The High‐Intrinsic Diels—Alder Reactivity of (‐)‐Galiellalactone; Generating Four Quaternary Carbon Centers under Mild Conditions.

Nussbaum, Franz von; Hanke, Roman; Fahrig, Thomas; Benet‐Buchholz, Jordi

doi:10.1002/chin.200446213

Cited by 2 publications

(2 citation statements)

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“…Galiellalactone contains a reactive ␣,␤-unsaturated lactone functionality, and galiellalactone has been demonstrated to react with nitrogen-and sulfur-nucleophiles to produce inactive adducts (22). With the reactive potential of galiellalactone toward biological nucleophiles in consideration, we were interested in investigating whether galiellalactone can alkylate STAT3 and thereby inhibit the DNA binding as there is precedence that direct covalent modification of STAT3 with small molecules (23,24) or through cysteine oxidation (25) can block the transcriptional activity of STAT3.…”

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confidence: 99%

Galiellalactone Is a Direct Inhibitor of the Transcription Factor STAT3 in Prostate Cancer Cells

Don‐Doncow

Escobar

Johansson

et al. 2014

Journal of Biological Chemistry

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Background: STAT3 is constitutively active in castration-resistant prostate cancer and the fungal metabolite galiellalactone inhibits STAT3 signaling. Results: Galiellalactone binds covalently to one or more cysteines in STAT3 and prevents STAT3 binding to DNA. Conclusion: Galiellalactone inhibits STAT3 signaling by binding directly to STAT3. Significance: Galiellalactone is a promising direct STAT3 inhibitor for treatment of castration-resistant prostate cancer.

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confidence: 99%

Galiellalactone Is a Direct Inhibitor of the Transcription Factor STAT3 in Prostate Cancer Cells

Don‐Doncow

Escobar

Johansson

et al. 2014

Journal of Biological Chemistry

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“…Recent data suggest that Stat3 is involved in the development of prostate cancer [Calo et al, 2003;Tam et al, 2007]. Galiellalactone was isolated from the ascomycete Galiella rufa and inhibits the interleukin-6 signaling pathway by interfering with Stat3 signaling [Weidler et al, 2000;von Nussbaum et al, 2004]. Galiellalactone has been reported to show growthinhibitory effects on Stat3-expressing prostate cancer cells both in vivo and in vitro [Hellsten et al, 2008].…”

Section: Signal Transducer and Activator Of Transcription 3 (Stat3) Imentioning

confidence: 99%

Development of drugs against hormone‐refractory prostate cancer

Kageyama

2008

Drug Development Research

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The development of novel drugs for prostate cancer refractory to androgen deprivation therapy has been of great interest due to the lack of effective treatment modalities that can prolong the survival of such patients. The recent introduction of docetaxel-based combination chemotherapy has been a breakthrough with a modest, but significant, survival benefit. However, the improved survival period measured in months is far from ideal considering the non-negligible adverse events associated with docetaxel. Thus, numerous preclinical and clinical studies have been conducted to explore more favorable approaches to hormone-refractory prostate cancer. The novel agents under investigation include new chemotherapeutic drugs, drugs targeting signal transduction pathways, apoptosis modulators, drugs targeting the tumor microenvironment, molecular chaperone inhibitors, and dietary ingredients. Unfortunately, none of these agents have shown superior single-agent activity relative to docetaxel-based therapy to date. Therefore, developing the most effective combination therapies of new agents and docetaxel-based chemotherapy seems to be a reasonable approach until novel agents that can overcome the drug resistance of hormone-refractory prostate cancer cells emerge. Drug Dev Res 69 : 431-450, 2008.

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The High‐Intrinsic Diels—Alder Reactivity of (‐)‐Galiellalactone; Generating Four Quaternary Carbon Centers under Mild Conditions.

Cited by 2 publications

References 1 publication

Galiellalactone Is a Direct Inhibitor of the Transcription Factor STAT3 in Prostate Cancer Cells

Galiellalactone Is a Direct Inhibitor of the Transcription Factor STAT3 in Prostate Cancer Cells

Development of drugs against hormone‐refractory prostate cancer

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