The Experts below are selected from a list of 139578 Experts worldwide ranked by ideXlab platform
Glenn C. Micalizio - One of the best experts on this subject based on the ideXlab platform.
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A biomimetic polyketide-Inspired Approach to small-molecule ligand discovery
Nature Chemistry, 2012Co-Authors: Claudio Aquino, Mohosin Sarkar, Michael J. Chalmers, Kimberly Mendes, Thomas Kodadek, Glenn C. MicalizioAbstract:The discovery of new compounds for the pharmacological manipulation of protein function often embraces the screening of compound collections, and it is widely recognized that natural products offer beneficial characteristics as protein ligands. Much effort has therefore been focused on ‘natural product-like’ libraries, yet the synthesis and screening of such libraries is often limited by one or more of the following: modest library sizes and structural diversity, conformational heterogeneity and the costs associated with the substantial infrastructure of modern high-throughput screening centres. Here, we describe the design and execution of an Approach to this broad problem by merging principles associated with biologically Inspired oligomerization and the structure of polyketide-derived natural products. A novel class of chiral and conformationally constrained oligomers is described (termed ‘chiral oligomers of pentenoic amides’, COPA), which offers compatibility with split-and-pool methods and can be screened en masse in a batch mode. We demonstrate that a COPA library containing 160,000 compounds is a useful source of novel protein ligands by identifying a non-covalent synthetic ligand to the DNA-binding domain of the p53 transcription factor. The design and synthesis of a family of chiral and conformationally constrained oligomers is described. Asymmetric synthesis of the monomers is presented and the preparation of a 160,000-member library of diverse tetramers via split-and-pool methods is discussed. From this library, a non-covalent ligand to the DNA-binding domain of p53 was discovered.
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a biomimetic polyketide Inspired Approach to small molecule ligand discovery
Nature Chemistry, 2012Co-Authors: Claudio Aquino, Mohosin Sarkar, Michael J. Chalmers, Thomas Kodadek, Kimberly R Mendes, Glenn C. MicalizioAbstract:The design and synthesis of a family of chiral and conformationally constrained oligomers is described. Asymmetric synthesis of the monomers is presented and the preparation of a 160,000-member library of diverse tetramers via split-and-pool methods is discussed. From this library, a non-covalent ligand to the DNA-binding domain of p53 was discovered.
Jean-pol Vigneron - One of the best experts on this subject based on the ideXlab platform.
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Bio-Inspired Approach of the fluorescence emission properties in the scarabaeid beetle Hoplia coerulea (Coleoptera): Modeling by transfer-matrix optical simulations
Journal of Applied Physics, 2012Co-Authors: Eloise Van Hooijdonk, Serge Berthier, Jean-pol VigneronAbstract:Scales of the scarabaeid beetle Hoplia coerulea (Coleoptera) contain fluorescent molecules embedded in a multilayer structure. The consequence of this source confinement is a modification of the fluorescence properties, i.e., an enhancement or inhibition of the emission of certain wavelengths. In this work, we propose a bio-Inspired Approach to this problem. In other words, we use numerical simulations based on the one-dimensional transfer-matrix formalism to investigate the influence of a Hoplia-like system on emission characteristics and, from the results, we deduce potential technical applications. We reveal that depending on the choice of some parameters (layer thickness, dielectric constant, and position of the emitting source in the structure), it is possible to enhance or inhibit the fluorescence emission for certain wavelengths. This observation could be of great interest to design new optical devices in the field of optoelectronic, solar cells, biosensors, etc.
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Bio-Inspired Approach of the fluorescence emission properties in the scarabaeid beetle Hoplia coerulea (Coleoptera): Modeling by transfer-matrix optical simulations
Journal of Applied Physics, 2012Co-Authors: Eloise Van Hooijdonk, Serge Berthier, Jean-pol VigneronAbstract:Scales of the scarabaeid beetle Hoplia coerulea (Coleoptera) contain fluorescent molecules embedded in a multilayer structure. The consequence of this source confinement is a modification of the fluorescence properties, i.e., an enhancement or inhibition of the emission of certain wavelengths. In this work, we propose a bio-Inspired Approach to this problem. In other words, we use numerical simulations based on the one-dimensional transfer-matrix formalism to investigate the influence of a Hoplia-like system on emission characteristics and, from the results, we deduce potential technical applications. We reveal that depending on the choice of some parameters (layer thickness, dielectric constant, and position of the emitting source in the structure), it is possible to enhance or inhibit the fluorescence emission for certain wavelengths. This observation could be of great interest to design new optical devices in the field of optoelectronic, solar cells, biosensors, etc. (C) 2012 American Institute of Physics. [http://dx.doi.org/10.1063/1.4768896]
Claudio Aquino - One of the best experts on this subject based on the ideXlab platform.
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A biomimetic polyketide-Inspired Approach to small-molecule ligand discovery
Nature Chemistry, 2012Co-Authors: Claudio Aquino, Mohosin Sarkar, Michael J. Chalmers, Kimberly Mendes, Thomas Kodadek, Glenn C. MicalizioAbstract:The discovery of new compounds for the pharmacological manipulation of protein function often embraces the screening of compound collections, and it is widely recognized that natural products offer beneficial characteristics as protein ligands. Much effort has therefore been focused on ‘natural product-like’ libraries, yet the synthesis and screening of such libraries is often limited by one or more of the following: modest library sizes and structural diversity, conformational heterogeneity and the costs associated with the substantial infrastructure of modern high-throughput screening centres. Here, we describe the design and execution of an Approach to this broad problem by merging principles associated with biologically Inspired oligomerization and the structure of polyketide-derived natural products. A novel class of chiral and conformationally constrained oligomers is described (termed ‘chiral oligomers of pentenoic amides’, COPA), which offers compatibility with split-and-pool methods and can be screened en masse in a batch mode. We demonstrate that a COPA library containing 160,000 compounds is a useful source of novel protein ligands by identifying a non-covalent synthetic ligand to the DNA-binding domain of the p53 transcription factor. The design and synthesis of a family of chiral and conformationally constrained oligomers is described. Asymmetric synthesis of the monomers is presented and the preparation of a 160,000-member library of diverse tetramers via split-and-pool methods is discussed. From this library, a non-covalent ligand to the DNA-binding domain of p53 was discovered.
