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 …
Control of protein stability by post-translational modifications
Post-translational modifications (PTMs) can occur on specific amino acids localized within
regulatory domains of target proteins, which control a protein's stability. These regions …
regulatory domains of target proteins, which control a protein's stability. These regions …
Protein degraders enter the clinic—a new approach to cancer therapy
D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …
Targeting RNA structures with small molecules
JL Childs-Disney, X Yang, QMR Gibaut… - Nature Reviews Drug …, 2022 - nature.com
RNA adopts 3D structures that confer varied functional roles in human biology and
dysfunction in disease. Approaches to therapeutically target RNA structures with small …
dysfunction in disease. Approaches to therapeutically target RNA structures with small …
Lysosome-targeting chimaeras for degradation of extracellular proteins
The majority of therapies that target individual proteins rely on specific activity-modulating
interactions with the target protein—for example, enzyme inhibition or ligand blocking …
interactions with the target protein—for example, enzyme inhibition or ligand blocking …
Targeted protein degradation: mechanisms, strategies and application
L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …
development and application of protein activity modulators, particularly inhibitors, has been …
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 …
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 …
Targeted protein degradation: expanding the toolbox
M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …