Targeting protein kinase C-alpha (PKC-alpha) in cancer with the phosphorothioate antisense oligonucleotide aprinocarsen.
Antisense oligonucleotides (ASOs) offer a novel pharmacological platform to develop highly specific drugs. As shown by the clinical development of aprinocarsen, an ASO directed against protein kinase C-alpha (PKC-alpha), this platform has made a remarkable advance from the bench to the bedside. This review summarizes the rationale of the early development of aprinocarsen and current clinical experience.
Lahn
Michael
M
Eli Lilly and Company, Indianapolis, Indiana 46285, USA. mlahn@lilly.com
Sundell
Karen
K
Moore
Stephanie
S
D006801:Humans; D016376:Oligonucleotides, Antisense / Q000494:pharmacology*; D011493:Protein Kinase C / Q000037:antagonists & inhibitors* / Q000096:biosynthesis / Q000235:genetics; D051571:Protein Kinase C-alpha; D012333:RNA, Messenger / Q000187:drug effects*
D016376:Oligonucleotides, Antisense; D012333:RNA, Messenger; C496628:PRKCA protein, human; D011493:Protein Kinase C; D051571:Protein Kinase C-alpha