Fraunhofer Institute for Translational Medicine and Pharmacology ITMP
Fraunhofer Institute for Translational Medicine and Pharmacology ITMP

© Fraunhofer ITMP | Bernd Müller

Drug Screening & Compound Repurposing

For Drug Screening & Compound Repurposing, we offer a comprehensive High-Throughput Screening, Hit validation and profiling capability, supported by a bioinformatics and IT infrastructure to aid rapid data processing and decision making. The primary focus of our work is the development of biologically relevant and screening compatible assays in the most common microtiter plate formats for use in biomedical research, chemical biology and drug discovery. These assays encompass the major protein target classes with readouts in all optical, label-free and High Content imaging technologies and can be operated making use of our fully integrated robotic screening platform. There are several small molecule screening libraries available, which include collections of up to 200,000 diverse compounds as well as target class focused, natural product and drug repurposing sets including approved drugs that have reached clinical use across 600 indications and pre-clinical compounds of varying degrees of validation, supported by a curated database. The selection of compounds for Hit to Lead progression takes place following mechanism-of-action, selectivity and ADMET studies aided by bioinformatics support.

 

Core competencies:

  • State of the art tools and technologies for developing innovative assays
  • Assay readout technologies include optical, label-free and high content imaging
  • Access to a variety of small molecule compound libraries
  • Triaging of compounds using mechanism-of-action, selectivity and ADMET profiling
  • Delivery of high-quality compounds as starting points for drug discovery
  • Expertise in progressing compounds to industry standard Lead and Candidate milestones
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Best practice in in assay development and screening

Expertise in developing of a broad range of assays, from biochemical assays to phenotypic or highly complex cell-based assays that make use of primary cells and induced pluripotent stem cells.

Access to compound libraries

Availability of compound libraries to address all chemical biology, drug discovery and drug repurposing projects. Information relating to the compounds can be shared with partners in order to allow selection of customized sets of compounds.

Provision of automated screening infrastructure

Most assays are developed in microtiter plate formats so they can be rapidly screened against our compound libraries. The screening activities take place using a state-of-the-art automated screening system with integrated liquid handling and reader devices. All raw data is accessed remotely and processed rapidly to identify active compounds for progression in the respective project value chain.

Development of critical paths for chemical biology and drug discovery projects

Our personnel have diverse backgrounds having been employed in academia, biotech and the pharmaceutical industry. They have the experience and track-record of developing critical paths that enable project progression to industry standards. A major focus is ensuring projects assets can be packaged for further progression.

REMEDi4ALL

REMEDi4ALL is dedicated to building and managing a comprehensive and accessible value chain that covers all aspects of drug repurposing, including scientific, methodological, financial, legal, regulatory, and intellectual property. By collaborating closely with research funders and the patient community, REMEDi4ALL aims to support a wide range of user projects and secure ongoing investments to become a sustainable entity. As a community of practice, REMEDi4ALL brings together all necessary infrastructure, expertise, and stakeholders involved in drug repurposing. The platform focuses on patient-centric research and development, offers extensive education and training, and works to establish consensus-driven policy positioning.

Additional Information

PROXIDRUGS

Funded through the Clusters4Future initiative, the PROXIDRUGS focuses particularly on developing new therapies for diseases with a high unmet medical need by utilizing the innovative concept of targeted protein degradation. Proximity-induced drugs can specifically trigger the degradation of disease-relevant proteins by directing them to the cellular recycling system, opening new therapeutic avenues for a broad spectrum of diseases. It is anticipated that 80% of proteins previously considered non-druggable could be targeted with this strategy. PROXIDRUGS aims to enhance this new class of drugs in several ways: The strategy includes identifying suitable functional subunits for molecular engineering, targeted optimization of pharmacological properties, and progression to clinical trials. To this end, the cluster connects partners from academia and industry, covering the entire value chain from basic to translational research. Academic partners include Goethe University Frankfurt, TU Darmstadt, University of Heidelberg, the Max Planck Institute for Biophysics, and the Fraunhofer Institute for Translational Medicine and Pharmacology. These institutions work closely with major pharmaceutical partners, namely AbbVie Germany, Merck Healthcare, and GlaxoSmithKline, along with Revvity as an associated partner.

Additional Information

canSERV

© https://www.canserv.eu/

Funded through the EU Horizon Europe programme, canSERV provides cutting edge, interdisciplinary and customised oncology services. It offers a comprehensive portfolio of oncology-related research services available to all scientists in EU member countries, associated countries and beyond. The ITMP is offering experimental services related to high-content image-based profiling of compounds and high-throughput microscopy services and generation and validation of in-vitro disease models and training services for cancer drug discovery – from target identification to drug approval and exploring high throughput biochemical and cellular assays in cancer drug discovery. These services are currently being adopted by partners at the University of Veterinary Medicine Vienna (Austria) and University of Florence (Italy), in particular assay development and screening of focussed compound libraries. It is anticiapted that the output will include understanding of disease biology and novel anti-cancer compounds.

