Orally Bioavailable Proteolysis-Targeting Chimeras: An Innovative Approach in the Golden Era of Discovering Small-Molecule Cancer Drugs
Proteolysis-targeting chimeras (PROTACs) are an emerging therapeutic modality that show
promise to open a target space not accessible to conventional small molecules via a …
promise to open a target space not accessible to conventional small molecules via a …
[HTML][HTML] Proteolysis Targeting Chimeras (PROTACs) based on celastrol induce multiple protein degradation for triple-negative breast cancer treatment
X Gan, F Wang, J Luo, Y Zhao, Y Wang, C Yu… - European Journal of …, 2024 - Elsevier
The pursuit of single drugs targeting multiple targets has become a prominent trend in
modern cancer therapeutics. Natural products, known for their multi-targeting capabilities …
modern cancer therapeutics. Natural products, known for their multi-targeting capabilities …
A selective HK2 degrader suppresses SW480 cancer cell growth by degrading HK2
Y Liu, Y Liu, K Yang, Z Zhang, W Zhang, B Yang… - Chinese Chemical …, 2024 - Elsevier
Abstract Hexokinase 2 (HK2) is the rate-limiting enzyme in the first step of glycolysis,
catalyzing glucose to glucose-6-phosphate, and overexpressed in most cancer cells. HK2 …
catalyzing glucose to glucose-6-phosphate, and overexpressed in most cancer cells. HK2 …
EGFR degraders in non‐small‐cell lung cancer: Breakthrough and unresolved issue
J Shen, L Chen, J Liu, A Li, L Zheng… - Chemical Biology & …, 2024 - Wiley Online Library
The epidermal growth factor receptor (EGFR) has been well validated as a therapeutic target
for anticancer drug discovery. Osimertinib has become the first globally accessible third …
for anticancer drug discovery. Osimertinib has become the first globally accessible third …
[HTML][HTML] Therapeutic potential of targeting protein tyrosine phosphatases in liver diseases
A Wang, Y Zhang, X Lv, G Liang - Acta Pharmaceutica Sinica B, 2024 - Elsevier
Protein tyrosine phosphorylation is a post-translational modification that regulates protein
structure to modulate demic organisms' homeostasis and function. This physiological …
structure to modulate demic organisms' homeostasis and function. This physiological …
Synthetic approaches to constructing proteolysis targeting chimeras (PROTACs)
The development of various heterobifunctional constructs dubbed PRoteolysis-TArgeting
Chimeras (PROTACs) has gained a significant impetus in the last few years. A viable …
Chimeras (PROTACs) has gained a significant impetus in the last few years. A viable …
COVID-19 Therapies: Protease Inhibitions and Novel Degrader Strategies
M Reboud-Ravaux, C El Amri - Frontiers in Drug Discovery, 2022 - frontiersin.org
The global spread of severe acute respiratory syndrome corona virus-2 (SARS-CoV-2)
variants is alarming. In addition to vaccines, effective antiviral agents are urgently needed to …
variants is alarming. In addition to vaccines, effective antiviral agents are urgently needed to …
[HTML][HTML] Single-cell RNA sequencing reveals the effects of hederasaponin C in the treatment of diabetic nephropathy
J Liu, Q Zhang, W Zhao, J Guo, YK Wong… - Acta Materia …, 2023 - ucl.scienceopen.com
There is great demand for the development of novel efficient therapeutic strategies or
preventative measures to alleviate the life-threatening complications of type 2 diabetes …
preventative measures to alleviate the life-threatening complications of type 2 diabetes …
UPS: Opportunities and challenges for gastric cancer treatment
H Yang, H Ai, J Zhang, J Ma, K Liu, Z Li - Frontiers in Oncology, 2023 - frontiersin.org
Gastric cancer remains the fourth most frequently diagnosed malignancy and the fifth
leading cause of cancer-related mortality worldwide owning to the lack of efficient drugs and …
leading cause of cancer-related mortality worldwide owning to the lack of efficient drugs and …
Artificial Nucleic Acid Tractor-Directed Simultaneous Depletion of Oncogenic Membrane Proteins Without Hijacking Proteolysis-Specific Actuator
Z Zou, S Pan, Q Xue, T Chen, Z Huang, B Qing… - CCS …, 2024 - chinesechemsoc.org
Targeted protein degradation (TPD) is an emerging tool for degrading proteins of interest,
which affords an attractive modality for cancer therapy. However, the present TPD …
which affords an attractive modality for cancer therapy. However, the present TPD …