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Small molecule inhibitors of p21

Specific inhibitors of protein p21 as therapeutic agents

Ansprechpartner

Dr. Sabina Heim

Kurzbeschreibung

Challenge

Cancer is the second leading cause of deaths among seniors and the prevalence is rising due to population ageing. The amount and severity of side effects of available drugs underlines the need to generate novel and efficacious drugs, which target specifically signaling pathways that are misregulated in the relevant disease. The CDK-Inhibitor 1, also called p21, was identified as a promising target as increased p21 levels have been found in acute promyelocytic leukemia (APL), kidney and breast cancer, whereas genetic deletions of p21 inhibit APL tumorigenesis and tumor progression in mice. In addition, downregulation of p21 causes positive effects on stem cell function and ageing as well as on wound healing in suitable mouse models. Although a beneficial effect of p21 inhibition could be demonstrated, so far no p21 inhibitors have reached the market yet.
Technology
The present technology relates to novel inhibitors of p21 as therapeutic agents for promoting cell regeneration and for the treatment of cancer. The p21 inhibitors were identified in a cell-based assay. The selected compunds show no effect on p53 itself or on targets of p53 with the aim of leaving desirable functions of p53, such as e.g. apoptosis, unaffected. The compounds do not show cytotoxic effects and the IC50 values range in the nM-1μM concentration. Currently, SAR studies on the most promising candidates are ongoing.
Further Reading
Viale A., et al., Nature. 2009 Jan 1;457(7225):51-6.

Choudhury A. R. et al., Nat Genet. 2007 Jan;39(1):99-105.

Bedelbaeva K. et al., Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5845-50.
Rudolph et al., J. Med. Chem. 2015, 58, 111−129. 

Technologie

Entwicklungsstand

Compounds were validated in in vitro and cellular assays, SAR studies are ongoing in vivo studies in well-established mouse models are in preparation.

Vorteile/Nutzen

The present technology relates to novel inhibitors of p21 as therapeutic agents for promoting cell regeneration and for the treatment of cancer.

Publikationsnummer

Priority filed 13.09.2012 (WO2014051125), patent applications pending in EP, US and JP.

Ansprechpartner Patentverwertung

Dr. Sabina Heim
Technology Manager
Ascenion GmbH
T: +49 531 618120-90
F: +49 531 618120-98
heim@ascenion.de

Angebot ist interessant für

Commercial Opportunity The technology is offered for co-development or in-licensing.

 

Anschrift

  • Beutenbergstraße 11
  • 07745 Jena

Ansprechpartner

 
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