Slow diffusion of lactose out of galectin-3 crystals monitored by X-ray crystallography: possible implications for ligand-exchange protocols

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Title Slow diffusion of lactose out of galectin-3 crystals monitored by X-ray crystallography: possible implications for ligand-exchange protocols
Author Collins, Patrick; Hidari, Kazuya I.P.J.; Blanchard, Helen
Journal Name Acta Crystallographica. Section D: Biological Crystallography
Year Published 2007
Place of publication Denmark
Publisher Blackwell Munksgaard
Abstract Galectin-3 is a multifunctional carbohydrate-binding protein with roles in cancer progression. Besides carbohydrate-dependent extracellular functions, galectin-3 participates in carbohydrate-independent intracellular signalling pathways, including apoptosis, via protein-protein interactions, some engaging the carbohydrate-binding groove. When ligands bind within this site conformational rearrangements are induced and therefore information of un-liganded galectin-3 is valuable for structure-based drug-design. Removal of co-crystallised lactose from the human galectin-3 carbohydrate-recognition domain was achieved via crystal soaking, but took weeks, despite low affinity. Pre-soaking to remove lactose enabled subsequent binding of cryo-protectant glycerol, whereas when lactose was not removed a priori then the glycerol could not displace it over the short cryo-soak timeframe. Slow diffusion of lactose removal from crystals contrasts glycerol entering within minutes. The importance of removal of incumbent ligands prior to attempts to introduce alternative ligands is indicated, even for proteins exhibiting low affinity for ligands, and has significance for ligand exchange in structure based drug desig
Peer Reviewed Yes
Published Yes
Publisher URI http://journals.iucr.org/d/journalhomepage.html
Alternative URI http://dx.doi.org/10.1107/S090744490605270X
Copyright Statement Copyright 2007 Blackwell Publishing. The definitive version is available at www.blackwell-synergy.com
Volume D63
Page from 415
Page to 419
ISSN 0907-4449
Date Accessioned 2007-10-17
Language en_AU
Research Centre Institute for Glycomics
Faculty Faculty of Science, Environment, Engineering and Technology
Subject PRE2009-Physical Chemistry of Macromolecules
URI http://hdl.handle.net/10072/15546
Publication Type Journal Articles (Refereed Article)
Publication Type Code c1

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