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- Bunyapaiboonsri, T., et al.
(författare)
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Generation of Bis-cationic heterocyclic inhibitors of Bacillus subtilis HPr kinase/phosphatase from a ditopic dynamic combinatorial library
- 2003
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Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 46:26, s. 5803-5811
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Tidskriftsartikel (refereegranskat)abstract
- Ditopic dynamic combinatorial. libraries were generated and screened toward inhibition of the bifunctional enzyme HPr kinase/phosphatase from Bacillus subtilis. The libraries were composed of all possible combinations resulting from the dynamic interconversion of 16 hydrazides and five monoaldehyde or dialdehyde building blocks, resulting in libraries containing up to 440 different constituents. Of all possible acyl hydrazones formed, active compounds containing two terminal cationic heterocyclic recognition groups separated by a spacer of appropriate structure could be rapidly identified using a dynamic deconvolution procedure. Thus, parallel testing of sublibraries where one specific component was excluded basically revealed all the essential components. A potent ditopic inhibitor, based on 2-amino-benzimidazole, was identified from the process.
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| 3. |
- Duner, Gunnar, et al.
(författare)
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Signal Enhancement in Ligand-Receptor Interactions using Dynamic Polymers at Quartz Crystal Microbalance Surfaces
- 2016
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Ingår i: The Analyst. - : Royal Society of Chemistry (RSC). - 0003-2654 .- 1364-5528. ; 141:13, s. 3993-3996
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Tidskriftsartikel (refereegranskat)abstract
- The potential for signal amplification on QCM sensors by use of in situ polymerized poly(acrylic acid) brushes has been studied. A biotin derivative was immobilized on these surfaces and the interaction with anti-biotin Fabs was evaluated. Interaction data was found to be specific for the studied binding events, and the level of non-specific binding was shown to be low. The surface was proven to be suitable for regeneration, of importance for biomolecular interaction analysis and repetitive immunoassays.For comparison, the same interaction system was tested using commercial sensor surfaces with carboxylated self-assembled monolayers. The poly(acrylic acid) surface showed a dramatic increase in signal response with more than ten times the signal of the carboxylated self-assembled monolayer surface. Thus, the present study shows that polymers can be successfully applied to amplify responses on QCM sensors, valuable for studies of interactions between receptors and low molecular weight compounds.
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