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Translating Tudor domain splicing inhibitors for oncological applications

Project description

From diabetes research to cancer therapy

The Tudor domain protein SMNDC1 plays a crucial role in gene expression by regulating RNA splicing events. It has been implicated in both the repression of insulin in pancreatic alpha cells and the splicing of key signalling molecules in cancer, making it a significant focus of research for therapeutic development. Given that SMNDC1 exhibits broad expression, it is not an ideal target for diabetes treatment. Researchers of the ERC-funded ONCO-SPLICE project propose to test SMNDC1 inhibitors in cancer models for treatment. The study will investigate the protein’s effects and develop a strategy for the clinical translation of SMNDC1 inhibitors as cancer therapeutics.

Objective

In our effort to characterize metabolic activities in the cells nucleus, we discovered that the understudied Tudor domain protein SMNDC1 controls the repression of insulin in pancreatic alpha cells through its role as a splicing modulator. Based on this finding, we developed the first selective SMNDC1 Tudor domain inhibitors, for which we observe interesting preliminary data on insulin induction in primary human pancreatic islets. However, as a pan-essential gene expressed in most tissues, SMNDC1 is not an ideal therapeutic target in diabetes, where exceptionally high safety margins are required.
Interestingly, independent findings published in a preprint established a role for SMNDC1 in cancer. These data show that SMNDC1 controls splicing of the ERK1 exon that bears the phosphorylation signal mediating RAS/RAF/MEK/ERK signaling. A significant fraction of ovarian and pancreatic carcinomas harbor SMNDC1 amplifications, and cells derived from these tumors depend on SMNDC1 both in vitro and in xenograft models.
We here propose to evaluate the potential of our SMNDC1 inhibitors for cancer therapy. Experimentally, we will test these compounds in the ERK1 splicing dependent models in collaboration with the groups that described these findings, and we will profile their antiproliferative effects against a panel of >900 cancer cell lines. In parallel, we will conduct detailed analysis on the chemical scaffolds we discovered and develop a medicinal chemistry proposal to expand the scope of the filed patent application. Additionally, we will commission analyses for an optimal translation pathway of these compounds to the clinic, aiming an ideal positioning for certain cancer subtypes based on market size, competitive situation, clinical needs and trial design opportunities.
Finally, we will develop a plan for the further translation of our discoveries, ideally by foundation of a new spin-off company following successful completion of the ONCO-SPLICE project.

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HORIZON-ERC-POC - HORIZON ERC Proof of Concept Grants

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Call for proposal

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(opens in new window) ERC-2024-POC

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Host institution

CEMM - FORSCHUNGSZENTRUM FUER MOLEKULARE MEDIZIN GMBH
Net EU contribution

Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.

€ 150 000,00
Address
LAZARETTGASSE 14 AKH BT 25.3
1090 Wien
Austria

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Region
Ostösterreich Wien Wien
Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
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Total cost

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Beneficiaries (1)

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