PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

Proximity-based modalities for biology and medicine

X Liu, A Ciulli - ACS Central Science, 2023 - ACS Publications
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …

Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders

CJ Diehl, A Ciulli - Chemical Society Reviews, 2022 - pubs.rsc.org
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …

Discovery of XL01126: a potent, fast, cooperative, selective, orally bioavailable, and blood–brain barrier penetrant PROTAC degrader of leucine-rich repeat kinase 2

X Liu, AF Kalogeropulou, S Domingos… - Journal of the …, 2022 - ACS Publications
Leucine-rich repeat kinase 2 (LRRK2) is one of the most promising targets for Parkinson's
disease. LRRK2-targeting strategies have primarily focused on type 1 kinase inhibitors …

New insights into genome folding by loop extrusion from inducible degron technologies

E de Wit, EP Nora - Nature Reviews Genetics, 2023 - nature.com
Chromatin folds into dynamic loops that often span hundreds of kilobases and physically
wire distant loci together for gene regulation. These loops are continuously created …

PROTAC degraders as chemical probes for studying target biology and target validation

V Němec, MP Schwalm, S Müller… - Chemical Society Reviews, 2022 - pubs.rsc.org
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …

Strategies for the discovery of oral PROTAC degraders aimed at cancer therapy

X Han, Y Sun - Cell Reports Physical Science, 2022 - cell.com
In the past two decades, we have witnessed the discovery and development of many potent
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …

CURTAIN—A unique web-based tool for exploration and sharing of MS-based proteomics data

TK Phung, K Berndsen, R Shastry… - Proceedings of the …, 2024 - National Acad Sciences
To facilitate analysis and sharing of mass spectrometry (MS)-based proteomics data, we
created online tools called CURTAIN (https://curtain. proteo. info) and CURTAIN-PTM …

Targeted protein degradation via intramolecular bivalent glues

O Hsia, M Hinterndorfer, AD Cowan, K Iso, T Ishida… - Nature, 2024 - nature.com
Targeted protein degradation is a pharmacological modality that is based on the induced
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …

[HTML][HTML] Proteomic approaches advancing targeted protein degradation

G Sathe, GP Sapkota - Trends in pharmacological sciences, 2023 - cell.com
Targeted protein degradation (TPD) is an emerging modality for research and therapeutics.
Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways …