RGNCY-0064 (NASTRp (CREB)-CREB CBP inhibitor)

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NASTRp (Ntpthol AS-TR phosphate) is an inhibitor of cyclic-AMP responsive element-binding protein (CREB)-CREB binding protein (CBP) transcription factor complex.  NASTRp is a potential therapeutic agent for lung adenocarcinoma.  NASTRp was shown to inhibit oncogenic cell properties through cell cycle arrest with concomitant suppression of tumor-promoting autophagy with down-regulation of of Atg5-12 and Atg7 and accumulation of p62 in human lung cancer cell lines. Furthermore, NASTRp was also shown to induce expression of endoplasmic reticulum stress marker,s DDIT3/CHOP and led to apoptosis along with BIM induction.  NASTRp targeting the CREB-CBP transcription complex is a novel and potent anti-cancer agent showing multiple effects on critical pathways in cell biology.  This represents a novel class of targeted therapies in cancer.

Systematic Name:  3-((4-chloro-2-methylphenyl)carbamoyl)naphthalen-2-yl dihydrogen phosphate   

SMILES:  OP(OC1=CC2=CC=CC=C2C=C1C(NC3=C(C)C=C(Cl)C=C3)=O)(O)=O

Formula:  C18H15ClNO5P

Mol Wt:  391.74

PMID:  25897662