Combinatorial chemistry in drug discovery

Hogan, Joseph C.

doi:10.1038/nbt0497-328

Cited by 80 publications

(25 citation statements)

References 3 publications

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“…As plants produce a lot of antioxidants to control the oxidative stress, they represent a natural source of antioxidant and antibacterial activity, which can be observed in fruits, vegetables, roots, leaves and seeds [11]. When compared with plethora of synthetic substances, natural products offer the prospects of discovering a greater number of compounds, with sterically more complex structures [12,13].…”

Section: Introductionmentioning

confidence: 99%

Isolation and characterization of antioxidant and antibacterial compound from mango ginger (Curcuma amada Roxb.) rhizome

Policegoudra

Abiraj

Gowda

et al. 2007

Journal of Chromatography B

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Section: Introductionmentioning

confidence: 99%

Isolation and characterization of antioxidant and antibacterial compound from mango ginger (Curcuma amada Roxb.) rhizome

Policegoudra

Abiraj

Gowda

et al. 2007

Journal of Chromatography B

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“…NanA-specific mAbs were generated by in vitro selection using full length human IgG1 libraries expressed by yeast as previously published [61–64] and biotinylated NanA-variants as baits. Antibody clones were characterized as described below and selected for affinity-maturation (light chain diversification and subsequent heavy chain mutagenesis).…”

Section: Methodsmentioning

confidence: 99%

Assessing the function of pneumococcal neuraminidases NanA, NanB and NanC inin vitroandin vivolung infection models using monoclonal antibodies

et al. 2018

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Streptococcus pneumoniae isolates express up to three neuraminidases (sialidases), NanA, NanB and NanC, all of which cleave the terminal sialic acid of glycan-structures that decorate host cell surfaces. Most research has focused on the role of NanA with limited investigations evaluating the roles of all three neuraminidases in host-pathogen interactions. We generated two highly potent monoclonal antibodies (mAbs), one that blocks the enzymatic activity of NanA and one cross-neutralizing NanB and NanC. Total neuraminidase activity of clinical S. pneumoniae isolates could be inhibited by this mAb combination in enzymatic assays. To detect desialylation of cell surfaces by pneumococcal neuraminidases, primary human tracheal/bronchial mucocilial epithelial tissues were infected with S. pneumoniae and stained with peanut lectin. Simultaneous targeting of the neuraminidases was required to prevent desialylation, suggesting that inhibition of NanA alone is not sufficient to preserve terminal lung glycans. Importantly, we also found that all three neuraminidases increased the interaction of S. pneumoniae with human airway epithelial cells. Lectin-staining of lung tissues of mice pre-treated with mAbs before intranasal challenge with S. pneumoniae confirmed that both anti-NanA and anti-NanBC mAbs were required to effectively block desialylation of the respiratory epithelium in vivo. Despite this, no effect on survival, reduction in pulmonary bacterial load, or significant changes in cytokine responses were observed. This suggests that neuraminidases have no pivotal role in this murine pneumonia model that is induced by high bacterial challenge inocula and does not progress from colonization as it happens in the human host.

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“…[5][6][7][8][9] Many of the methods and techniques used in these fields have been applied in polymer science and many new methods specific to polymer synthesis and characterization have been developed.…”

Section: The Combinatorial Approachmentioning

confidence: 99%

Combinatorial and High‐Throughput Methods in Macromolecular Materials Research and Development

Webster

2008

Macro Chemistry & Physics

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Combinatorial and high‐throughput experimentation is used to accelerate the rate of experimentation in macromolecular science. Combinatorial and high‐throughput methods are used in macromolecular science to discover and optimize catalysts for polymerization reactions, discover compositions that have specific desired properties, and systematically explore polymer structure–property relationships. The use of high‐throughput methods can enable the discovery of complex catalyst systems or polymer compositions that would not be feasible using conventional experimental methods. In addition, combinatorial data can be used as inputs into computer models to enable the accurate prediction of material properties as a function of composition.magnified image

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Combinatorial chemistry in drug discovery

Cited by 80 publications

References 3 publications

Isolation and characterization of antioxidant and antibacterial compound from mango ginger (Curcuma amada Roxb.) rhizome

Isolation and characterization of antioxidant and antibacterial compound from mango ginger (Curcuma amada Roxb.) rhizome

Assessing the function of pneumococcal neuraminidases NanA, NanB and NanC inin vitroandin vivolung infection models using monoclonal antibodies

Combinatorial and High‐Throughput Methods in Macromolecular Materials Research and Development

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