Smart ligand

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Smart ligands are affinity ligands selected with pre-defined equilibrium (K_{d}), kinetic (k_{off}, k_{on}) and thermodynamic (ΔH, ΔS) parameters of biomolecular interaction.

Ligands with desired parameters can be selected from large combinatorial libraries of biopolymers using instrumental separation techniques with well-described kinetic behaviour, such as Kinetic capillary electrophoresis (KCE), Surface Plasmon Resonance (SPR), Microscale Thermophoresis (MST),[1][2] etc. Known examples of smart ligands include DNA smart aptamers; however, RNA and peptide smart aptamers can also be developed.

Smart ligands can find a set of unique applications in biomedical research, drug discovery and proteomic studies. For example, a panel of DNA smart aptamers has been recently used to develop affinity analysis of proteins with ultra-wide dynamic range of measured concentrations.

References[edit]

  1. ^ Baaske P, Wienken CJ, Reineck P, Duhr S, Braun D (Feb 2010). "Optical Thermophoresis quantifies Buffer dependence of Aptamer Binding". Angew. Chem. Int. Ed. 49 (12): 1–5. doi:10.1002/anie.200903998. PMID 20186894. Lay summaryPhsyorg.com. 
  2. ^ Wienken CJ et al. (Oct 2010). "Protein-binding assays in biological liquids using microscale thermophoresis". Nature Communications 1 (7): 100. Bibcode:2010NatCo...1E.100W. doi:10.1038/ncomms1093. PMID 20981028. 
  • Drabovich AP, Berezovski MV, Musheev MU, Krylov SN (January 2009). "Selection of smart small-molecule ligands: the proof of principle". Anal. Chem. 81 (1): 490–4. doi:10.1021/ac8023813. PMID 19055427. 
  • Drabovich A, Berezovski M, Krylov SN (August 2005). "Selection of smart aptamers by equilibrium capillary electrophoresis of equilibrium mixtures (ECEEM)". J. Am. Chem. Soc. 127 (32): 11224–5. doi:10.1021/ja0530016. PMID 16089434. 
  • Drabovich AP, Berezovski M, Okhonin V, Krylov SN (May 2006). "Selection of smart aptamers by methods of kinetic capillary electrophoresis". Anal. Chem. 78 (9): 3171–8. doi:10.1021/ac060144h. PMID 16643010. 
  • Drabovich AP, Okhonin V, Berezovski M, Krylov SN (June 2007). "Smart aptamers facilitate multi-probe affinity analysis of proteins with ultra-wide dynamic range of measured concentrations". J. Am. Chem. Soc. 129 (23): 7260–1. doi:10.1021/ja072269p. PMID 17503828. 
  • Krylov SN (January 2007). "Kinetic CE: foundation for homogeneous kinetic affinity methods". Electrophoresis 28 (1–2): 69–88. doi:10.1002/elps.200600577. PMID 17245689. 

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