pone.0226661.g006.tif (496.83 kB)
Comparing small molecule activity profiles using the LSC assay and the biochemical assay.
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posted on 2020-04-02, 17:33 authored by Teresa L. Burgess, Joshua D. Amason, Jeffrey S. Rubin, Damien Y. Duveau, Laurence Lamy, David D. Roberts, Catherine L. Farrell, James Inglese, Craig J. Thomas, Thomas W. Miller(A) The structures of the compounds compared to the parent screening active compound (NCGC00138783). (B) Biochemical (ALPHAScreen) SIRPα-CD47 antagonism activity of NCGC00138783 and the structurally related analogs shown in A were compared to (C) antagonism activity of SIRPα binding to CD47 expressed on live Jurkat cells in the LSC assay. Normalized activity calculated with neutral control (CD47 + SIRPα, no inhibitor) as 0% and negative control (CD47—SIRPα, no inhibitor) as -100% activity. Assay activity with tested agents was then compared and normalized to these controls.
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amino-terminal pyroglutamate formationcell surface bindingstructure activity relationshipsCD 47SIRPlaser scanning cytometrycell-based binding assayhumanized CD 47LSC assaycancer immunotherapy agentsimmuno-oncology CD 47glutaminyl cyclase inhibitor SEN 177throughput screening assay platformmolecule drug development
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