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Wnt pathway inhibitor: New Substance Class for Promising Novel Anti-Tumor Agent

Ref-Nr: TA-P-916


Kurzfassung

The Wnt signaling pathway plays an important role in the regulation of cell proliferation and differentiation. Aberrant activation of the Wnt signaling pathway is known to promote uncontrolled cell growth and survival. Compound library screening and med-chem based structure activity improvement revealed potent Wnt signaling inhibitors that selectively affected carcinoma cell lines. In addition, further experiments proved these compounds to induce apoptosis.


Hintergrund

The Wnt signalling pathway plays an important role in the regulation of cell proliferation and differentiation. Aberrant activation of the Wnt signalling pathway is known to promote uncontrolled cell growth and survival and can therefore be a major driving force in a broad spectrum of human cancers and diseases such as colon, skin, liver and ovary cancer. For example, the inhibition of aberrant Wnt signalling pathway activity in cancer cell lines effectively blocks their growth1 . Other disorders and diseases are considered to be influenced by an aberrant Wnt signaling pathway, too.

The lead compound shows low nM IC50 against colon cancer (stem) cell lines and specificity in epistasis and suppression of double axis formation. PD analyses revealed good CYP/kinase & hERG-profiles, metabolic stability as well as promising t1/2/AUC in mice. Further optimization of in vitro & in vivo ADMET is ongoing.


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Lösung

The systematic evaluation of Structure Activity Relationships (SAR) of several 100 hit variants have been investigated to yield a lead structure. Intensive medicinal chemistry on the lead compound improved the pharmacologic profile. 


Anwendungsbereiche

Development of a small molecule drug candidate for chemotherapy of cancer types such as colon, skin, liver and ovary cancer.


Deutsches Krebsforschungszentrum DKFZ

Dr. Frieder Kern
+49-6221-42-2952
f.kern@dkfz.de
www.dkfz.de
Adresse
Im Neuenheimer Feld 280
69120 Heidelberg



Entwicklungsstand

Präklinik


Stichworte

Therapeutics

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