[HTML][HTML] Expanding the horizons of targeted protein degradation: A non-small molecule perspective
X Huang, F Wu, J Ye, L Wang, X Wang, X Li… - … Pharmaceutica Sinica B, 2024 - Elsevier
Targeted protein degradation (TPD) represented by proteolysis targeting chimeras
(PROTACs) marks a significant stride in drug discovery. A plethora of innovative …
(PROTACs) marks a significant stride in drug discovery. A plethora of innovative …
Emerging Strategies in Proteolysis-Targeting Chimeras (PROTACs): Highlights from 2022
R Tamatam, D Shin - International Journal of Molecular Sciences, 2023 - mdpi.com
Targeted protein degradation (TPD) is a promising therapeutic modality that has garnered
attention in academic, industrial, and pharmaceutical research for treating diseases such as …
attention in academic, industrial, and pharmaceutical research for treating diseases such as …
PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs
The vast majority of currently marketed drugs rely on small molecules with an 'occupancy-
driven'mechanism of action (MOA). Therefore, the efficacy of these therapeutics depends on …
driven'mechanism of action (MOA). Therefore, the efficacy of these therapeutics depends on …
[HTML][HTML] The rise and rise of protein degradation: opportunities and challenges ahead
The transformational mechanism of action underpinning targeted protein degradation
strategies, including proteolysis-targeting chimeras (PROTACs), gives potential for potent in …
strategies, including proteolysis-targeting chimeras (PROTACs), gives potential for potent in …
Targeted protein degradation: elements of PROTAC design
SL Paiva, CM Crews - Current opinion in chemical biology, 2019 - Elsevier
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …
Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …
targeted protein degradation (TPD) has changed the landscape of drug development …
Novel design strategies to enhance the efficiency of proteolysis targeting chimeras
C Zhao, FJ Dekker - ACS Pharmacology & Translational Science, 2022 - ACS Publications
Despite the success of drug discovery over the past decades, many potential drug targets
still remain intractable for small molecule modulation. The development of proteolysis …
still remain intractable for small molecule modulation. The development of proteolysis …
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 …
Integrated Direct-to-Biology Platform for the Nanoscale Synthesis and Biological Evaluation of PROTACs
R Stevens, E Bendito-Moll, DJ Battersby… - Journal of Medicinal …, 2023 - ACS Publications
Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules that co-opt the
cell's natural proteasomal degradation mechanisms to degrade undesired proteins. A …
cell's natural proteasomal degradation mechanisms to degrade undesired proteins. A …
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 …