Boc3Arg-Linked Ligands Induce Degradation by Localizing Target Proteins to the 20S Proteasome
Targeted protein degradation is a promising strategy for drug design and functional
assessment. Several small molecule approaches have been developed that localize target …
assessment. Several small molecule approaches have been developed that localize target …
Chemical approaches to targeted protein degradation through modulation of the ubiquitin–proteasome pathway
I Collins, H Wang, JJ Caldwell, R Chopra - Biochemical Journal, 2017 - portlandpress.com
Manipulation of the ubiquitin–proteasome system to achieve targeted degradation of
proteins within cells using chemical tools and drugs has the potential to transform …
proteins within cells using chemical tools and drugs has the potential to transform …
Chemical specification of E3 ubiquitin ligase engagement by cysteine-reactive chemistry
Targeted protein degradation relies on small molecules that induce new protein–protein
interactions between targets and the cellular protein degradation machinery. Most of these …
interactions between targets and the cellular protein degradation machinery. Most of these …
Development of a small hybrid molecule that mediates degradation of His-Tag fused proteins
K Okitsu, T Hattori, T Misawa, T Shoda… - Journal of Medicinal …, 2018 - ACS Publications
In recent years, the induction of target–protein degradation via the ubiquitin–proteasome
system (UPS) mediated by small molecules has attracted attention, and this approach has …
system (UPS) mediated by small molecules has attracted attention, and this approach has …
[HTML][HTML] A critical evaluation of the approaches to targeted protein degradation for drug discovery
There is a great deal of excitement around the concept of targeting proteins for degradation
as an alternative to conventional inhibitory small molecules and antibodies. Protein …
as an alternative to conventional inhibitory small molecules and antibodies. Protein …
Targeted protein degradation: current and future challenges
Traditional approaches in the development of small-molecule drugs typically aim to inhibit
the biochemical activity of functional protein domains. In contrast, targeted protein …
the biochemical activity of functional protein domains. In contrast, targeted protein …
Targeted protein degradation and the enzymology of degraders
SL Fisher, AJ Phillips - Current opinion in chemical biology, 2018 - Elsevier
Targeted protein degradation is an emerging strategy for drug discovery that employs small
molecules to catalyze the ubiquitination of target proteins, ultimately causing their …
molecules to catalyze the ubiquitination of target proteins, ultimately causing their …
[HTML][HTML] Targeted degradation via direct 26S proteasome recruitment
C Bashore, S Prakash, MC Johnson… - Nature Chemical …, 2023 - nature.com
Engineered destruction of target proteins by recruitment to the cell's degradation machinery
has emerged as a promising strategy in drug discovery. The majority of molecules that …
has emerged as a promising strategy in drug discovery. The majority of molecules that …
[HTML][HTML] Bivalent ligands for protein degradation in drug discovery
M Scheepstra, KFW Hekking, L van Hijfte… - Computational and …, 2019 - Elsevier
Targeting the “undruggable” proteome remains one of the big challenges in drug discovery.
Recent innovations in the field of targeted protein degradation and manipulation of the …
Recent innovations in the field of targeted protein degradation and manipulation of the …
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 …