new HSD17beta1 inhibitors in Cancer Therapy

Popis technologie

Název technologie: new HSD17beta1 inhibitors in Cancer Therapy
Motivace: 17βHSD1 is an enzyme that has been known to play a pivotal role in tissue specific estradiol (E2) synthesis for more than fifty years. E2 is a very potent hormone, which regulates the expression of a variety of genes by binding to estrogen receptors (ER) and thus it plays a crucial role in the physiological as well as pathological proliferation and differentiation of the target cell. 17βHSD1 affects breast cancer cell proteome and modulates expression of several genes at both mRNA and protein levels. Furthermore, it is associated with an increased risk of cell migration and cancer relapse. Therefore regulation of 17βHSD1 should be considered as potential novel endocrine therapy or 17βHSD1 expression as an independent prognostic marker in breast cancer patients.
Popis: We have successfully developed highly potent and specific non-estrogenic inhibitors of 17βHSDs. We have recently shown the efficacy of these compounds in in vitro and in vivo testing of E1 to E2 conversion after application of lead compounds.

SAFETY - NOVELTY
No toxic effect up to 2mg/kg
Low estrogenisity of lead compound EP449
Experiments on T47D cells show inhibition of HSD17b1 (accumulation of E1 in HPLC MS/MS detectable)
proof of concept experiment in eggs has been successful - with reduced tumor size and number of metastases, in comparison to Tamoxifen (standard care)
Komerční využití: We are looking for out-licensing partners or partners to co-develop the project further
Status IP ochrany: PCT/CZ2017/050022
Fáze vývoje technologie:
Strategie pro hledání partnera: Licencování Spolupráce
Další informace:
Ilustrační obrázky: Žádný obrázek není vložen
Klíčová slova: breast cancer endometriosis estrogen HSD17beta1
Kategorie: Farmacie Věda o životě a zdraví Chemie
Vlastník technologie: IOCB, IMG Pague, IMTM Olomouc and Helmholtz Zenter Munich
Instituce: Ústav organické chemie a biochemie AV ČR, v.v.i.
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