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Identification and X-ray co-crystal structure of a small-molecule activator of LFA-1-ICAM-1 binding. | LitMetric

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Article Abstract

Stabilization of protein-protein interactions by small molecules is a concept with few examples reported to date. Herein we describe the identification and X-ray co-crystal structure determination of IBE-667, an ICAM-1 binding enhancer for LFA-1. IBE-667 was designed based on the SAR information obtained from an on-bead screen of tagged one-bead one-compound combinatorial libraries by confocal nanoscanning and bead picking (CONA). Cellular assays demonstrate the activity of IBE-667 in promoting the binding of LFA-1 on activated immune cells to ICAM-1.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4314669PMC
http://dx.doi.org/10.1002/anie.201310240DOI Listing

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