Tuning isoform selectivity and bortezomib sensitivity with a new class of alkenyl indene PDI inhibitor

Protein disulfide isomerase (PDI, PDIA1) is an emerging therapeutic target in oncology. PDI inhibitors have demonstrated a unique propensity to selectively induce apoptosis in cancer cells and overcome resistance to existing therapies, although drug candidates have not yet progressed to the stage of...

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Veröffentlicht in:	European journal of medicinal chemistry 2020-01, Vol.186, p.111906-111906, Article 111906
Hauptverfasser:	Robinson, Reeder M., Reyes, Leticia, Duncan, Ravyn M., Bian, Haiyan, Strobel, Eric D., Hyman, Sarah L., Reitz, Allen B., Dolloff, Nathan G.
Format:	Artikel
Sprache:	eng
Schlagworte:	Bortezomib - chemical synthesis Bortezomib - chemistry Bortezomib - pharmacology Cell Line Cell Survival - drug effects Dose-Response Relationship, Drug Drug resistance ER stress Humans Isoenzymes - antagonists & inhibitors Isoenzymes - metabolism Molecular Structure Multiple myeloma Procollagen-Proline Dioxygenase - antagonists & inhibitors Procollagen-Proline Dioxygenase - metabolism Proteasome inhibitor Proteasome Inhibitors - chemical synthesis Proteasome Inhibitors - chemistry Proteasome Inhibitors - pharmacology Protein disulfide isomerase (PDI) Protein Disulfide-Isomerases - antagonists & inhibitors Protein Disulfide-Isomerases - metabolism Structure-Activity Relationship UPR
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