Recent update on development of small-molecule STAT3 inhibitors for cancer therapy: from phosphorylation inhibition to protein degradation
Signal transducer and activator of transcription 3 (STAT3) is a transcription factor that
regulates various biological processes, including proliferation, metastasis, angiogenesis …
regulates various biological processes, including proliferation, metastasis, angiogenesis …
Protein degradation technology: a strategic paradigm shift in drug discovery
Targeting pathogenic proteins with small-molecule inhibitors (SMIs) has become a widely
used strategy for treating malignant tumors. However, most intracellular proteins have been …
used strategy for treating malignant tumors. However, most intracellular proteins have been …
Application of quinoline ring in structural modification of natural products
YQ Zhao, X Li, HY Guo, QK Shen, ZS Quan, T Luan - Molecules, 2023 - mdpi.com
Natural compounds are rich in pharmacological properties that are a hot topic in
pharmaceutical research. The quinoline ring plays important roles in many biological …
pharmaceutical research. The quinoline ring plays important roles in many biological …
Natural product-inspired targeted protein degraders: advances and perspectives
J Li, Z Cai, XW Li, C Zhuang - Journal of Medicinal Chemistry, 2022 - ACS Publications
Targeted protein degradation (TPD), a promising therapeutic strategy in drug discovery, has
great potential to regulate the endogenous degradation of undruggable targets with small …
great potential to regulate the endogenous degradation of undruggable targets with small …
Discovery of benzochalcone derivative as a potential antigastric cancer agent targeting signal transducer and activator of transcription 3 (STAT3)
J Dong, J Yang, W Yu, H Li, M Cai, JL Xu… - Journal of Enzyme …, 2022 - Taylor & Francis
Gastric cancer remains a significant health burden worldwide. In continuation of our
previous study and development of effective small molecules against gastric cancer, a series …
previous study and development of effective small molecules against gastric cancer, a series …
Synthesis and evaluation of novel tetrahydroisoquinoline-benzo [h] chromen-4-one conjugates as dual ABCB1/CYP1B1 inhibitors for overcoming MDR in cancer
J Dong, YL Li, Z **, Z Wu, M Cai, G Pan, W Ye… - Bioorganic & Medicinal …, 2024 - Elsevier
The emergence of multidrug resistance (MDR) in malignant tumors is one of the major
threats encountered currently by many chemotherapeutic agents. Among the various …
threats encountered currently by many chemotherapeutic agents. Among the various …
Synthesis and evaluation of WK-X-34 derivatives as P-glycoprotein (P-gp/ABCB1) inhibitors for reversing multidrug resistance
F Cao, Y Li, F Ma, Z Wu, Z Li, ZS Chen… - RSC Medicinal …, 2024 - pubs.rsc.org
The emergence of multidrug resistance (MDR) in malignant tumors is one of the leading
threats encountered currently by many chemotherapeutic agents. A proposed strategy to …
threats encountered currently by many chemotherapeutic agents. A proposed strategy to …
A comprehensive review of emerging approaches in machine learning for de novo PROTAC design
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 …
α-naphthoflavone-derived cytochrome P450 (CYP) 1B1 degraders specific for sensitizing CYP1B1-mediated drug resistance to prostate cancer DU145: Structure …
P Chen, S Wang, C Cao, W Ye, M Wang, C Zhou… - Bioorganic …, 2021 - Elsevier
We previously discovered extrahepatic cytochrome P450 1B1 (CYP1B1) degraders able to
overcome drug resistance toward docetaxel using a PROTACs technology, however, the …
overcome drug resistance toward docetaxel using a PROTACs technology, however, the …
New perspectives of CYP1B1 inhibitors in the light of molecular studies
R Mikstacka, Z Dutkiewicz - Processes, 2021 - mdpi.com
Human cytochrome P450 1B1 (CYP1B1) is an extrahepatic heme-containing
monooxygenase. CYP1B1 contributes to the oxidative metabolism of xenobiotics, drugs, and …
monooxygenase. CYP1B1 contributes to the oxidative metabolism of xenobiotics, drugs, and …