MilliporeSigma
  • Home
  • Search Results
  • A Novel Small-Molecule Inhibitor Targeting CREB-CBP Complex Possesses Anti-Cancer Effects along with Cell Cycle Regulation, Autophagy Suppression and Endoplasmic Reticulum Stress.

A Novel Small-Molecule Inhibitor Targeting CREB-CBP Complex Possesses Anti-Cancer Effects along with Cell Cycle Regulation, Autophagy Suppression and Endoplasmic Reticulum Stress.

PloS one (2015-04-22)
Jong Woo Lee, Hee Sun Park, Sin-Aye Park, Seung-Hee Ryu, Wuyi Meng, Juliane M Jürgensmeier, Jonathan M Kurie, Waun Ki Hong, Julie L Boyer, Roy S Herbst, Ja Seok Koo
ABSTRACT

Lung adenocarcinoma, the most common subtype of lung cancer, is the leading cause of cancer death worldwide. Despite attempts for the treatment of lung cancer which have been accumulating, promising new therapies are still needed. Here, we found that cyclic-AMP response element-binding protein (CREB)-CREB binding protein (CBP) transcription factors complex inhibitor, Naphthol AS-TR phosphate (NASTRp), is a potential therapeutic agent for lung cancer. We show that NASTRp inhibited oncogenic cell properties through cell cycle arrest with concomitant suppression of tumor-promoting autophagy with down-regulations of Atg5-12 and Atg7, and accumulation of p62 in human lung cancer cell lines. In addition, NASTRp induced expression of endoplasmic reticulum stress markers such as DDIT3/CHOP, and led to apoptosis along with Bim induction. These findings suggest that transcription factor/co-activator complex, CREB-CBP, can be a potential therapeutic target and its inhibition could be a novel therapeutic strategy for lung cancer.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Sodium phosphate dibasic, BioReagent, suitable for cell culture, suitable for insect cell culture, ≥99.0%, free-flowing, Redi-Dri
Sigma-Aldrich
Sodium phosphate dibasic, puriss. p.a., ACS reagent, anhydrous, ≥99.0% (T)
Fluorescein, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
Sodium phosphate dibasic, puriss., meets analytical specification of Ph. Eur., BP, USP, FCC, E 339, anhydrous, 98-100.5% (calc. to the dried substance)
Sigma-Aldrich
Ethylenediaminetetraacetic acid solution, BioUltra, for molecular biology, pH 8.0, ~0.5 M in H2O
Sigma-Aldrich
Anti-GADD153 antibody produced in rabbit, affinity isolated antibody
Sigma-Aldrich
Monoclonal Anti-ATG5 antibody produced in mouse, clone 3D2, purified immunoglobulin, buffered aqueous solution
Sigma-Aldrich
Monoclonal Anti-NUP62 antibody produced in mouse, clone 2D3, purified immunoglobulin, buffered aqueous solution
Sigma-Aldrich
Monoclonal Anti-MAP1LC3B antibody produced in mouse, clone 4E11, purified immunoglobulin, buffered aqueous solution
Sigma-Aldrich
Monoclonal Anti-CCND1 antibody produced in mouse, clone CD1.1, purified immunoglobulin, buffered aqueous solution
Sigma-Aldrich
Anti-CCNA2 antibody produced in rabbit, Prestige Antibodies® Powered by Atlas Antibodies, affinity isolated antibody, buffered aqueous glycerol solution
Sigma-Aldrich
Monoclonal Anti-CCNB1 antibody produced in mouse, clone 1C8, purified immunoglobulin, buffered aqueous solution
Sigma-Aldrich
Monoclonal Anti-GTF2H1 antibody produced in mouse, clone 1F12-1B5, purified immunoglobulin, buffered aqueous solution
Sigma-Aldrich
Anti-Cyclin B1 antibody produced in rabbit, affinity isolated antibody
Sigma-Aldrich
Anti-CASP3 antibody produced in rabbit, affinity isolated antibody
Sigma-Aldrich
Anti-CCNE2 antibody produced in rabbit, purified immunoglobulin, buffered aqueous solution
Sigma-Aldrich
Anti-CASP3 antibody produced in rabbit, Prestige Antibodies® Powered by Atlas Antibodies, affinity isolated antibody, buffered aqueous glycerol solution
Sigma-Aldrich
Sodium phosphate dibasic, 99.95% trace metals basis
Sigma-Aldrich
Sodium phosphate dibasic, purum p.a., anhydrous, ≥98.0% (T)
Sigma-Aldrich
Sodium phosphate dibasic, BioUltra, for molecular biology, ≥99.5% (T)
Sigma-Aldrich
Anti-CASP3 antibody produced in rabbit, IgG fraction of antiserum
Sigma-Aldrich
Monoclonal Anti-DDIT3 antibody produced in mouse, clone 2G3, purified immunoglobulin, buffered aqueous solution
Sigma-Aldrich
Anti-BCL2L11 (Ab-69) antibody produced in rabbit, affinity isolated antibody
Sigma-Aldrich
Anti-CCND1 antibody produced in mouse, purified immunoglobulin, buffered aqueous solution
Sigma-Aldrich
Anti-phospho-CREB1 (pSer129) antibody produced in rabbit, affinity isolated antibody
Sigma-Aldrich
Anti-GADD153 antibody produced in rabbit, affinity isolated antibody, buffered aqueous solution
Sigma-Aldrich
DAPI, for nucleic acid staining
Sigma-Aldrich
Digitonin, Used as non-ionic detergent
Sigma-Aldrich
Ethylenediaminetetraacetic acid, BioUltra, anhydrous, ≥99% (titration)
Sigma-Aldrich
Sodium phosphate dibasic, BioReagent, suitable for cell culture, suitable for insect cell culture, ≥99.0%