CDK5 Inhibitor Downregulates Mcl-1 and Sensitizes Pancreatic Cancer Cell Lines to Navitoclax

Developing small molecules that indirectly regulate Mcl-1 function has attracted a lot of attention in recent years. Here, we report the discovery of an aminopyrazole, 2-([1,1′-biphenyl]-4-yl)-N-(5-cyclobutyl-1H-pyrazol-3-yl)acetamide (analog 24), which selectively inhibited cyclin-dependent kinase...

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Veröffentlicht in:	Molecular pharmacology 2019-10, Vol.96 (4), p.419-429
Hauptverfasser:	Kour, Smit, Rana, Sandeep, Contreras, Jacob I., King, Hannah M., Robb, Caroline M., Sonawane, Yogesh A., Bendjennat, Mourad, Crawford, Ayrianne J., Barger, Carter J., Kizhake, Smitha, Luo, Xu, Hollingsworth, Michael A., Natarajan, Amarnath
Format:	Artikel
Sprache:	eng
Schlagworte:	Aniline Compounds - pharmacology Cell Line, Tumor Cell Proliferation - drug effects Cell Survival - drug effects Cyclin-Dependent Kinase 5 - antagonists & inhibitors Cyclin-Dependent Kinase 5 - genetics Dose-Response Relationship, Drug Drug Synergism Gene Expression Regulation, Neoplastic - drug effects HeLa Cells Humans Myeloid Cell Leukemia Sequence 1 Protein - metabolism Pancreatic Neoplasms - drug therapy Pancreatic Neoplasms - genetics Pancreatic Neoplasms - metabolism Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Pyrazoles - chemistry Pyrazoles - pharmacology Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology Sulfonamides - pharmacology
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