Abstract

Abstract Over the past two decades, an increasing number of small molecule drugs that target unique molecular changes underlying a specific cancer have been approved, and small molecule drugs represent a major therapeutic class for cancer treatment. Chemical ‘probes’ are also indispensable tools to advance our understanding of pathologies at the molecular and cellular level and to validate novel drug targets. A major bottleneck in identifying and developing these chemical compounds in academia is often access to robust disease-relevant assays, high-throughput screening platforms, comprehensive screening libraries, medicinal expertise for the hit-to-lead optimization. In order to democratize access to these resources for a broader scientific community, the publicly funded EU-OPENSCREEN (www.eu-openscreen.eu) initiative has been established with the aim to accelerate drug discovery efforts in an open-access setting in collaboration with researchers from academia and industry. EU-OPENSCREEN’s 30 expert centers offer access to their cancer target-based and phenotypic drug screening expertise, capabilities in developing disease-relevant assays and hit-to-lead optimization capabilities. The identified bioactive ‘hit’ compounds will be progressed into high-quality chemical starting points to be further developed into drug leads or chemical probes for the elucidation of mechanisms of cancer onset, progression, resistance and effects of drug therapy. All generated tool compounds and associated bioactivity data are made available to the global scientific community. Here we will present an overview of anti-cancer drug discovery projects of EU-OPENSCREEN and explain the opportunities and benefits for other international scientists to collaboratively develop novel anti-cancer drug leads and chemical probes. EU-OPENSCREEN receives funding from the European Union's Horizon 2020 and Horizon Europe research and innovation programs under grant agreements No 654248 and 101058620. Citation Format: Bahne Stechmann, Charlotte Wit. EU-OPENSCREEN - An open-access initiative in chemical biology to support anti-cancer drug discovery. [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2023; Part 1 (Regular and Invited Abstracts); 2023 Apr 14-19; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2023;83(7_Suppl):Abstract nr 5319.

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