Piece by piece
Various biotechnology companies have adopted fragment-based lead discovery (FBLD) as an efficient and emerging drug discovery strategy. Fragment libraries are designed with various clustering techniques and selecting fragments that are chemically diverse and excluding compounds with known reactive or toxic groups. Medicinal chemists make use of the opportunity to grow an FBLD compound by starting with an initial fragment hit and adding chemistry that avoids intellectual property issues. X-ray crystallography screening has become more predominant that NMR in industry for FBLD screening as more companies are better set up for medium-throughput X-ray crystallography than medium throughput NMR. Some biotechnical research groups are building upon existing FBLD protocols to create new sophisticated screening strategies, including attaching paramagnetic moieties near the active site of the biological target.
Everts, S. (2008). Piece by piece.