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NHR2 inhibitors


Abstract

Treatment of AML by inhibitors of NHR2 and/or RUNX1/ETO-tetramerization


Background

The formation and onset of the prevalent form of acute myeloid leukemia (AML, FAB subtype M2) requires RUNX1/ETO, the product of the t(8;21) chromosomal translocation. Tetramerization through the nervy homology region 2 (NHR2) of ETO is essential for the RUNX1/ETO-mediated transformation.


Solution

The inventors demonstrated that inhibition of NHR2 tetramerization by first-in-class small molecules is a viable entry point for the treatment of AML. Drug candidates have been identified by a small-molecule in silico screening and have been validated in cellular assays. Several compounds proved to be successful in inhibiting NHR2 tetramerization. Preferred compound 7.44 was able to slow tumor growth in a xenograft mouse model (SKNO 1 xenograft).

The pending patent application covers claims directed to a variety of chemotypes that proved activity against AML.


Advantages

  • Compounds for treatment of AML: unique mode of action, medical use/compound protection achievable, in vivo data from mouse model available
  • Access to inventor know-how

Service

On behalf of University of Düsseldorf, PROvendis offers this opportunity for licensing or co-development.


PROvendis GmbH

Dr. Andreas Wagener
+49.208 94105-38
aw@provendis.info
www.provendis.info
Address
Schloßstr. 11-15
45468 Mülheim an der Ruhr



Development status

Proof of concept


Keywords

NHR2 Inhibitors, acute myeloid leukemia, small molecules, Treatment, AML, chemotypes, provendis

Offer at Providers website


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