Johan G. Hollander

Identification of novel small molecule inhibitors of ETS transcription factors

Zary Forghany, Jin Ma, Johan G. Hollander, Ruta Nachane et autres

The evolutionarily conserved E-Twenty-Six (ETS) family of transcription factors acts downstream of major signal transduction pathways and plays a pivotal role in tissue development and maintenance. Importantly, their function is frequently corrupted in a substantial proportion of tumour types, and they are …

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Author response for "Identification of novel small molecule inhibitors of ETS transcription factors"

Zary Forghany, Jin Ma, Johan G. Hollander, Ruta Nachane et autres

Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography

Christopher R. Smith, Dan Chen, James G. Christensen, René Coulombe et autres

SOS1 and SOS2 are guanine nucleotide exchange factors that mediate RTK-stimulated RAS activation. Selective SOS1:KRAS PPI inhibitors are currently under clinical investigation, whereas there are no reports to date of SOS2:KRAS PPI inhibitors. SOS2 activity is implicated in MAPK rebound when divergent …

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NMR in target driven drug discovery: why not?

Sébastien Keiffer, Marta G. Carneiro, Johan G. Hollander, Masakazu Kobayashi et autres

No matter the source of compounds, drug discovery campaigns focused directly on the target are entirely dependent on a consistent stream of reliable data that reports on how a putative ligand interacts with the protein of interest. The data will derive from …

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Interrogating the Essential Bacterial Cell Division Protein FtsQ with Fragments Using Target Immobilized NMR Screening (TINS)

Marjolein Glas, Eiso AB, Johan G. Hollander, Gregg Siegal et autres

The divisome is a large protein complex that regulates bacterial cell division and therefore represents an attractive target for novel antibacterial drugs. In this study, we report on the ligandability of FtsQ, which is considered a key component of the divisome. For …

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Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain

A. Chaikuad, Steffen Lang, Paul E. Brennan, Claudia Temperini et autres

The P300/CBP-associated factor plays a central role in retroviral infection and cancer development, and the C-terminal bromodomain provides an opportunity for selective targeting. Here, we report several new classes of acetyl-lysine mimetic ligands ranging from mM to low micromolar affinity that were …

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Increasing Chemical Space Coverage by Combining Empirical and Computational Fragment Screens

Sarah Barelier, O. Eidam, Inbar Fish, Johan G. Hollander et autres

Most libraries for fragment-based drug discovery are restricted to 1,000-10,000 compounds, but over 500,000 fragments are commercially available and potentially accessible by virtual screening. Whether this larger set would increase chemotype coverage, and whether a computational screen can pragmatically prioritize them, is …

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Target Immobilization as a Strategy for NMR-Based Fragment Screening: Comparison of TINS, STD, and SPR for Fragment Hit Identification

Masakazu Kobayashi, Kim Retra, Francis Figaroa, Johan G. Hollander et autres

Fragment-based drug discovery (FBDD) has become a widely accepted tool that is complementary to high-throughput screening (HTS) in developing small-molecule inhibitors of pharmaceutical targets. Because a fragment campaign can only be as successful as the hit matter found, it is critical that …

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Target Immobilization and NMR Screening of Fragments in Early Drug Discovery

Gregg Siegal, Johan G. Hollander

Using localized NMR spectroscopy on immobilized targets provides us with a method to simultaneously assess binding of small molecules to two different samples. This Target Immobilized NMR Screening (TINS) has a number of advantages, not least is the requirement for minimal quantities …

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A solid-state NMR study of changes in lipid phase induced by membrane-fusogenic LV-peptides

Prashant Agrawal, Suzanne Kiihne, Johan G. Hollander, Mathias W. Hofmann et autres

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13C and 15N NMR evidence for peripheral intercalation of uniformly labeled fusogenic peptides incorporated in a biomimetic membrane

Prashant Agrawal, Suzanne Kiihne, Johan G. Hollander, Dieter Langosch et autres

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Solid State NMR Investigation of the Interaction between Biomimetic Lipid Bilayers and de novo Designed Fusogenic Peptides

Prashant Agrawal, Suzanne Kiihne, Johan G. Hollander, Frans B. Hulsbergen et autres

Learning curve. We have studied the interaction of two de novo designed hydrophobic peptides with a biomimetic three-lipid mixture and pure POPC bilayer by using 31P solid-state NMR spectroscopy. The observed peptide-induced phase changes correlated with the fusogenic behaviour of the peptides …

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