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Structure-Based Optimization of a Peptidyl Inhibitor against Calcineurin-Nuclear Factor of Activated T Cell (NFAT) Interaction

[Image: see text] Calcineurin inhibitors such as cyclosporine A and FK506 are effective immunosuppressants but produce severe side effects. Rational modification of a previously reported peptide inhibitor, GPHPVIVITGPHEE (K(D) ∼ 500 nM), by replacing the two valine residues with tert-leucine and the...

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Detalles Bibliográficos
Autores principales: Qian, Ziqing, Dougherty, Patrick G., Liu, Tao, Oottikkal, Shameema, Hogan, Patrick G., Hadad, Christopher M., Pei, Dehua
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4174996/
https://www.ncbi.nlm.nih.gov/pubmed/25162754
http://dx.doi.org/10.1021/jm500743t