Molecular glues: the adhesive connecting targeted protein degradation to the clinic

JM Sasso, R Tenchov, DS Wang, LS Johnson… - Biochemistry, 2022 - ACS Publications
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 …

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” …

[HTML][HTML] 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 …

[HTML][HTML] 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 …

[HTML][HTML] 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 developing proteolysis targeting chimeras (PROTACs) is the establishment of
a universal platform applicable in multiple scenarios for precise degradation of proteins of …

[HTML][HTML] The current status and future prospects for therapeutic targeting of KEAP1-NRF2 and β-TrCP-NRF2 interactions in cancer chemoresistance

R Srivastava, R Fernández-Ginés, JA Encinar… - Free Radical Biology …, 2022 - Elsevier
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 …

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 …

Targeting the epidermal growth factor receptor with molecular degraders: State-of-the-art and future opportunities

P Maity, J Chatterjee, KT Patil, S Arora… - Journal of Medicinal …, 2023 - ACS Publications
Epidermal growth factor receptor (EGFR) is an oncogenic drug target and plays a critical role
in several cellular functions including cancer cell growth, survival, proliferation …

[HTML][HTML] Digesting the role of JAK-STAT and cytokine signaling in oral and gastric cancers

Y Ni, JT Low, J Silke, LA O'Reilly - Frontiers in Immunology, 2022 - frontiersin.org
When small proteins such as cytokines bind to their associated receptors on the plasma
membrane, they can activate multiple internal signaling cascades allowing information from …

A comprehensive review of BET-targeting PROTACs for cancer therapy

XL Zhou, F Zhao, YT Xu, YY Guan, T Yu… - Bioorganic & Medicinal …, 2022 - Elsevier
Targeted protein degradation using proteolysis-targeting chimeras (PROTACs) has
emerged as an effective strategy for drug discovery, given their unique advantages over …