Targeting ferroptosis opens new avenues for the development of novel therapeutics

S Sun, J Shen, J Jiang, F Wang, J Min - Signal transduction and …, 2023 - nature.com
Ferroptosis is an iron-dependent form of regulated cell death with distinct characteristics,
including altered iron homeostasis, reduced defense against oxidative stress, and abnormal …

Targeted protein degradation: from mechanisms to clinic

JM Tsai, RP Nowak, BL Ebert, ES Fischer - Nature Reviews Molecular …, 2024 - nature.com
Targeted protein degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …

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 …

PROTAC targeted protein degraders: the past is prologue

M Békés, DR Langley, CM Crews - Nature reviews Drug discovery, 2022 - nature.com
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …

Chemistries of bifunctional PROTAC degraders

C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …

Protein posttranslational modifications in health and diseases: Functions, regulatory mechanisms, and therapeutic implications

Q Zhong, X **ao, Y Qiu, Z Xu, C Chen, B Chong… - MedComm, 2023 - Wiley Online Library
Protein posttranslational modifications (PTMs) refer to the breaking or generation of covalent
bonds on the backbones or amino acid side chains of proteins and expand the diversity of …

Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - Nature Reviews …, 2021 - nature.com
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …

An overview of PROTACs: a promising drug discovery paradigm

Z Liu, M Hu, Y Yang, C Du, H Zhou, C Liu, Y Chen… - Molecular …, 2022 - Springer
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …

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 …

A proteome-wide atlas of drug mechanism of action

DC Mitchell, M Kuljanin, J Li, JG Van Vranken… - Nature …, 2023 - nature.com
Defining the cellular response to pharmacological agents is critical for understanding the
mechanism of action of small molecule perturbagens. Here, we developed a 96-well-plate …