Confirming Target Engagement for Reversible Inhibitors In Vivo by Kinetically Tuned Activity-Based Probes

The development of small-molecule inhibitors for perturbing enzyme function requires assays to confirm that the inhibitors interact with their enzymatic targets in vivo. Determining target engagement in vivo can be particularly challenging for poorly characterized enzymes that lack known biomarkers...

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Hlavní autoři: Adibekian, Alexander, Martin, Brent R., Chang, Jae Won, Hsu, Ku-Lung, Tsuboi, Katsunori, Bachovchin, Daniel A., Speers, Anna E., Brown, Steven J., Spicer, Timothy, Fernandez-Vega, Virneliz, Ferguson, Jill, Hodder, Peter S., Rosen, Hugh, Cravatt, Benjamin F.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2012
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Article
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC3392194/
https://ncbi.nlm.nih.gov/pubmed/22690931
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ja303400u
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