings, A Chantry - Drug Discovery Today, 2021 - Elsevier
Targeting protein–protein interactions (PPI) is a key focus in the development of new and
emerging small-molecule therapeutics. Shallow interacting surfaces can render PPI …

[PDF][PDF] PROTACs: an emerging therapeutic modality in precision medicine

DA Nalawansha, CM Crews - Cell chemical biology, 2020 - cell.com
Targeted protein degradation (TPD) has emerged as an exciting new era in chemical
biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets …

Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization

MP Schwalm, A Krämer, A Dölle, J Weckesser, X Yu… - Cell chemical …, 2023 - cell.com
The multi-step degradation process of PROteolysis TArgeting Chimeras (PROTACs) poses a
challenge for their rational development, as the rate-limiting steps that determine PROTACs …