Tools for efficient high-throughput synthesis

Chighine, Alessandra; Sechi, Gianluca; Bradley, Mark

doi:10.1016/j.drudis.2007.04.004

Cited by 40 publications

(18 citation statements)

References 48 publications

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“…In recent years, there has been intense activity in the discovery and development of new drug candidates due to the emergence of disciplines such as combinatorial chemistry and high‐throughput screening 29,30 . However, not all potent candidates possess the correct bioavailability characteristics required for cellular entry.…”

Section: Microspheres For Cellular Deliverymentioning

confidence: 99%

Multifunctionalized Biocompatible Microspheres for Sensing

Sánchez‐Martín¹,

Alexander²,

Bradley³

2008

Annals of the New York Academy of Sciences

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We present our achievements in the synthesis and application of multifunctionalized, cross-linked, polystyrene microspheres, which remarkably and quite generally are taken up by all cell types studied to date. Importantly, the nature of these synthetic beads allows multistep solid-phase chemistry and the ability to bind essentially any molecule/sensor/nucleic acid to them. These microspheres have a number of advantages over other cellular delivery approaches. First, a diverse range of compounds can be attached to the microspheres, and we have demonstrated that these materials are effectively delivered into cells; second, the cellular cargo can be modulated through modification of bead loading; third, they are large enough to be visualized using standard microscopy techniques; and fourth, their cargos are not diluted within the cell. Populations of cells containing beads can be readily sorted from other cells for subsequent analysis with very high, but controllable, uptake rates, which can be modulated through modulation of the bead size and incubation time. Recent work has focused on the development of these microspheres as sensors for intracellular calcium and pH.

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Section: Microspheres For Cellular Deliverymentioning

confidence: 99%

Multifunctionalized Biocompatible Microspheres for Sensing

Sánchez‐Martín¹,

Alexander²,

Bradley³

2008

Annals of the New York Academy of Sciences

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“…11 The application of automated methods to the synthesis of focused libraries to populate screening collections is an important field of research, particularly for the biopharmaceutical sector. The use of combinatorial chemistry techniques has become common place to generate compounds for the screening and optimization tools for library generation in drug discovery.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 3,5-disubstituted 1,2,4-oxadiazoles using ionic liquid-phase organic synthesis (IoLiPOS) methodology

et al. 2010

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“…Computational chemistry and structural biology have increased our ability to examine drugprotein interactions at the molecular level [7,8]. High-speed synthesis and screening have enabled us to rapidly prepare and test millions of compounds [9]. Contract research organizations (CROs) have been widely adopted to reduce costs so that internal medicinal chemists can focus beyond synthetic challenges [10].…”

Section: Introductionmentioning

confidence: 99%