Compound Screening Platform

We collaborate with researchers at the Center as well as national/international cooperation partners and custom-design screening assays for the identification of novel bioactive molecules.

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We collaborate with researchers at the Center as well as national/international cooperation partners and custom-design screening assays for the identification of novel bioactive molecules. Here, a major focus is devoted to the development of phenotypic assays for high-content-screening (HCS) in order to better reflect the biology of the underlying disease state. We use machine learning techniques to analyze high-content images. We provide state-of-the-art equipment and screening techniques as well as oversee the in-house diversity and focused compound libraries.

Biochemical assays:

Protein-Protein-Interaction (PPI) assays:
- AlphaScreen interaction assay (homogenous assay)
- TR-FRET (HTRF) interaction assay (homogenous assay)
- DELFIA time-resolved fluorescence assay (ELISA based assay)
- Microscale thermophoresis (MST)
- Pull down assays (GST, StrepTagII, His, GFP-Trap, etc.)
Enzymatic assays:
- DUBs (AMC, IQF-diUb, AlphaScreen, etc.)
- Protease cleavage assay (e.g., AMC substrates)
- Kinase assays (AlphaScreen, HTRF, ELISA)
- Phosphatase assays (AlphaScreen, HTRF)
Protein-Compound and Nucleic Acid-Compound Interactions:
- Microscale thermophoresis

Cell-based HCS/HTS assays:

High-Content Screening (HCS) using the Operetta System:
- Stem Cell screening
- 3D cell systems
- Morphology analysis (e.g., neurons)
- Cellular profiling using Cell painting assay
- Cellular substructures (e.g., spots, organelles, etc.)
- Cellular translocation analysis (e.g., between Nucleus and Cytoplasm)
- Protein-Protein Interactions (e.g., BiFC, FRET)
- High-Content Image Analysis with specialized software and Machine Learning/Deep Learning
High-Throughput Screening (HTS):
- Protein-Protein Interactions (NanoBRET)
- Fluorescence-based reporter assays
- Cell viability assays
- Apoptosis assays

Diversity libraries (30,000 bioactive compounds):

ChemDiv subset
- Diversity selection of 10,000 compounds
- Approx. 50% of the compounds have the ability to cross the blood brain barrier (information from calculations)
Enamine subset
- Diversity selection of 10,000 compound
ChemBridge subset
- Diversity selection of 5,000 compounds
ChemDiv Protein-Protein Interaction (PPI) subset
- Diversity selection of 5,000 compounds
- Focus on PPI inhibition

Focussed libraries:

Prestwick FDA approved drugs
Medchem Express FDA approved drugs
Repurposing library
GPCR compound library

Dr. rer. nat. Kamyar Hadian

Deputy Director of the Research Unit Signaling and Translation / Group Leader Cell Signaling and Chemical Biology / Head Compound Screening Platform

Dr. Kenji Schorpp

Postdoc Hadian Lab

Dr. rer. nat. Ina Rothenaigner

Postdoc Hadian Lab

Christian Pütz

Technical Assistant, IT Administrator Hadian Lab

Stefanie Brandner

Technical Assistant Hadian Lab

Mr. Roboto

The Mysterious Machine

Anand Ramani, Giovanni Pasquini, Niklas J. Gerkau, Vaibhav Jadhav, Omkar Suhas Vinchure, Nazlican Altinisik, Hannes Windoffer, Sarah Muller, Ina Rothenaigner, Sean Lin, Aruljothi Mariappan, Dhanasekaran Rathinam, Ali Mirsaidi, Olivier Goureau, Lucia Ricci-Vitiani, Quintino Giorgio D’Alessandris, Bernd Wollnik, Alysson Muotri, Limor Freifeld, Nathalie Jurisch-Yaksi, Roberto Pallini, Christine R. Rose, Volker Busskamp, Elke Gabriel, Kamyar Hadian* & Jay Gopalakrishnan*

Reliability of high-quantity human brain organoids for modeling microcephaly, glioma invasion and drug screening

Tschuck, J. ; Tonnus, W. ; Gavali, S. ; Kolak, A. ; Mallais, M. ; Maremonti, F. ; Sato, M. ; Rothenaigner, I. ; Friedmann Angeli, J.P. ; Pratt, D.A. ; Linkermann, A. ; Hadian, K.*

Seratrodast inhibits ferroptosis by suppressing lipid peroxidation.

