Disease relevance of NSC 287492

• Selective cytotoxicity of ascochlorin in ER-negative human breast cancer cell lines [1].
• Antiviral (HSV-1) and cytotoxic activities of these ascochlorin analogs were evaluated [2].

High impact information on NSC 287492

• The AP-1 family member most specifically affected by ascochlorin was Fra-1 [3].
• Here we examined the effect of ascochlorin, a prenyl-phenol anti-tumor compound from the fungus Ascochyta viciae, on the regulation of signaling pathways that control MMP-9 expression in human renal carcinoma (Caki-1) cells [3].
• Ascochlorin inhibits matrix metalloproteinase-9 expression by suppressing activator protein-1-mediated gene expression through the ERK1/2 signaling pathway: inhibitory effects of ascochlorin on the invasion of renal carcinoma cells [3].
• Ascochlorin did not affect the activation of the c-Jun N-terminal or p38 kinase pathways [3].
• Ascochlorin reduced the invasive activity of Caki-1 cells and inhibited phorbol 12-myristate 13-acetate-induced increases in MMP-9 expression and activity in a dose-dependent manner [3].

Biological context of NSC 287492

• An ascochlorin derivative, AS-6, reduces insulin resistance in the genetically obese diabetic mouse, db/db [4].
• The prenylphenol antibiotic ascochlorin suppressed the AP-1 activity of MX-1 cells, and selectively killed MX-1 cells, partly due to induction of apoptosis [1].

Anatomical context of NSC 287492

• Treatment with an ascochlorin derivative, AS-6 increases 45Ca2+ binding on the plasma membrane of adipocytes in db/db mice [5].
• The ascochlorin derivative, AS-6, inhibits TNF-alpha-induced adhesion molecule and chemokine expression in rat vascular smooth muscle cells [6].
• However, 4-O-methyl ascochlorin induced apoptosis in Jurkat cells deficient of caspase-8 or Fas-associated death domain protein [7].

Associations of NSC 287492 with other chemical compounds

• The prenyl-phenol antibiotics ascochlorin-related compounds, are known to reduce serum cholesterol and triglyceride, suppress hypertension, and ameliorate types-I and II diabetes [8].

Gene context of NSC 287492

• We previously found that one ascochlorin (1) derivative, 4-O-carboxymethyl-ascochlorin (2), is a potent agonist of peroxisome proliferator activated receptor gamma (PPARgamma) [9].
• Here we report that the ascochlorin derivative, 4-O-carboxymethyl ascochlorin (AS-6) acts as a potent activator of the nuclear hormone receptor, PPARgamma, although it does not activate the related receptors, PPARalpha, PPARdelta or RARalpha [8].

Analytical, diagnostic and therapeutic context of NSC 287492

• An ascochlorin derivative, AS-6, is a new hypoglycemic agent orally active in both obese hyperinsulinemic and insulin-deficient diabetic animal models [4].

References