Transforming fragments into candidates: small becomes big in medicinal chemistry
2009; Elsevier BV; Volume: 14; Issue: 13-14 Linguagem: Inglês
10.1016/j.drudis.2009.03.009
ISSN1878-5832
AutoresGerdien E. de Kloe, David Bailey, Rob Leurs, Iwan J. P. de Esch,
Tópico(s)Chemical Synthesis and Analysis
ResumoFragment-based drug discovery (FBDD) represents a logical and efficient approach to lead discovery and optimisation. It can draw on structural, biophysical and biochemical data, incorporating a wide range of inputs, from precise mode-of-binding information on specific fragments to wider ranging pharmacophoric screening surveys using traditional HTS approaches. It is truly an enabling technology for the imaginative medicinal chemist. In this review, we analyse a representative set of 23 published FBDD studies that describe how low molecular weight fragments are being identified and efficiently transformed into higher molecular weight drug candidates. FBDD is now becoming warmly endorsed by industry as well as academia and the focus on small interacting molecules is making a big scientific impact.
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