Identification and X-ray co-crystal structure of a small-molecule activator of LFA-1-ICAM-1 binding.
Angew Chem Int Ed Engl
; 53(17): 4322-6, 2014 Apr 22.
Article
em En
| MEDLINE
| ID: mdl-24692345
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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ligação Proteica
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Azepinas
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Antígeno-1 Associado à Função Linfocitária
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Molécula 1 de Adesão Intercelular
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Bibliotecas de Moléculas Pequenas
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Indazóis
Tipo de estudo:
Diagnostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article