Molecular glues: the adhesive connecting targeted protein degradation to the clinic
Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …
Progress and challenges in targeted protein degradation for neurodegenerative disease therapy
Y Fang, J Wang, M Zhao, Q Zheng, C Ren… - Journal of Medicinal …, 2022 - ACS Publications
Neurodegenerative diseases (NDs) are currently incurable diseases that cause progressive
degeneration of nerve cells. Many of the disease-causing proteins of NDs are “undruggable” …
degeneration of nerve cells. Many of the disease-causing proteins of NDs are “undruggable” …
Focal adhesion kinase: from biological functions to therapeutic strategies
X Tan, Y Yan, B Song, S Zhu, Q Mei, K Wu - Experimental Hematology & …, 2023 - Springer
Focal adhesion kinase (FAK), a nonreceptor cytoplasmic tyrosine kinase, is a vital
participant in primary cellular functions, such as proliferation, survival, migration, and …
participant in primary cellular functions, such as proliferation, survival, migration, and …
Journey of Von Hippel-Lindau (VHL) E3 ligase in PROTACs design: From VHL ligands to VHL-based degraders
The scientific community has shown considerable interest in proteolysis-targeting chimeras
(PROTACs) in the last decade, indicating their remarkable potential as a means of achieving …
(PROTACs) in the last decade, indicating their remarkable potential as a means of achieving …
DNA framework-engineered chimeras platform enables selectively targeted protein degradation
L Zhou, B Yu, M Gao, R Chen, Z Li, Y Gu, J Bian… - Nature …, 2023 - nature.com
A challenge in develo** proteolysis targeting chimeras (PROTACs) is the establishment of
a universal platform applicable in multiple scenarios for precise degradation of proteins of …
a universal platform applicable in multiple scenarios for precise degradation of proteins of …
Heat Shock Protein 90 Interactome-Mediated Proteolysis Targeting Chimera (HIM-PROTAC) Degrading Glutathione Peroxidase 4 to Trigger Ferroptosis
J Dong, F Ma, M Cai, F Cao, H Li, H Liang… - Journal of Medicinal …, 2024 - ACS Publications
Targeted protein degradation (TPD) is an emerging therapeutic paradigm aimed at
eliminating the disease-causing protein with aberrant expression. Herein, we report a new …
eliminating the disease-causing protein with aberrant expression. Herein, we report a new …
Bromodomain and extraterminal (BET) proteins: biological functions, diseases, and targeted therapy
ZQ Wang, ZC Zhang, YY Wu, YN Pi, SH Lou… - Signal transduction and …, 2023 - nature.com
BET proteins, which influence gene expression and contribute to the development of cancer,
are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic …
are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic …
Hydrophobic tag-based protein degradation: Development, opportunity and challenge
Q He, X Zhao, D Wu, S Jia, C Liu, Z Cheng… - European Journal of …, 2023 - Elsevier
Targeted protein degradation (TPD) has emerged as a promising approach for drug
development, particularly for undruggable targets. TPD technology has also been …
development, particularly for undruggable targets. TPD technology has also been …
[HTML][HTML] The current status and future prospects for therapeutic targeting of KEAP1-NRF2 and β-TrCP-NRF2 interactions in cancer chemoresistance
Drug resistance is one of the biggest challenges in cancer treatment and limits the potential
to cure patients. In many tumors, sustained activation of the protein NRF2 makes tumor cells …
to cure patients. In many tumors, sustained activation of the protein NRF2 makes tumor cells …
An updated patent review of BRD4 degraders
Introduction Bromodomain-containing protein 4 (BRD4), an important epigenetic reader, is
closely associated with the pathogenesis and development of many diseases, including …
closely associated with the pathogenesis and development of many diseases, including …