Solid supports for combinatorial chemistry

Yu, Zhanru; Bradley, Mark

doi:10.1016/s1367-5931(02)00327-7

Cited by 29 publications

(11 citation statements)

References 26 publications

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“…Biomimetic ligands result from the integration of rational design, combinatorial chemistry and screening in parallel for binding to the target protein. Sepharose qualities desired in a matrix for affinity chromatography, and has been utilized as the solid support for the synthesis and affinity-chromatographic screening of biomimetic ligands (Guillier et al, 2000;Yu and Bradley, 2002).…”

Section: Introductionmentioning

confidence: 99%

A new method for the screening of solid‐phase combinatorial libraries for affinity chromatography

Roque

Taipa

Lowe

2004

J of Molecular Recognition

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A new methodology for the rapid assessment of affinity ligands synthesized by combinatorial solid-phase chemistry is reported. This screening strategy utilizes the target protein conjugated to FITC, and represents an almost universal technique for the preliminary screening of solid-phase combinatorial libraries. The assessment of a triazine-scaffolded solid-phase combinatorial library of ligands, designed to bind to human IgG, was performed with FITC-human IgG, and the results compared with those obtained by conventional affinity chromatographic screening assays. The effect of different molar conjugation ratios of FITC-IgG (F/P) was evaluated. Independently of the F/P ratio, no false negative results were observed, although lower F/P ratios diminished non-specific interactions and the number of false positives. The nature of the substituents on the triazine scaffold was not related to the number of false positive IgG-binding ligands. The reproducibility of the FITC technique, using FITC-human IgG conjugates with low F/P ratio (F/P=2), was also evaluated. The FITC-based technique proved to be efficient and accurate in the identification of strongly binding ligands (binding >50% of loaded protein, by standard affinity chromatographic assays), and is envisaged as a versatile and cost-effective method to screen other systems, and evaluate several binding/elution conditions at small-scale, prior to scale-up to standard affinity chromatography.

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Section: Introductionmentioning

confidence: 99%

A new method for the screening of solid‐phase combinatorial libraries for affinity chromatography

Roque

Taipa

Lowe

2004

J of Molecular Recognition

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“…Cleavage from the support was carried out under TFA vapor in desiccator for 30 min, using the method of Blackwell et al 20 The yields and purities of the synthesized dipeptoids 7−10 (Figure 1) were determined using HPLC and LCMS measurements, and the eight synthesis methods were systematically compared (Table 1). The methods using bromoacetic acid (11) or chloroacetic acid (12) in DMF and microwave (entries 6−7, Table 1) did not provide satisfying purities. An overview of the best methods is given in Table 2.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

“…Combinatorics is a well-known approach in chemical biology and medical chemistry research . Solid-phase synthesis is one of the most frequent strategies for preparation of combinatorial libraries, including the synthesis of peptoid libraries. , However, the conventional polymeric supports (i.e., insoluble resin beads) have some disadvantages. These hydrophobic polymers are often expensive, fragile, difficult to manipulate and often incompatible with biological assays performed directly on the carrier.…”

Section: Introductionmentioning

confidence: 99%

Microwave-Facilitated SPOT-Synthesis of Antibacterial Dipeptoids

et al. 2017

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With microwave irradiation, the submonomer synthesis of dipeptoids on functionalized cellulose can be accelerated with good yields and purity. Optimization provided a library of 96 dipeptoids. From these, 29 compounds were found with an antibacterial activity against MRSA at a concentration of 25 μM. Large nonpolar residues, such as undecylamine and dehydroabiethylamine, are the key components engendering the observed antibacterial activity of these peptoids.

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“…Consequently to the large acceptance achieved by the split-and-mix strategy, several identification techniques have been also developed, such as nucleotide- [45,46], peptide- [47,48], chemical- [49], radiofrecuency- [50], color- [51], and shape- [52][53][54] encoded or iterative [55][56][57] and recursive [58,59] [65], in which reagents used to cleave products from the solid support are incorporated into the product; use of scavenger resins [66]; the introduction of safety-catch linkers [67][68][69] or the improvement of resin properties and loading capacities [70][71][72].…”

Section: Solid-phase and Solution-phase Combinatorial Chemistrymentioning

confidence: 99%