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 …

COVID-19 and cellular senescence

CA Schmitt, T Tchkonia, LJ Niedernhofer… - Nature Reviews …, 2023 - nature.com
The clinical severity of coronavirus disease 2019 (COVID-19) is largely determined by host
factors. Recent advances point to cellular senescence, an ageing-related switch in cellular …

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 …

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - … and Targeted Therapy, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

[PDF][PDF] 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 …

[HTML][HTML] PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective

X Han, W Wei, Y Sun - Acta materia medica, 2022 - ncbi.nlm.nih.gov
Abstract Mouse double minute 2 (MDM2) is an E3 ubiquitin ligase which effectively
degrades tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt …

The rise of degrader drugs

M Teng, NS Gray - Cell Chemical Biology, 2023 - cell.com
The cancer genomics revolution has served up a plethora of promising and challenging
targets for the drug discovery community. The field of targeted protein degradation (TPD) …

Strategies to Reduce the On‐Target Platelet Toxicity of Bcl‐xL Inhibitors: PROTACs, SNIPERs and Prodrug‐Based Approaches

A Negi, AS Voisin‐Chiret - ChemBioChem, 2022 - Wiley Online Library
Apoptosis is a highly regulated cellular process. Aberration in apoptosis is a common
characteristic of various disorders. Therefore, proteins involved in apoptosis are prime …

Novel approaches to targeted protein degradation technologies in drug discovery

Y Xue, AA Bolinger, J Zhou - Expert Opinion on Drug Discovery, 2023 - Taylor & Francis
Introduction Target protein degradation (TPD) provides a novel therapeutic modality, other
than inhibition, through the direct depletion of target proteins. Two primary human protein …

[PDF][PDF] Targeted protein degradation in cancers: Orthodox PROTACs and beyond

J Li, X Chen, A Lu, C Liang - The Innovation, 2023 - cell.com
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis targeting chimera (PROTAC) technology …