Miniaturization of the Luminescent Oxygen Channeling Immunoassay (LOCITM) for Use in Multiplex Array Formats and Other Biochips

Dafforn, Alan; Kirakossian, Hrair; Lao, Kaiqin

doi:10.1093/clinchem/46.9.1495

Cited by 8 publications

(3 citation statements)

References 4 publications

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“…AlphaScreen technology was first described in 1994 and is based on the principle of luminescent oxygen channeling [ 186 , 187 ]. AlphaScreen is a bead-based, nonradioactive amplified luminescent proximity homogeneous assay in which a donor and an acceptor pair of 250-nm-diameter reagent-coated polystyrene microbeads are brought into proximity by a molecular interaction of binding partners immobilized to these beads [ 187 , 188 , 189 ]. The detection system of AlphaScreen can be time-gated, as the signal is long lived, thus, eliminating short-lived background signals.…”

Section: Strategies For the Discovery Of Novel Ligands For Nuclearmentioning

confidence: 99%

Targeting Nuclear Receptors with Marine Natural Products

Yang

2014

Marine Drugs

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Nuclear receptors (NRs) are important pharmaceutical targets because they are key regulators of many metabolic and inflammatory diseases, including diabetes, dyslipidemia, cirrhosis, and fibrosis. As ligands play a pivotal role in modulating nuclear receptor activity, the discovery of novel ligands for nuclear receptors represents an interesting and promising therapeutic approach. The search for novel NR agonists and antagonists with enhanced selectivities prompted the exploration of the extraordinary chemical diversity associated with natural products. Recent studies involving nuclear receptors have disclosed a number of natural products as nuclear receptor ligands, serving to re-emphasize the translational possibilities of natural products in drug discovery. In this review, the natural ligands of nuclear receptors will be described with an emphasis on their mechanisms of action and their therapeutic potentials, as well as on strategies to determine potential marine natural products as nuclear receptor modulators.

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Section: Strategies For the Discovery Of Novel Ligands For Nuclearmentioning

confidence: 99%

Targeting Nuclear Receptors with Marine Natural Products

Yang

2014

Marine Drugs

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“…The energy is transferred to fluorophores present in the same bead that subsequently emit light at a wavelength of 520 to 620 nm. With the generation of ∼60,000 singlet oxygen molecules per donor bead, signal amplification is obtained (Dafforn et al, 2000).…”

Section: Luminescencementioning

confidence: 99%

Overview of High‐Throughput Screening

2009

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High-throughput screening (HTS) is a key process used in drug discovery to identify hits from compound libraries that may become leads for medicinal chemistry optimization. This updated overview discusses the utilization of compound libraries, compounds derived from combinatorial and parallel synthesis campaigns and natural product sources; creation of mother and daughter plates; and compound storage, handling, and bar coding in HTS. The unit also presents an overview of established and emerging assay technologies (i.e., time-resolved fluorescence, fluorescence polarization, fluorescence-correlation spectroscopy, functional whole cell assays, and high-content assays) and their integration in automation hardware and IT systems. This revised unit provides updated descriptions of state-of-the-art instrumentation and technologies in this rapidly changing environment. The section on assay methodologies now also covers enzyme complementation assays and methods for high-throughput screening of ion channel activities. Finally, a section on criteria for assay robustness is included discussing the Z'-factor, which is now a widely accepted criterion for evaluation and validation of high throughput screening assays.

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“…The energy is transferred to fluorophores present in the same bead that subsequently emit light at 520 to 620 nm. With the generation of ∼60,000 singlet oxygen molecules per donor, bead amplification is achieved (Dafforn et al, 2000).…”

Section: Luminescencementioning

confidence: 99%

Overview on High‐Throughput Screening

Entzeroth¹

2003

CP Pharmacology

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The known effects of drugs from a variety of pharmacological/therapeutic classes on the respiratory system, the life‐threatening consequences of respiratory dysfunction, and world‐wide regulatory safety guidelines all support the need for conducting respiratory evaluations in safety pharmacology. This unit provides an overview of the functional disorders of the respiratory system and presents the techniques and strategies considered to be most appropriate for detecting and characterizing drug‐induced respiratory disorders in safety pharmacology studies.

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Miniaturization of the Luminescent Oxygen Channeling Immunoassay (LOCITM) for Use in Multiplex Array Formats and Other Biochips

Cited by 8 publications

References 4 publications

Targeting Nuclear Receptors with Marine Natural Products

Targeting Nuclear Receptors with Marine Natural Products

Overview of High‐Throughput Screening

Overview on High‐Throughput Screening

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