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Differential Expression of Axl and Gas6 in Renal Cell Carcinoma Reflecting Tumor Advancement and Survival
Tumor Gas6 mRNA levels correlated to survival, tumor-associated variables, and disease severity as did serum levels of soluble sAxl and Gas6 protein, but no correlation between Axl protein in tumor tissue and survival was found. Expand
TRPV4 Regulates Breast Cancer Cell Extravasation, Stiffness and Actin Cortex
Metastasis is a significant health issue. The standard mode of care is combination of chemotherapy and targeted therapeutics but the 5-year survival rate remains low. New/better drug targets that canExpand
Galiellalactone Is a Direct Inhibitor of the Transcription Factor STAT3 in Prostate Cancer Cells*♦
It is demonstrated with chemical and molecular pharmacological methods that galiellalactone is a cysteine reactive inhibitor that covalently binds to one or more cysteines in STAT3 and that this leads to inhibition of STAT3 binding to DNA and thus blocks STAT3 signaling without affecting phosphorylation. Expand
Tensin3 Is a Negative Regulator of Cell Migration and All Four Tensin Family Members Are Downregulated in Human Kidney Cancer
The findings indicate that the Tensins may represent a novel group of metastasis suppressors in the kidney, the loss of which leads to greater tumor cell motility and consequent metastasis. Expand
Galiellalactone Inhibits Stem Cell-Like ALDH-Positive Prostate Cancer Cells
Targeting the STAT3 pathway in prostate cancer cells, including prostate cancer stem cell-like cells, is a promising therapeutic approach and galiellalactone is an interesting compound for the development of future prostate cancer drugs. Expand
Reversible Michael additions: covalent inhibitors and prodrugs.
This review focuses on biologically active compounds that are Michael acceptors and how the reversible nature of the Michael addition reaction influences biological activity and how this can be exploited in designing prodrugs. Expand
Galiellalactone is a novel therapeutic candidate against hormone‐refractory prostate cancer expressing activated Stat3
In this study, the in vitro and in vivo effects of the fungal metabolite galiellalactone, a direct inhibitor of Stat3, on PCa cells are investigated. Expand
Biologically active secondary metabolites from the ascomycete A111-95. 2. Structure elucidation.
Eight secondary metabolites were isolated from submerged cultures of the ascomycete A111-95 during a search for new nematicidal metabolites and all compounds showed moderate or weak cytotoxic activities. Expand
CD73 Immune Checkpoint Defines Regulatory NK-cells within the Tumor Microenvironment.
It is found that tumor-infiltrating NK cells upregulate CD73 expression and the frequency of these CD73+ NK cells correlated with larger tumor size in breast cancer patients, and thatCD73 expression defines an inducible population of NK cells with immune regulatory properties within the tumor microenvironment. Expand
Preclinical Characterization of 3β-(N-Acetyl l-cysteine methyl ester)-2aβ,3-dihydrogaliellalactone (GPA512), a Prodrug of a Direct STAT3 Inhibitor for the Treatment of Prostate Cancer.
In vitro studies showed that 6 is rapidly converted to 1 in plasma and is stable in a buffer solution and the favorable druglike properties and safety profile of 6 warrant further studies of 6 for the treatment of castration-resistant prostate cancer. Expand