Smart ligand

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

^
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): 2238–41. doi:10.1002/anie.200903998. PMID 20186894. S2CID 42489892.
- "A hot road to new drugs". Phys.org. February 24, 2010.
^ Wienken CJ, et al. (Oct 2010). "Protein-binding assays in biological liquids using microscale thermophoresis". Nature Communications. 1 (7): 100. Bibcode:2010NatCo...1..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. S2CID 263508678.
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. S2CID 34123687.
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. S2CID 12488366.
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. S2CID 36937603.
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. S2CID 29641423.

External links edit

Extending Protein Detection

[Baaske-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): 2238–41. doi:10.1002/anie.200903998. PMID 20186894. S2CID 42489892.
"A hot road to new drugs". Phys.org. February 24, 2010.

[2] "A hot road to new drugs". Phys.org. February 24, 2010.

[Wienken-2] Wienken CJ, et al. (Oct 2010). "Protein-binding assays in biological liquids using microscale thermophoresis". Nature Communications. 1 (7): 100. Bibcode:2010NatCo...1..100W. doi:10.1038/ncomms1093. PMID 20981028.

[1]

[2]