Get e-Alerts Abstract Prostate cancer cell types, we report on the synthesis, enzymatic stability, and antitumor activity of novel bioconjugates containing the chemotherapeutic agent daunorubicin attached through an oxime bond to various gonadotropin-releasing hormone-III GnRH-III derivatives.
In order to increase the enzymatic stability of the bioconjugates in particular against chymotrypsin4Ser was replaced by N-Me-Ser or Lys Ac.
A compound in which 4Lys was not acetylated was also prepared, with the aim of investigating the influence of the free ε-amino group on the biochemical properties.
The in vitro cytostatic effect of the bioconjugates was determined on MCF-7 human breast, HT human colon, and LNCaP human prostate cancer cells by 3- 4,5-dimethylthiazolyl -2,5-diphenyltetrazolium bromide assay. The results showed that 1 all synthesized bioconjugates had in vitro cytostatic effect, 2 they were stable in human serum at least for 24 h, and 3 they were hydrolyzed in the presence of lysosomal homogenate.
- Afala krónikus prosztatitis
- Fájdalom prosztata a végbélben
- A prosztatitis kiszámítása és kalcinálása
- A prosztatitis okai korai életkorban
All compounds were stable in the presence of 1 pepsin and 2 trypsin except for the 4Lys containing bioconjugate. In the presence of chymotrypsin, all bioconjugates were digested; the degradation rate strongly depending on their structure.
The bioconjugates in which 4Ser was replaced by N-Me-Ser or Lys Ac had the highest enzymatic stability, making them potential candidates for oral administration. In vivo tumor growth inhibitory effect of two selected bioconjugates was evaluated on orthotopically developed C26 murine colon carcinoma bearing mice.
The results indicated that the compound containing Lys Ac in position 4 had significantly higher antitumor activity than the parent bioconjugate.
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- Visszatér a prostatitisből
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- This is extremely important since gastric cancer is the second most common cause of cancer deaths worldwide, claiming almostlives annually, 60 percent of which are Asians.
- Pituitary adenoma xenografts were generated in immunocompromised mice.
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Bioorganic Chemistry88 Pharmaceutics10 4 Comparative cell biological study of in vitro antitumor and antimetastatic activity on melanoma cells of GnRH-III-containing conjugates modified with short-chain prostate cancer cell types acids. Beilstein Journal of Organic Chemistry14 Synthesis and in vitro biochemical evaluation of oxime bond-linked daunorubicin—GnRH-III conjugates developed for targeted drug delivery. Drug targeting to decrease cardiotoxicity — determination of the cytotoxic effect of GnRH-based conjugates containing doxorubicin, daunorubicin and methotrexate on human cardiomyocytes and endothelial cells.
On the design principles of peptide—drug conjugates for ásványi fürdők prosztatitis drug delivery to the malignant tumor site. Improved in prostate cancer cell types antitumor effect of a daunorubicin - GnRH-III bioconjugate modified by apoptosis inducing agent butyric acid on colorectal carcinoma bearing mice.
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Modification of daunorubicin-GnRH-III bioconjugates with oligoethylene glycol derivatives to improve solubility and bioavailability for targeted cancer chemotherapy. Biopolymers3 Drug delivery and release systems for targeted tumor therapy.
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Journal of Chromatography B, Gonadotropin-releasing hormone receptors as molecular therapeutic targets in prostate cancer: Current options and emerging strategies.
Cancer Treatment Reviews39 6 Metabolic stability of long-acting luteinizing hormone-releasing hormone antagonists.