Challenges and advances in computational docking: 2009 in review

Docking is a computational technique that places a small molecule (ligand) in the binding site of its macromolecular target (receptor) and estimates its binding affinity. This review addresses methodological developments that have occurred in the docking field in 2009, with a particular focus on the...

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Main Authors: Yuriev, E., Agostino, Mark, Ramsland, P.
Format: Journal Article
Published: John Wiley & Sons Ltd. 2011
Subjects:
Online Access:http://hdl.handle.net/20.500.11937/35703
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author Yuriev, E.
Agostino, Mark
Ramsland, P.
author_facet Yuriev, E.
Agostino, Mark
Ramsland, P.
author_sort Yuriev, E.
building Curtin Institutional Repository
collection Online Access
description Docking is a computational technique that places a small molecule (ligand) in the binding site of its macromolecular target (receptor) and estimates its binding affinity. This review addresses methodological developments that have occurred in the docking field in 2009, with a particular focus on the more difficult, and sometimes controversial, aspects of this promising computational discipline. These developments aim to address the main challenges of docking: receptor representation (such aspects as structural waters, side chain protonation, and, most of all, flexibility (from side chain rotation to domain movement)), ligand representation (protonation, tautomerism and stereoisomerism, and the effect of input conformation), as well as accounting for solvation and entropy of binding. This review is strongly focused on docking advances in the context of drug design, specifically in virtual screening and fragment-based drug design.
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publishDate 2011
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spelling curtin-20.500.11937-357032017-09-13T15:32:01Z Challenges and advances in computational docking: 2009 in review Yuriev, E. Agostino, Mark Ramsland, P. receptor flexibility computational docking binding mode prediction protein-ligand complexes scoring Docking is a computational technique that places a small molecule (ligand) in the binding site of its macromolecular target (receptor) and estimates its binding affinity. This review addresses methodological developments that have occurred in the docking field in 2009, with a particular focus on the more difficult, and sometimes controversial, aspects of this promising computational discipline. These developments aim to address the main challenges of docking: receptor representation (such aspects as structural waters, side chain protonation, and, most of all, flexibility (from side chain rotation to domain movement)), ligand representation (protonation, tautomerism and stereoisomerism, and the effect of input conformation), as well as accounting for solvation and entropy of binding. This review is strongly focused on docking advances in the context of drug design, specifically in virtual screening and fragment-based drug design. 2011 Journal Article http://hdl.handle.net/20.500.11937/35703 10.1002/jmr.1077 John Wiley & Sons Ltd. restricted
spellingShingle receptor flexibility
computational docking
binding mode prediction
protein-ligand complexes
scoring
Yuriev, E.
Agostino, Mark
Ramsland, P.
Challenges and advances in computational docking: 2009 in review
title Challenges and advances in computational docking: 2009 in review
title_full Challenges and advances in computational docking: 2009 in review
title_fullStr Challenges and advances in computational docking: 2009 in review
title_full_unstemmed Challenges and advances in computational docking: 2009 in review
title_short Challenges and advances in computational docking: 2009 in review
title_sort challenges and advances in computational docking: 2009 in review
topic receptor flexibility
computational docking
binding mode prediction
protein-ligand complexes
scoring
url http://hdl.handle.net/20.500.11937/35703