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a biomimetic polyketide Inspired Approach to small molecule ligand discovery
Nature Chemistry, 2012Co-Authors: Claudio Aquino, Mohosin Sarkar, Michael J. Chalmers, Thomas Kodadek, Kimberly R Mendes, Glenn C. MicalizioAbstract:The design and synthesis of a family of chiral and conformationally constrained oligomers is described. Asymmetric synthesis of the monomers is presented and the preparation of a 160,000-member library of diverse tetramers via split-and-pool methods is discussed. From this library, a non-covalent ligand to the DNA-binding domain of p53 was discovered.
Eloise Van Hooijdonk - One of the best experts on this subject based on the ideXlab platform.
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Bio-Inspired Approach of the fluorescence emission properties in the scarabaeid beetle Hoplia coerulea (Coleoptera): Modeling by transfer-matrix optical simulations
Journal of Applied Physics, 2012Co-Authors: Eloise Van Hooijdonk, Serge Berthier, Jean-pol VigneronAbstract:Scales of the scarabaeid beetle Hoplia coerulea (Coleoptera) contain fluorescent molecules embedded in a multilayer structure. The consequence of this source confinement is a modification of the fluorescence properties, i.e., an enhancement or inhibition of the emission of certain wavelengths. In this work, we propose a bio-Inspired Approach to this problem. In other words, we use numerical simulations based on the one-dimensional transfer-matrix formalism to investigate the influence of a Hoplia-like system on emission characteristics and, from the results, we deduce potential technical applications. We reveal that depending on the choice of some parameters (layer thickness, dielectric constant, and position of the emitting source in the structure), it is possible to enhance or inhibit the fluorescence emission for certain wavelengths. This observation could be of great interest to design new optical devices in the field of optoelectronic, solar cells, biosensors, etc.
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Bio-Inspired Approach of the fluorescence emission properties in the scarabaeid beetle Hoplia coerulea (Coleoptera): Modeling by transfer-matrix optical simulations
Journal of Applied Physics, 2012Co-Authors: Eloise Van Hooijdonk, Serge Berthier, Jean-pol VigneronAbstract:Scales of the scarabaeid beetle Hoplia coerulea (Coleoptera) contain fluorescent molecules embedded in a multilayer structure. The consequence of this source confinement is a modification of the fluorescence properties, i.e., an enhancement or inhibition of the emission of certain wavelengths. In this work, we propose a bio-Inspired Approach to this problem. In other words, we use numerical simulations based on the one-dimensional transfer-matrix formalism to investigate the influence of a Hoplia-like system on emission characteristics and, from the results, we deduce potential technical applications. We reveal that depending on the choice of some parameters (layer thickness, dielectric constant, and position of the emitting source in the structure), it is possible to enhance or inhibit the fluorescence emission for certain wavelengths. This observation could be of great interest to design new optical devices in the field of optoelectronic, solar cells, biosensors, etc. (C) 2012 American Institute of Physics. [http://dx.doi.org/10.1063/1.4768896]
Mohosin Sarkar - One of the best experts on this subject based on the ideXlab platform.
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A biomimetic polyketide-Inspired Approach to small-molecule ligand discovery
Nature Chemistry, 2012Co-Authors: Claudio Aquino, Mohosin Sarkar, Michael J. Chalmers, Kimberly Mendes, Thomas Kodadek, Glenn C. MicalizioAbstract:The discovery of new compounds for the pharmacological manipulation of protein function often embraces the screening of compound collections, and it is widely recognized that natural products offer beneficial characteristics as protein ligands. Much effort has therefore been focused on ‘natural product-like’ libraries, yet the synthesis and screening of such libraries is often limited by one or more of the following: modest library sizes and structural diversity, conformational heterogeneity and the costs associated with the substantial infrastructure of modern high-throughput screening centres. Here, we describe the design and execution of an Approach to this broad problem by merging principles associated with biologically Inspired oligomerization and the structure of polyketide-derived natural products. A novel class of chiral and conformationally constrained oligomers is described (termed ‘chiral oligomers of pentenoic amides’, COPA), which offers compatibility with split-and-pool methods and can be screened en masse in a batch mode. We demonstrate that a COPA library containing 160,000 compounds is a useful source of novel protein ligands by identifying a non-covalent synthetic ligand to the DNA-binding domain of the p53 transcription factor. The design and synthesis of a family of chiral and conformationally constrained oligomers is described. Asymmetric synthesis of the monomers is presented and the preparation of a 160,000-member library of diverse tetramers via split-and-pool methods is discussed. From this library, a non-covalent ligand to the DNA-binding domain of p53 was discovered.
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a biomimetic polyketide Inspired Approach to small molecule ligand discovery
Nature Chemistry, 2012Co-Authors: Claudio Aquino, Mohosin Sarkar, Michael J. Chalmers, Thomas Kodadek, Kimberly R Mendes, Glenn C. MicalizioAbstract:The design and synthesis of a family of chiral and conformationally constrained oligomers is described. Asymmetric synthesis of the monomers is presented and the preparation of a 160,000-member library of diverse tetramers via split-and-pool methods is discussed. From this library, a non-covalent ligand to the DNA-binding domain of p53 was discovered.
