Amaury E. Fernández‐Montalván

A high throughput screening platform for label-free identification and characterization of GPCR ligands using impedance-based real-time cellular analysis

Frederik Bangnowski, Robert Ries, Michael Karnath, Amaury E. Fernández‐Montalván et autres

Real-time cell analysis (RTCA) is a biosensor technology that enables kinetic monitoring of cellular activities via electrical impedance. Among its multiple applications, this label-free method offers a holistic approach to monitoring the activity of G protein-coupled receptors (GPCRs) by capturing integrated cellular …

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Protein–ligand data at scale to support machine learning

A.M. Edwards, Dafydd R. Owen, Leili Zhang, Damian W. Young et autres

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Inhibition of EphB4 Receptor Signaling by Ephrin-B2-Competitive and Non-Competitive DARPins Prevents Angiogenesis

Weronika Trun, Amaury E. Fernández‐Montalván, Yong-Jiang Cao, Bernard Haendler et autres

The receptor tyrosine kinase EphB4 is involved in tumor angiogenesis, proliferation, and metastasis. Designed ankyrin repeat proteins (DARPins) binding to the EphB4 extracellular domain were identified from a combinatorial library using phage display. Surface plasmon resonance (SPR) allowed us to distinguish between …

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Discovery and Characterization of BAY-184: A New Potent and Selective Acylsulfonamide-Benzofuran In Vivo-Active KAT6AB Inhibitor

Antonius ter Laak, Roman Christian Hillig, Steven J. Ferrara, Daniel Korr et autres

High Resolution Image Download MS PowerPoint Slide KAT6A and KAT6B genes are two closely related lysine acetyltransferases that transfer an acetyl group from acetyl coenzyme A (AcCoA) to lysine residues of target histone substrates, hence playing a key role in chromatin regulation. …

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A miniaturized mode-of-action profiling platform enables high throughput characterization of the molecular and cellular dynamics of EZH2 inhibition

Lilia Falkenstern, Victoria Georgi, Stefanie Bunse, Volker Badock et autres

The market approval of Tazemetostat (TAZVERIK) for the treatment of follicular lymphoma and epithelioid sarcoma has established "enhancer of zeste homolog 2" (EZH2) as therapeutic target in oncology. Despite their structural similarities and common mode of inhibition, Tazemetostat and other EZH2 inhibitors …

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Dual targeting of the androgen receptor and PI3K / AKT / mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis

Tatsuo Sugawara, Ekaterina Nevedomskaya, Simon R. Heller, Annika Böhme et autres

Prostate cancer is a frequent malignancy in older men and has a very high 5-year survival rate if diagnosed early. The prognosis is much less promising if the tumor has already spread outside the prostate gland. Targeted treatments mainly aim at blocking …

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Author response for "Dual targeting of the androgen receptor and PI3K / AKT / mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis"

Tatsuo Sugawara, Ekaterina Nevedomskaya, Simon R. Heller, Annika Böhme et autres

Author response for "Dual targeting of the androgen receptor and PI3K / AKT / mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis"

Tatsuo Sugawara, Ekaterina Nevedomskaya, Simon R. Heller, Annika Böhme et autres

Label-free high-throughput screening via acoustic ejection mass spectrometry put into practice

Martin Winter, Roman P. Simon, Tim T. Häbe, Robert J. Ries et autres

Acoustic droplet ejection-open port interface-mass spectrometry (ADE-OPI-MS) is a novel label-free analytical technique, promising to become a versatile readout for high-throughput screening (HTS) applications. The recent introduction of ADE-OPI-MS devices to the laboratory equipment market, paired with their compatibility with laboratory automation …

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Figure S2 from Inhibition of BUB1 Kinase by BAY 1816032 Sensitizes Tumor Cells toward Taxanes, ATR, and PARP Inhibitors In Vitro and In Vivo

Gerhard Siemeister, Anne Mengel, Amaury E. Fernández‐Montalván, Wilhelm Bone et autres

Cellular assays

Supplementary Table S5 from Inhibition of BUB1 Kinase by BAY 1816032 Sensitizes Tumor Cells toward Taxanes, ATR, and PARP Inhibitors In Vitro and In Vivo

Gerhard Siemeister, Anne Mengel, Amaury E. Fernández‐Montalván, Wilhelm Bone et autres

Exposure data from xenograft studies

Supplementary Table S2 from Inhibition of BUB1 Kinase by BAY 1816032 Sensitizes Tumor Cells toward Taxanes, ATR, and PARP Inhibitors In Vitro and In Vivo

Gerhard Siemeister, Anne Mengel, Amaury E. Fernández‐Montalván, Wilhelm Bone et autres

Anti-proliferative cell line profile of BAY 1816032