Finding novel compounds as starting points for optimization is a major challenge in drug
discovery research. Fragment-based methods have emerged in the past ten years as an …

There has been considerable interest recently in what is known asfragment-based lead
discovery'. The novel feature of the approach is to begin with small low-affinity compounds …

Fragment-based drug discovery has come a long way in a short period of time and is now
being used throughout the biopharmaceutical industry. Here we review the origin of the …

From its origins as a niche technique more than 15 years ago, fragment-based approaches
have become a major tool for drug and ligand discovery, often yielding results where other …

Fragment-based drug discovery as a source of preliminary hits has become a significant
alternative to conventional drug discovery. A large variety of elegant biophysical validation …

© 2013 Macmillan Publishers Limited. All rights reserved and the nature of the
measurements. Among the many reasons for the discrepancy, only about 5% of a fragment …

Fragment-based drug design (FBDD) has emerged as a mainstream approach for the rapid
and efficient identification of building blocks that can be used to develop high-affinity ligands …

“The whole is more than the sum of its parts” is a phrase that is attributed to the Greek
philosopher Aristotle (384–322 BC), who in his book Metaphysica compared a syllable with …

This review summarizes recent developments in fragment-based drug-discovery methods
with an emphasis on informatics and modeling requirements. Fragment-based methods …

Fragment-based drug design began more than ten years ago and has been steadily gaining
in popularity. This review discusses how fragments have been used to choose druggable …