Selective degradation of hyperphosphorylated tau by proteolysis-targeting chimeras ameliorates cognitive function in Alzheimer's disease model mice

D Yao, T Li, L Yu, M Hu, Y He, R Zhang, J Wu… - Frontiers in …, 2024 - frontiersin.org
Alzheimer's disease (AD) is one of the most common chronic neurodegenerative diseases.
Hyperphosphorylated tau plays an indispensable role in neuronal dysfunction and synaptic …

Clinical pharmacology of RNAi-based therapeutics: a summary based on FDA-approved small-interfering RNAs

X Jing, V Arya, KS Reynolds, H Rogers - Drug Metabolism and Disposition, 2022 - ASPET
RNA-based oligonucleotide therapeutics are revolutionizing drug development for disease
treatment. This class of therapeutics differ from small molecules and protein therapeutics in …

PROTAC: a novel drug delivery technology for targeting proteins in cancer cells

R Bala, RK Sindhu, R Madaan… - Current Drug Discovery …, 2023 - ingentaconnect.com
The treatment measures of malignant carcinomas are most important for human health. In
recent years the use of targeted therapy based on small molecule compounds and identical …

Discovery of novel PROTACs based on multi-targeted angiogenesis inhibitors

R Si, P Hai, Y Zheng, N Liu, J Wang, Q Zhang… - Bioorganic & Medicinal …, 2023 - Elsevier
Anti-angiogenesis has been proved to be an effective strategy for the treatment of tumors.
Anti-angiogenic drugs had achieved certain therapeutic effects. However, drug resistance …

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 …

High affinity and low PARP-trapping benzimidazole derivatives as a potential warhead for PARP1 degraders

X Peng, Y Li, J Qu, L Jiang, K Wu, D Liu, Y Chen… - European Journal of …, 2024 - Elsevier
PARPi have been explored and applied in the treatment of various cancers with remarkable
efficacy, especially BRCA1/2 mutated ovarian, breast, prostate, and pancreatic cancers …

Pan-cancer analysis reveals the prognostic and immunologic roles of cereblon and its significance for PROTAC design

SH Zhang, N Zeng, JX Sun, CQ Liu, JZ Xu, MY Xu… - Heliyon, 2023 - cell.com
Background Cereblon (CRBN) has emerged as a vital E3 ubiquitin ligase for Proteolysis-
targeting chimera (PROTAC) design. However, few studies focus on the physiological …

Recent advances in the molecular design and applications of proteolysis targeting chimera-based multi-specific antiviral modality

Y Zhou, S Xua, N López-Carrobles, D Ding… - 2023 - digital.csic.es
Viral infections represent a major threat to human health and the global economy; however,
most of the currently available antiviral drugs are not fully effective in restricting viral …

[HTML][HTML] Targeted protein degradation: A promising approach for cancer treatment

MZI Khan, A Nazli, I Naz, D Khan, I Haq… - Journal of Pharmaceutical …, 2023 - Elsevier
Targeted protein degradation (TPD) is a promising approach that has the ability to address
disease-causing proteins. Compared to traditional inhibition, proteolysis targeting chimera …

A Comprehensive Review of Emerging Approaches in Machine Learning for De Novo PROTAC Design

Y Gharbi, R Mercado - arXiv preprint arXiv:2406.16681, 2024 - arxiv.org
Targeted protein degradation (TPD) is a rapidly growing field in modern drug discovery that
aims to regulate the intracellular levels of proteins by harnessing the cell's innate …