The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Affinity-Driven Peptide Selection of an NFAT Inhibitor More Selective Than Cyclosporin A
Abstract
The flow of information from calcium-mobilizing receptors to nuclear factor of activated T cells (NFAT)–dependent genes is critically dependent on interaction between the phosphatase calcineurin and the transcription factor NFAT. A high-affinity calcineurin-binding peptide was selected from combinatorial peptide libraries based on the calcineurin docking motif of NFAT. This peptide potently inhibited NFAT activation and NFAT-dependent expression of endogenous cytokine genes in T cells, without affecting the expression of other cytokines that require calcineurin but not NFAT. Substitution of the optimized peptide sequence into the natural calcineurin docking site increased the calcineurin responsiveness of NFAT. Compounds that interfere selectively with the calcineurin-NFAT interaction without affecting calcineurin phosphatase activity may be useful as therapeutic agents that are less toxic than current drugs.
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Cites
A Mammalian Scaffold Complex That Selectively Mediates MAP Kinase Activation
Whitmarsh, A. J., Cavanagh, J., Tournier, C., Yasuda, J., & Davis, R. J. (1998) · Science · doi:10.1126/science.281.5383.1671 · Cited by 652
Cited by
Drug Discovery: A Historical Perspective
Drews, J. (2000) · Science · doi:10.1126/science.287.5460.1960 · Cited by 2,760
Transcriptional regulation by calcium, calcineurin, and NFAT
Hogan, P. G., Chen, L., Nardone, J., & Rao, A. (2003) · Genes & Development · doi:10.1101/gad.1102703 · Cited by 1,991
Self-citationCrabtree, G. R., & Olson, E. N. (2002) · Cell · doi:10.1016/s0092-8674(02)00699-2 · Cited by 1,323
Selective Inhibition of Vascular Endothelial Growth Factor–Mediated Angiogenesis by Cyclosporin a
Hernández, G. L., Volpert, O. V., Íñiguez, M. A., Lorenzo, E., Martínez-Martínez, S., Grau, R., Fresno, M., & Redondo, J. M. (2001) · The Journal of Experimental Medicine · doi:10.1084/jem.193.5.607 · Cited by 432
Rothermel, B., Vega, R. B., Yang, J., Wu, H., Bassel-Duby, R., & Williams, R. S. (2000) · Journal of Biological Chemistry · doi:10.1074/jbc.275.12.8719 · Cited by 414
Metadata
- Authors
- Aramburu, J., Yaffe, M. B., López-Rodrı́guez, C., Cantley, L. C., Hogan, P. G., & Rao, A.
- Venue
- Science
- Published
- 1999-09-24
- Volume
- 285
- Issue
- 5436
- Pages
- 2129-2133
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2028211858
- Cited by
- 613
- References
- 1
- FWCI
- 8.26
- Type
- journal article
- Language
- en
- Open access
- closed
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- The paper
- Aramburu, J., Yaffe, M. B., López-Rodrı́guez, C., Cantley, L. C., Hogan, P. G., & Rao, A. (1999). Affinity-Driven Peptide Selection of an NFAT Inhibitor More Selective Than Cyclosporin A. Science. https://doi.org/10.1126/science.285.5436.2129
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
