Mass spectrometric screening of ligands with lower off-rate from a clicked-based pooled library.
ACS Comb Sci
; 14(8): 451-5, 2012 Aug 13.
Article
em En
| MEDLINE
| ID: mdl-22809242
ABSTRACT
This paper describes a convenient screening method using ion trap electrospray ionization mass spectrometry to classify ligands to a target molecule in terms of kinetic parameters. We demonstrate this method in the screening of ligands to a hexahistidine tag from a pooled library synthesized by click chemistry. The ion trap mass spectrometry analysis revealed that higher stabilities of ligand-target complexes in the gas phase were related to lower dissociation rate constants, i.e., off-rates in solution. Finally, we prepared a fluorescent probe utilizing the ligand with lowest off-rate and succeeded in performing single molecule observations of hexahistidine-tagged myosin V walking on actin filaments.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Espectrometria de Massas por Ionização por Electrospray
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Bibliotecas de Moléculas Pequenas
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Corantes Fluorescentes
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Ligantes
Tipo de estudo:
Diagnostic_studies
/
Screening_studies
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article