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 …
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
RNA-based oligonucleotide therapeutics are revolutionizing drug development for disease
treatment. This class of therapeutics differ from small molecules and protein therapeutics in …
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
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 …
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 …
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 …
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 …
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 …
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 …
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
Targeted protein degradation (TPD) is a promising approach that has the ability to address
disease-causing proteins. Compared to traditional inhibition, proteolysis targeting chimera …
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 …
aims to regulate the intracellular levels of proteins by harnessing the cell's innate …