A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P‑Loop Conformation

STK17B is a member of the death-associated protein kinase family and has been genetically linked to the development of diverse diseases. However, the role of STK17B in normal and disease pathology is poorly defined. Here, we present the discovery of thieno[3,2-d] pyrimidine SGC-STK17B-1 (11s), a hi...

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Veröffentlicht in:	Journal of medicinal chemistry 2020-12, Vol.63 (23), p.14626-14646
Hauptverfasser:	Picado, Alfredo, Chaikuad, Apirat, Wells, Carrow I, Shrestha, Safal, Zuercher, William J, Pickett, Julie E, Kwarcinski, Frank E, Sinha, Parvathi, de Silva, Chandi S, Zutshi, Reena, Liu, Shubin, Kannan, Natarajan, Knapp, Stefan, Drewry, David H, Willson, Timothy M
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Apoptosis Regulatory Proteins - antagonists & inhibitors Apoptosis Regulatory Proteins - chemistry Apoptosis Regulatory Proteins - metabolism Catalytic Domain HEK293 Cells Humans Mice Microsomes, Liver - metabolism Molecular Dynamics Simulation Molecular Structure Protein Binding Protein Conformation Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - metabolism Protein Kinase Inhibitors - pharmacology Protein Serine-Threonine Kinases - antagonists & inhibitors Protein Serine-Threonine Kinases - chemistry Protein Serine-Threonine Kinases - metabolism Pyrimidines - chemical synthesis Pyrimidines - metabolism Pyrimidines - pharmacology Structure-Activity Relationship Thiophenes - chemical synthesis Thiophenes - metabolism Thiophenes - pharmacology
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