Title:
PLATFORM USING DNA-ENCODED SMALL MOLECULE LIBRARIES AND RNA SELECTION TO DESIGN SMALL MOLECULES THAT TARGET RNA
Document Type and Number:
WIPO Patent Application WO/2023/108090
Kind Code:
A3
Abstract:
A dual screen technique using DEL and 2DCS screens with libraries of synthesized small molecules and synthesized RNA structures (4,096 targets) delivers bona fide ligand-RNA 3D fold target pairs. One of the newly discovered ligands bound a 5'GAG/3'CCC internal loop that is present in pri-miR-27a, the oncogenic precursor of microRNA-27a. The DEL-derived pri-miR-27a ligand is cell-active, potently and selectively inhibits pri-miR-27a processing to reprogram gene expression and halt an otherwise invasive phenotype in triple-negative breast cancer cells.
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Inventors:
DISNEY MATTHEW (US)
PAEGEL BRIAN (US)
PAEGEL BRIAN (US)
Application Number:
PCT/US2022/081215
Publication Date:
July 27, 2023
Filing Date:
December 08, 2022
Export Citation:
Assignee:
UNIV FLORIDA (US)
International Classes:
G16B15/00; G01N33/53; G16B30/00; G16B30/10; A61K38/06
Foreign References:
| US20200324287A1 | 2020-10-15 | |||
| US20200385709A1 | 2020-12-10 | |||
| US20190156912A1 | 2019-05-23 |
Other References:
KUNIG VERENA ET AL: "DNA-encoded libraries – an efficient small molecule discovery technology for the biomedical sciences", BIOLOGICAL CHEMISTRY, WALTER DE GRUYTER GMBH & CO., BERLIN, DE, vol. 399, no. 7, 1 July 2018 (2018-07-01), BERLIN, DE , pages 691 - 710, XP093081303, ISSN: 1431-6730, DOI: 10.1515/hsz-2018-0119
BENHAMOU RAPHAEL I. ET AL: "DNA-encoded library versus RNA-encoded library selection enables design of an oncogenic noncoding RNA inhibitor", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, NATIONAL ACADEMY OF SCIENCES, vol. 119, no. 6, 8 February 2022 (2022-02-08), pages 1 - 8, XP093081306, ISSN: 0027-8424, DOI: 10.1073/pnas.2114971119
BENHAMOU RAPHAEL I. ET AL: "DNA-encoded library versus RNA-encoded library selection enables design of an oncogenic noncoding RNA inhibitor", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, NATIONAL ACADEMY OF SCIENCES, vol. 119, no. 6, 8 February 2022 (2022-02-08), pages 1 - 8, XP093081306, ISSN: 0027-8424, DOI: 10.1073/pnas.2114971119
Attorney, Agent or Firm:
HSI, Jeffrey, D. et al. (US)
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