ArticleBioorganic & medicinal chemistry letters2013
Identification, synthesis and evaluation of substituted benzofurazans as inhibitors of CREB-mediated gene transcription.
Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 19 citations in OpenAlex.
- Review
- Review
- Direct Targeting of CREB1 with Imperatorin Inhibits TGFAdvanced science (Weinheim, Baden-Wurttemberg, Germany) · 2020Article
- A suite of bioassays to evaluate CREB inhibitors.Methods in enzymology · 2020Article
- Compounds with capacity to quench the tyrosyl radical in Pseudomonas aeruginosa ribonucleotide reductase.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2019Article
- Design, synthesis and biological evaluation of regioisomers of 666-15 as inhibitors of CREB-mediated gene transcription.Bioorganic & medicinal chemistry letters · 2017Article
- Small molecule inhibition of cAMP response element binding protein in human acute myeloid leukemia cells.Leukemia · 2016Article
- Systemic Inhibition of CREB is Well-tolerated in vivo.Scientific reports · 2016Article
- Control of CREB expression in tumors: from molecular mechanisms and signal transduction pathways to therapeutic target.Oncotarget · 2016Review
- Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity.Journal of medicinal chemistry · 2015Article
- PAINS in the assay: chemical mechanisms of assay interference and promiscuous enzymatic inhibition observed during a sulfhydryl-scavenging HTS.Journal of medicinal chemistry · 2015Article
- Irreversible binding of an anticancer compound (BI-94) to plasma proteins.Xenobiotica; the fate of foreign compounds in biological systems · 2015Article
- Novel Type of Prodrug Activation through a Long-Range O,N-Acyl Transfer: A Case of Water-Soluble CREB Inhibitor.ACS medicinal chemistry letters · 2014Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Cyclic-AMP response-element binding protein (CREB) is a stimulus-activated transcription factor. Its transcription activity requires its binding with CREB-binding protein (CBP) after CREB is phosphorylated at Ser133. The domains involved for CREB-CBP interaction are kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP. Recent studies suggest that CREB is an attractive target for novel cancer therapeutics. To identify novel chemotypes as inhibitors of KIX-KID interaction, we screened the NCI-diversity set of compounds using a split renilla luciferase assay and identified 2-[(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio]pyridine 1-oxide (compound 1, NSC228155) as a potent inhibitor of KIX-KID interaction. However, compound 1 was not particularly selective against CREB-mediated gene transcription in living HEK 293T cells. Further structure-activityrelationship studies identified 4-aniline substituted nitrobenzofurazans with improved selectivity.
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