PROTAC targeted protein degraders: the past is prologue
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 …
tackle disease-causing proteins that have historically been highly challenging to target with …
PROTACs: past, present and future
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 …
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …
Advancing targeted protein degradation for cancer therapy
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 …
than 600 of them are functionally important for various types of cancers, including nearly 400 …
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 …
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 …
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
Induced protein degradation: an emerging drug discovery paradigm
Small-molecule drug discovery has traditionally focused on occupancy of a binding site that
directly affects protein function, and this approach typically precludes targeting proteins that …
directly affects protein function, and this approach typically precludes targeting proteins that …
Phthalimide conjugation as a strategy for in vivo target protein degradation
The development of effective pharmacological inhibitors of multidomain scaffold proteins,
notably transcription factors, is a particularly challenging problem. In part, this is because …
notably transcription factors, is a particularly challenging problem. In part, this is because …
Molecular glues for targeted protein degradation: from serendipity to rational discovery
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
Structural basis of PROTAC cooperative recognition for selective protein degradation
Inducing macromolecular interactions with small molecules to activate cellular signaling is a
challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that …
challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that …
Proteolysis-targeting chimeras as therapeutics and tools for biological discovery
New biological tools provide new techniques to probe fundamental biological processes.
Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which …
Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which …