Fragment-based approaches in drug discovery and chemical biology
DE Scott, AG Coyne, SA Hudson, C Abell - Biochemistry, 2012 - ACS Publications
Fragment-based approaches to finding novel small molecules that bind to proteins are now
firmly established in drug discovery and chemical biology. Initially developed primarily in a …
firmly established in drug discovery and chemical biology. Initially developed primarily in a …
How well can fragments explore accessed chemical space? A case study from heat shock protein 90: miniperspective
SD Roughley, RE Hubbard - Journal of medicinal chemistry, 2011 - ACS Publications
1.1. Fragments. The central idea in fragment-based discovery is that screening a target
against a small number (as few as 500 compounds) of low molecular weight compounds …
against a small number (as few as 500 compounds) of low molecular weight compounds …
The SeeDs approach: integrating fragments into drug discovery
RE Hubbard, B Davis, I Chen… - Current Topics in …, 2007 - ingentaconnect.com
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 …
discovery research. Fragment-based methods have emerged in the past ten years as an …
Drugging challenging targets using fragment-based approaches
AG Coyne, DE Scott, C Abell - Current opinion in chemical biology, 2010 - Elsevier
Fragment-based approaches have now become firmly established in the drug discovery
armoury. After notable early successes against protein kinases, the versatility and power of …
armoury. After notable early successes against protein kinases, the versatility and power of …
Recent developments in fragment-based drug discovery
M Congreve, G Chessari, D Tisi… - Journal of medicinal …, 2008 - ACS Publications
The field of fragment-based drug discovery (FBDDa) has developed significantly over the
past 10 years and is now recognized as a tangible alternative to more traditional methods of …
past 10 years and is now recognized as a tangible alternative to more traditional methods of …
Fragment-based screening by protein crystallography: successes and pitfalls
Z Chilingaryan, Z Yin, AJ Oakley - International journal of molecular …, 2012 - mdpi.com
Fragment-based drug discovery (FBDD) concerns the screening of low-molecular weight
compounds against macromolecular targets of clinical relevance. These compounds act as …
compounds against macromolecular targets of clinical relevance. These compounds act as …
Fragment based drug design: from experimental to computational approaches
Fragment based drug design has emerged as an effective alternative to high throughput
screening for the identification of lead compounds in drug discovery in the past fifteen years …
screening for the identification of lead compounds in drug discovery in the past fifteen years …
Fragment hits: what do they look like and how do they bind?
F Giordanetto, C Jin, L Willmore, M Feher… - Journal of medicinal …, 2019 - ACS Publications
A “fragment hit”, a molecule of low molecular weight that has been validated to bind to a
target protein, can be an effective chemical starting point for a drug discovery project. Our …
target protein, can be an effective chemical starting point for a drug discovery project. Our …
Six biophysical screening methods miss a large proportion of crystallographically discovered fragment hits: a case study
J Schiebel, N Radeva, SG Krimmer, X Wang… - ACS chemical …, 2016 - ACS Publications
Fragment-based lead discovery (FBLD) has become a pillar in drug development. Typical
applications of this method comprise at least two biophysical screens as prefilter and a …
applications of this method comprise at least two biophysical screens as prefilter and a …
Application of fragment-based drug discovery to versatile targets
Q Li - Frontiers in molecular biosciences, 2020 - frontiersin.org
Fragment-based drug discovery (FBDD) is a powerful method to develop potent small-
molecule compounds starting from fragments binding weakly to targets. As FBDD exhibits …
molecule compounds starting from fragments binding weakly to targets. As FBDD exhibits …