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 …

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 …

Design principles for cyclin K molecular glue degraders

Z Kozicka, DJ Suchyta, V Focht, G Kempf… - Nature Chemical …, 2024 - nature.com
Molecular glue degraders are an effective therapeutic modality, but their design principles
are not well understood. Recently, several unexpectedly diverse compounds were reported …

Molecular glue discovery: current and future approaches

JA Dewey, C Delalande, SA Azizi, V Lu… - Journal of Medicinal …, 2023 - ACS Publications
The intracellular interactions of biomolecules can be maneuvered to redirect signaling,
reprogram the cell cycle, or decrease infectivity using only a few dozen atoms. Such …

[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 …

Direct-to-biology, automated, nano-scale synthesis, and phenotypic screening-enabled E3 ligase modulator discovery

Z Wang, S Shaabani, X Gao, YLD Ng… - Nature …, 2023 - nature.com
Thalidomide and its analogs are molecular glues (MGs) that lead to targeted ubiquitination
and degradation of key cancer proteins via the cereblon (CRBN) E3 ligase. Here, we …

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) …

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 …

Protein degradation: expanding the toolbox to restrain cancer drug resistance

H Ming, B Li, J Jiang, S Qin, EC Nice, W He… - Journal of hematology & …, 2023 - Springer
Despite significant progress in clinical management, drug resistance remains a major
obstacle. Recent research based on protein degradation to restrain drug resistance has …

Proteome-scale discovery of protein degradation and stabilization effectors

J Poirson, H Cho, A Dhillon, S Haider, AZ Imrit… - Nature, 2024 - nature.com
Targeted protein degradation and stabilization are promising therapeutic modalities
because of their potency, versatility and their potential to expand the druggable target space …