Additional Information

Weng J, Ju F, Lyu Z, Fan N, Smit DJ, Xu W, Wu X, Becker P, Xu Y, Schweiger MR, Hillmer AM, Harwig R, Gul S, Link A, Meder L, Fang N, Dong Q, Bruns CJ, Ren N, Zhao Y.
Single-cell insights into tumor microenvironment heterogeneity and plasticity: transforming precision therapy in gastrointestinal cancers.
J Exp Clin Cancer Res. 2025 Nov 28;44(1):314 
doi: 10.1186/s13046-025-03567-5

Haupt J, Keminer O, Neser C, Windshügel B, Wiltzsch V, Schmidt JR, Pliushcheuskaya P, Künze G, Scholz U, Müller C, Oliveira da Rocha GH, Biermann MK, Zdzieblo D, Metzger M, Schiefke I, Neurath MF, Siegmund B, Claussen C, Köhl U, Geisslinger G, Buchholz M, Kalkhof S, Lehmann J.
Novel aryl hydrocarbon receptor agonists as potential anti-inflammatory therapeutics: Identification and validation through drug repurposing. Biochem Pharmacol. 2025 Oct;240:117066
doi: 10.1016/j.bcp.2025.117066

Carotenuto L, Keminer O, Carleo G, Zaliani A, Leo A, Citraro R, De Sarro G, Dirkx N, Kaji M, Weckhuysen S, Reinshagen J, Barrese V, Guida N, Ostacolo C, Miceli F, Gribbon P, Taglialatela M.
The fast-dissociating D2 antagonist antipsychotic JNJ-37822681 is a neuronal Kv7 channel opener: Potential repurposing for epilepsy treatment.
Br J Pharmacol. 2025 Nov;182(22):5574-5595
doi: 10.1111/bph.70119

Borsari C, Santarem N, Coertzen D, Mazzolari A, Corfu AI, Coelho C, Barbosa F, Tamborini L, Birkholtz LM, Raffellini L, Keminer O, Basilico N, Parapini S, Gul S, Cordeiro-da-Silva A, Conti P.
From pan-active to parasite-selective antiparasitic agents: A scaffold hopping approach.
Eur J Med Chem. 2025 Dec 15;300:118095
doi: 10.1016/j.ejmech.2025.118095

Gorgogietas V, Weiss A, Cousin L, Hoffmann D, Schmitt K, Ogier A, Barbuti PA, Santos BFR, Boussaad I, Wittich A, Zaliani A, Pless O, Krüger R, Sommer P, Wilbertz JH.
Morphological profiling reveals neuroprotection via mitochondrial uncoupling in human dopaminergic neurons.
Sci Rep. 2025 Aug 12;15(1):29507
doi: 10.1038/s41598-025-14735-0. 

Huchting J, Weller A, Schweizer M, Brandt M, Heering J, Kuzikov M, Wolf M, Reinshagen J, Queisser MA, Gribbon P, Zaliani A, Pless O, Kannt A.
Optimization and Evaluation of Complementary Degrader Discovery Assays for Application in Screening.
ACS Pharmacol Transl Sci. 2025 Jul 20;8(8):2600-2611
doi: 10.1021/acsptsci.5c00195.

Okinaka Y, Suda Y, Matsumoto T, Kuroda R, Shinagawa Y, Gul S, Claussen C, Matsui I, Matsui Y, Taguchi A. Changes in metabolism-related RNA expression in circulating white blood cells of aged individual with physical frailty.
Aging (Albany NY). 2025 May 28;17(5):1206-1220
doi: 10.18632/aging.206256

Chatziefthymiou SD, Kuzikov M, Afandi S, Kovacs G, Srivastava S, Zaliani A, Gruzinov A, Pompidor G, Lunelli M, Ahmed GR, Labahn J, Hakanpää J, Windshügel B, Kolbe M.
Identification, validation, and characterization of approved and investigational drugs interfering with the SARS-CoV-2 endoribonuclease Nsp15.
Protein Sci. 2025 Jun;34(6):e70156.
doi: 10.1002/pro.70156

Castillo-Aguilera OO, Depreux P, Halby L, Bailly C, Domínguez-Ramírez L, Gul S, Arimondo PB, Goossens L. Design, synthesis and evaluation of pyrimidinobenzylamide and pyrimidinothiophenamide derivatives as inhibitors of DOT1L and related epigenetic targets DNMT3a, PRMT4 and other HMTs.
RSC Med Chem. 2025 Jan 30;16(5):2159-2173
doi: 10.1039/d4md00899e

Panecka-Hofman J, Linciano P, Pöhner I, Dyguda-Kazimierowicz E, Jedwabny W, Landi G, Santarem N, Witt G, Ellinger B, Kuzikov M, Luciani R, Ferrari S, Aiello D, Mangani S, Pozzi C, Cordeiro-da-Silva A, Gul S, Costi MP, Wade RC. Design of 2-Aminobenzothiazole Derivatives Targeting Trypanosomatid PTR1 by a Multidisciplinary Fragment Hybridization Approach.
J Med Chem. 2025 Oct 9;68(19):20595-20618
doi: 10.1021/acs.jmedchem.5c01799

Kuzikov M, Reinshagen J, Wycisk K, Corona A, Esposito F, Malune P, Manelfi C, Iaconis D, Beccari A, Tramontano E, Nowotny M, Windshügel B, Gribbon P, Zaliani A.
Drug repurposing screen to identify inhibitors of the RNA polymerase (nsp12) and helicase (nsp13) from SARS-CoV-2 replication and transcription complex.
Virus Res. 2024 May;343:199356
doi: 10.1016/j.virusres.2024.199356

Jalencas X, Berg H, Espeland LO, Sreeramulu S, Kinnen F, Richter C, Georgiou C, Yadrykhinsky V, Specker E, Jaudzems K, Miletić T, Harmel R, Gribbon P, Schwalbe H, Brenk R, Jirgensons A, Zaliani A, Mestres J.
Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection.
RSC Med Chem. 2024 Feb 12;15(4):1176-1188
doi: 10.1039/d3md00724c