PROTACs: a novel strategy for cancer therapy
J Liu, J Ma, Y Liu, J Xia, Y Li, ZP Wang… - Seminars in Cancer …, 2020 - Elsevier
Chemotherapeutic strategy has been widely used for treating malignance by targeting
irregular expressed or mutant proteins with small molecular inhibitors (SMIs) or monoclonal …
irregular expressed or mutant proteins with small molecular inhibitors (SMIs) or monoclonal …
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 …
Catalytic in vivo protein knockdown by small-molecule PROTACs
DP Bondeson, A Mares, IED Smith, E Ko… - Nature chemical …, 2015 - nature.com
The current predominant therapeutic paradigm is based on maximizing drug-receptor
occupancy to achieve clinical benefit. This strategy, however, generally requires excessive …
occupancy to achieve clinical benefit. This strategy, however, generally requires excessive …
From conception to development: investigating PROTACs features for improved cell permeability and successful protein degradation
C Cecchini, S Pannilunghi, S Tardy… - Frontiers in …, 2021 - frontiersin.org
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional degraders that
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
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 …
Recent advances of degradation technologies based on PROTAC mechanism
M Xiao, J Zhao, Q Wang, J Liu, L Ma - Biomolecules, 2022 - mdpi.com
PROTAC (proteolysis-targeting chimeras), which selectively degrades target proteins, has
become the most popular technology for drug development in recent years. Here, we …
become the most popular technology for drug development in recent years. Here, we …
Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five'chemical space: Recent progress and future challenges
SD Edmondson, B Yang, C Fallan - Bioorganic & Medicinal Chemistry …, 2019 - Elsevier
Proteolysis targeting chimeras (PROTACs) are heterobifunctional compounds with
molecular weights and other properties that lie outside the classic 'rule-of-five'space …
molecular weights and other properties that lie outside the classic 'rule-of-five'space …
Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs
SB Alabi, CM Crews - Journal of Biological Chemistry, 2021 - ASBMB
Of late, targeted protein degradation (TPD) has surfaced as a novel and innovative chemical
tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates …
tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates …
PROTACs–a game-changing technology
M Konstantinidou, J Li, B Zhang, Z Wang… - Expert opinion on …, 2019 - Taylor & Francis
ABSTRACT Introduction: Proteolysis–targeting chimeras (PROTACs) have emerged as a
new modality with the potential to revolutionize drug discovery. PROTACs are …
new modality with the potential to revolutionize drug discovery. PROTACs are …
The PROTACtable genome
M Schneider, CJ Radoux, A Hercules… - Nature reviews Drug …, 2021 - nature.com
Proteolysis-targeting chimeras (PROTACs) are an emerging drug modality that may offer
new opportunities to circumvent some of the limitations associated with traditional small …
new opportunities to circumvent some of the limitations associated with traditional small …