Near infrared fluorescence lifetime FRET imaging of target engagement at multiscale (Conference Presentation)

Barroso, Margarida; Rudkouskaya, Alena; Ward, Jamie; Mazurkiewicz, Joseph E.; Sinsuebphon, Nattawut; Chen, Sez-Jade; Intes, Xavier

doi:10.1117/12.2297567

Cited by 1 publication

(2 citation statements)

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Section: Established and Emerging Methods: In Vivo Imagingmentioning

confidence: 99%

“…36 Both luminescence and fluorescence imaging have demonstrated huge potential as a novel in vivo imaging approach to measure target engagement. This includes the monitoring of different biological processes in immunology, 37,38 oncology, 39,40 virology, 41,42 and neuroscience. 43,44 Receptor ligand engagement in vivo and quantification of intracellular receptor ligand binding can be achieved with whole-body macroscopic lifetime-based Förster resonance energy transfer (FRET) imaging (NIR MFLI FRET).…”

Section: Anatomical and Morphological Imaging: Ultrasound Mri And Ctmentioning

confidence: 99%

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The Opportunities and Use of Imaging to Measure Target Engagement

Maynard

Hart

2020

SLAS Discovery

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Lack of efficacy and poor safety outcomes are deemed to be the greatest causes of clinical failure of novel therapeutics. The use of biomarkers that give accurate information on target engagement, providing confidence that pharmacological activity in the target organ is being achieved, is key in optimizing clinical success. Without a measurement of target engagement, it can be very difficult to discern the basis for any lack of efficacy of a drug molecule within the pharmaceutical industry. Target engagement can be measured in both an in vitro and in vivo setting, and in recent years imaging measurements have been used frequently in drug discovery and development to assess target engagement and receptor occupancy in both human and animal models. From this perspective, we assess and look at the advancements in both in vivo and ex vivo imaging to demonstrate the enormous potential that imaging has as an application to provide a greater understanding of target engagement with a correlative therapeutic impact.

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