Identification and X-ray Co-crystal Structure of a Small-Molecule Activator of LFA-1-ICAM-1 Binding**

نویسندگان

  • Martin Hintersteiner
  • Jörg Kallen
  • Mario Schmied
  • Christine Graf
  • Thomas Jung
  • Gemma Mudd
  • Steven Shave
  • Hubert Gstach
  • Manfred Auer
چکیده

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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عنوان ژورنال:

دوره 53  شماره 

صفحات  -

تاریخ انتشار 2014