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 …
including altered iron homeostasis, reduced defense against oxidative stress, and abnormal …
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 …
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 …
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 …
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
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 …
Direct-to-biology, automated, nano-scale synthesis, and phenotypic screening-enabled E3 ligase modulator discovery
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 …
and degradation of key cancer proteins via the cereblon (CRBN) E3 ligase. Here, we …
Targeted protein degradation: from mechanisms to clinic
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 …
degradation of proteins. In its most common form, this degradation is achieved through …
Protein degradation: expanding the toolbox to restrain cancer drug resistance
Despite significant progress in clinical management, drug resistance remains a major
obstacle. Recent research based on protein degradation to restrain drug resistance has …
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 …
because of their potency, versatility and their potential to expand the druggable target space …