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 …
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders
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 …
proteasome system that recruits substrates such as the hypoxia inducible factor for …
Proximity-based modalities for biology and medicine
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
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 …
disease. LRRK2-targeting strategies have primarily focused on type 1 kinase inhibitors …
PROTAC degraders as chemical probes for studying target biology and target validation
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …
emerged as new promising pharmacological modalities and the first PROTAC drug …
New insights into genome folding by loop extrusion from inducible degron technologies
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 …
wire distant loci together for gene regulation. These loops are continuously created …
[PDF][PDF] Strategies for the discovery of oral PROTAC degraders aimed at cancer therapy
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 …
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
[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 …
Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways …
Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines
Z Yan, X Lyu, D Lin, G Wu, Y Gong, X Ren… - European Journal of …, 2023 - Elsevier
Targeted degradation of BET family proteins BRD2/3/4 or only BRD4 with PROTAC
molecules has been a promising strategy for the treatment of human cancer. Meanwhile …
molecules has been a promising strategy for the treatment of human cancer. Meanwhile …
Development of NanoLuc-targeting protein degraders and a universal reporter system to benchmark tag-targeted degradation platforms
C Grohmann, CM Magtoto, JR Walker, NK Chua… - Nature …, 2022 - nature.com
Modulation of protein abundance using t ag-T argeted P rotein D egrader (tTPD) systems
targeting FKBP12F36V (dTAGs) or HaloTag7 (HaloPROTACs) are powerful approaches for …
targeting FKBP12F36V (dTAGs) or HaloTag7 (HaloPROTACs) are powerful approaches for …