[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] Exploiting E3 ubiquitin ligases to reeducate the tumor microenvironment for cancer therapy

XM Li, ZY Zhao, X Yu, QD Xia, P Zhou… - … Hematology & Oncology, 2023 - Springer
Tumor development relies on a complex and aberrant tissue environment in which cancer
cells receive the necessary nutrients for growth, survive through immune escape, and …

[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 …

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 …

Bifunctional robots inducing targeted protein degradation

ME Sobhia, H Kumar, S Kumari - European Journal of Medicinal Chemistry, 2023 - Elsevier
The gaining importance of Targeted Protein Degradation (TPD) and PROTACs (PROteolysis-
TArgeting Chimeras) have drawn the scientific community's attention. PROTACs are …

Advancement of targeted protein degradation strategies as therapeutics for undruggable disease targets

MP Kannan, S Sreeraman, CS Somala… - Future Medicinal …, 2023 - Future Science
Targeted protein degradation (TPD) aids in developing novel bifunctional small-molecule
degraders and eliminates proteins of interest. The TPD approach shows promising results in …

Targeted protein modification as a paradigm shift in drug discovery

R Amirian, MA Badrbani, Z Izad, H Samadian… - European Journal of …, 2023 - Elsevier
Abstract Targeted Protein Modification (TPM) is an umbrella term encompassing numerous
tools and approaches that use bifunctional agents to induce a desired modification over the …

[HTML][HTML] Bromodomain and extraterminal (BET) proteins: biological functions, diseases, and targeted therapy

ZQ Wang, ZC Zhang, YY Wu, YN Pi, SH Lou… - … and Targeted Therapy, 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 …

Design and synthesis of proteolysis-targeting chimeras (PROTACs) as degraders of glutathione peroxidase 4

M Cai, F Ma, C Hu, H Li, F Cao, Y Li, J Dong… - Bioorganic & Medicinal …, 2023 - Elsevier
Ferroptosis is a new type of regulated, non-apoptotic cell death driven by iron-dependent
phospholipid peroxidation. Inducing cell ferroptosis by inactivating glutathione peroxidase 4 …