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Ligand efficiency as a guide in fragment hit selection and optimization

✍ Scribed by Sabine Schultes; Chris de Graaf; Eric E.J. Haaksma; Iwan J.P. de Esch; Rob Leurs; Oliver Krämer

Book ID
119226466
Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
169 KB
Volume
7
Category
Article
ISSN
1740-6749

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✍ Daniel Blasi; Gemma Arsequell; Gregori Valencia; Joan Nieto; Antoni Planas; Mart 📂 Article 📅 2011 🏛 Wiley (John Wiley & Sons) 🌐 English ⚖ 721 KB

## Abstract We have previously reported the design and synthesis of ligands that stabilize Transthyretin protein (TTR) in order to obtain therapeutically active compounds for Familial Amyloid Polyneuropathy (FAP). We are hereby reporting a drug design strategy to optimize these ligands and map them