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The Nature of Nanodisc Lipids Influences Fragment‐Based Drug Discovery Results

Chemical Biology and Drug Design

Fragment-based drug discovery (FBDD) was applied to cytochrome P450 3A4 reconstituted in Nanodiscs (NDs) with various lipid compositions. The choice of ND lipid influenced drug membrane interactions and fragment hit rates, demonstrating the critical role of the membrane environment in fragment screening for membrane proteins.

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Advancements in hit identification for membrane protein drug discovery

Drug Target Review

2 Considering 2530 percent of marketed drugs work by binding to GPCRs, 3 it is vital that these challenges are overcome through innovation and research. Fragment-based screening (FBS) has emerged as a powerful tool for discovering novel lead compounds, especially for challenging targets like the Adenosine A2a receptor.

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Target-directed cancer: protein-ligand interactions  

Drug Target Review

Could you provide an overview of your research on target directed cancer drug discovery, particularly your focus on protein lagging interactions. I work in the Centre for Cancer Drug Discovery (CCDD) at The Institute of Cancer Research in London, which is an academic drug discovery centre. Acta Cryst. Acta Cryst. 2013) 56, 2059-2073.

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High Throughput Screening (HTS)

Sygnature Discovery

Sygnature Discovery offers high throughput screening along with additional hit identification tools including virtual screening, knowledge-based design, and fragment screening. Utilising Titian Mosaic SampleBank software, linked with our HighRes automated system, we streamline the ordering of assay plates.

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SARS-CoV-2 Protease Inhibitors: An Attractive Approach for Treating COVID-19

PerkinElmer

Researchers are now studying the potential of protease inhibitors for the treatment of SARS-CoV-2. 2 In the present study, the researchers report that PF-07321332 demonstrated potent inhibition in FRET M pro assays representing M pro from all coronavirus types known to infect humans.

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Sygnature Discovery acquires Peak Proteins

Sygnature Discovery

Peak Proteins will continue to operate out of their new research facility in Macclesfield, near Sygnature’s Alderley Edge site. Their world-class expertise in protein crystallography will enhance our fragment screening and analysis activities, as well as our structure-based drug design work.”

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Covalent Modifiers - Untitled Article

Covalent Modifiers

Kjersti Julin, Franco Faucher, Marijn Hollander, Nichole Pedowitz, Daniel Abegg, Isabella Hammond, Ifeanyichukwu Eke, Sijie Wang, Shiyu Chen, John Bennett, Jeyun Jo, Christian Lentz, Alex Adibekian, Matthias Fellner Research Square Preprint 2025 [link] 10.21203/rs.3.rs-5494070/v1