Xiaohua Yang MD, Maria_E. Forstner MD, Ina Rothenaigner PhD, Marina Bullo MD, Tugba E. Şismanlar PhD, Ayse T. Aslan PhD, Philipp Latzin MD, Kamyar Hadian PhD*, Matthias Griese MD

Cyclosporine A in children with ABCA3 deficiency

Napolitano V, Dabrowska A, Schorpp K, Mourão A, Barreto-Duran E, Benedyk M, Botwina P, Brandner S, Bostock M, Chykunova Y, Czarna A, Dubin G, Fröhlich T, Hölscher M, Jedrysik M, Matsuda A, Owczarek K, Pachota M, Plettenburg O, Potempa J, Rothenaigner I, Schlauderer F, Slysz K, Szczepanski A, Mohn K G-I, Blomberg B, Sattler S*, Hadian K*, Popowicz G* and Pyrc K*

Acriflavine, a clinically approved drug, inhibits SARS-CoV-2 and other betacoronaviruses

Maria Forstner, Sean Lin, Xiaohua Yang, Susanna Kinting, Ina Rothenaigner, Kenji Schorpp, Yang Li, Kamyar Hadian*, & Matthias Griese*

High-Content Screening Identifies Cyclosporin A as a Novel ABCA3-Specific Molecular Corrector

Rita Costa, Darcy E. Wagner, Ali Doryab, Martina M. De Santis, Kenji Schorpp, Ina Rothenaigner, Mareike Lehmann, Hoeke A. Baarsma, Xueping Liu, Otmar Schmid, Monica Campillos, Ali Önder Yildirim, Kamyar Hadian* & Melanie Königshoff

A drug screen with approved compounds identifies amlexanox as a novel Wnt/β-catenin activator inducing lung epithelial organoid formation

Goetz Hartleben, Kenji Schorpp, Yun Kwon, Barbara Betz, Foivos‐Filippos Tsokanos, Zahra Dantes, Arlett Schäfer, Ina Rothenaigner, José Manuel Monroy Kuhn, Pauline Morigny, Lisa Mehr, Sean Lin, Susanne Seitz, Janina Tokarz, Anna Artati, Jerzy Adamsky, Oliver Plettenburg, Dominik Lutter, Martin Irmler, Johannes Beckers, Maximilian Reichert, Kamyar Hadian*, Anja Zeigerer, Stephan Herzig & Mauricio Berriel Diaz

Combination therapies induce cancer cell death through the integrated stress response and disturbed pyrimidine metabolism

Sean Lin, Kenji Schorpp, Ina Rothenaigner & Kamyar Hadian*

Image-based high-content screening in drug discovery

Adrian Fischer, Tim Koopmans, Pushkar Ramesh, Simon Christ, Maximilian Strunz, Juliane Wannemacher, Michaela Aichler, Annette Feuchtinger, Axel Walch, Meshal Ansari, Fabian J. Theis, Kenji Schorpp, Kamyar Hadian, Philipp-Alexander Neumann, Herbert B. Schiller & Yuval Rinkevich

Post-surgical adhesions are triggered by calcium-dependent membrane bridges between mesothelial surfaces

Aruljothi Mariappan, Komal Soni, Kenji Schorpp, Fan Zhao, Amin Minakar, Xiangdong Zheng, Sunit Mandad, Iris Macheleidt, Anand Ramani, Tomáš Kubelka, Maciej Dawidowski, Kristina Golfmann, Arpit Wason, Chunhua Yang, Judith Simons, Hans‐Günther Schmalz, Anthony A Hyman, Ritu Aneja, Roland Ullrich, Henning Urlaub, Margarete Odenthal, Reinhardt Büttner, Haitao Li, Michael Sattler, Kamyar Hadian* & Jay Gopalakrishnan

Inhibition of CPAP–tubulin interaction prevents proliferation of centrosome‐amplified cancer cells

Jara K. Brenke, Grzegorz M. Popowicz, Kenji Schorpp, Ina Rothenaigner, Manfred Roesner,
Isabel Meininger, Cédric Kalinski, Larissa Ringelstetter, Omar R'kyek, Gerrit Jürjens, Michelle Vincendeau, Oliver Plettenburg, Michael Sattler, Daniel Krappmann & Kamyar Hadian*

Targeting TRAF6 E3 ligase activity with a small-molecule inhibitor combats autoimmunity

M. Dawidowski*, L. Emmanouilidis*, V. C. Kalel*, K. Tripsianes*, K. Schorpp*, K. Hadian*, M. Kaiser, P. Mäser, M. Kolonko, S. Tanghe, A. Rodriguez, W. Schliebs, R. Erdmann, M. Sattler & G. M. Popowicz

Inhibitors of PEX14 disrupt protein import into glycosomes and kill Trypanosoma parasites

Kenji Schorpp , Ina Rothenaigner, Elena Salmina, Jeanette Reinshagen, Terence Low, Jara K. Brenke, Jay Gopalakrishnan, Igor V. Tetko, Sheraz Gul & Kamyar Hadian*

Identification of Small-Molecule Frequent Hitters from AlphaScreen High-Throughput Screens

Daniel Nagel, Stefani Spranger, Michelle Vincendeau, Michael Grau, Silke Raffegerst, Bernhard Kloo, Daniela Hlahla, Martin Neuenschwander, Jens Peter von Kries, Kamyar Hadian*, Bernd Dörken, Peter Lenz, Georg Lenz, Dolores J. Schendel & Daniel Krappmann

Pharmacological inhibition of the MALT1 protease by phenothiazines as a therapeutic approach for the treatment of aggressive ABC-DLBCL

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