[HTML][HTML] Comprehensive analysis of E3 ubiquitin ligases reveals ring finger protein 223 as a novel oncogene activated by KLF4 in pancreatic cancer

L Feng, J Wang, J Zhang, J Diao, L He, C Fu… - Frontiers in Cell and …, 2021 - frontiersin.org
Pancreatic cancer is one of the major malignancies and causes of mortality worldwide. E3
ubiquitin-protein ligases transfer activated ubiquitin from ubiquitin-conjugating enzymes to …

Discovery of Potent SOS1 PROTACs with Effective Antitumor Activities against NCI-H358 Tumor Cells In Vitro/In Vivo

X Pang, D Cui, B Lv, CY Wang - Journal of Medicinal Chemistry, 2024 - ACS Publications
Directly targeted KRAS inhibitors are now facing resistance problems, which might be
partially solved by the combination of SOS1 inhibitors with KRAS inhibitors. However, this …

Proteolysis Targeting Chimera Degraders of the METTL3–14 m6A-RNA Methyltransferase

F Errani, A Invernizzi, M Herok, E Bochenkova… - JACS Au, 2024 - ACS Publications
Methylation of adenine N6 (m6A) is the most frequent RNA modification. On mRNA, it is
catalyzed by the METTL3–14 heterodimer complex, which plays a key role in acute myeloid …

Microtubule‐targeting agents for cancer treatment: Seven binding sites and three strategies

X Wang, B Gigant, X Zheng, Q Chen - MedComm–Oncology, 2023 - Wiley Online Library
Microtubules are pivotal in diverse cellular functions encompassing cell signaling,
morphology, intracellular trafficking, and cell mitosis/division. They are validated targets for …

Photopharmacology of proteolysis-targeting chimeras: a new frontier for drug discovery

S Zeng, H Zhang, Z Shen, W Huang - Frontiers in Chemistry, 2021 - frontiersin.org
Photopharmacology is an emerging field that uses light to precisely control drug activity. This
strategy promises to improve drug specificity for reducing off-target effects. Proteolysis …

Advances in research on potential inhibitors of multiple myeloma

G Tang, S Huang, J Luo, Y Wu, S Zheng, R Tong… - European Journal of …, 2023 - Elsevier
Multiple myeloma (MM) is a common hematological malignancy. Although recent clinical
applications of immunomodulatory drugs, proteasome inhibitors and CD38-targeting …

Circular RNAs with efficacy in preclinical in vitro and in vivo models of esophageal squamous cell carcinoma

UH Weidle, T Sela, U Brinkmann… - Cancer Genomics & …, 2022 - cgp.iiarjournals.org
Esophageal cancer is associated with a dismal prognosis. The armamentarium of approved
drugs is focused on chemotherapy with modest therapeutic benefit. Recently, checkpoint …

It is theoretically possible to avoid misfolding into non-covalent lasso entanglements using small molecule drugs

Y Jiang, CM Deane, GM Morris… - PLoS computational …, 2024 - journals.plos.org
A novel class of protein misfolding characterized by either the formation of non-native
noncovalent lasso entanglements in the misfolded structure or loss of native entanglements …

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 …

[HTML][HTML] Novel inhibitors targeting the PGK1 metabolic enzyme in glycolysis exhibit effective antitumor activity against kidney renal clear cell carcinoma in vitro and in …

Y He, Y Luo, L Huang, D Zhang, H Hou, Y Liang… - European Journal of …, 2024 - Elsevier
Our previous research has revealed phosphoglycerate kinase 1 (PGK1) enhances
tumorigenesis and sorafenib resistance of kidney renal clear cell carcinoma (KIRC) by …