The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
GSK-3-Selective Inhibitors Derived from Tyrian Purple Indirubins
Open accessAbstract
Gastropod mollusks have been used for over 2500 years to produce the "Tyrian purple" dye made famous by the Phoenicians. This dye is constituted of mixed bromine-substituted indigo and indirubin isomers. Among these, the new natural product 6-bromoindirubin and its synthetic, cell-permeable derivative, 6-bromoindirubin-3'-oxime (BIO), display remarkable selective inhibition of glycogen synthase kinase-3 (GSK-3). Cocrystal structure of GSK-3beta/BIO and CDK5/p25/indirubin-3'-oxime were resolved, providing a detailed view of indirubins' interactions within the ATP binding pocket of these kinases. BIO but not 1-methyl-BIO, its kinase inactive analog, also inhibited the phosphorylation on Tyr276/216, a GSK-3alpha/beta activation site. BIO but not 1-methyl-BIO reduced beta-catenin phosphorylation on a GSK-3-specific site in cellular models. BIO but not 1-methyl-BIO closely mimicked Wnt signaling in Xenopus embryos. 6-bromoindirubins thus provide a new scaffold for the development of selective and potent pharmacological inhibitors of GSK-3.
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Cites
The specificities of protein kinase inhibitors: an update
BAIN, J., McLAUCHLAN, H., ELLIOTT, M., & COHEN, P. (2003) · Biochemical Journal · doi:10.1042/bj20021535 · Cited by 1,369
Indirubin and Indigo Are Potent Aryl Hydrocarbon Receptor Ligands Present in Human Urine
Adachi, J., Mori, Y., Matsui, S., Takigami, H., Fujino, J., Kitagawa, H., Miller, C. A., Kato, T., Saeki, K., & Matsuda, T. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.c100238200 · Cited by 407
Oxidation of Indole by Cytochrome P450 Enzymes
Gillam, E. M. J., Notley, L. M., Cai, H., De Voss, J. J., & Guengerich, F. P. (2000) · Biochemistry · doi:10.1021/bi001229u · Cited by 313
Cited by
The Wnt Signaling Pathway in Development and Disease
Logan, C. Y., & Nusse, R. (2004) · Annual Review of Cell and Developmental Biology · doi:10.1146/annurev.cellbio.20.010403.113126 · Cited by 5,325
Faulkner, D. J. (1990) · Natural Product Reports · doi:10.1039/np9900700269 · Cited by 4,866
Sato, N., Meijer, L., Skaltsounis, L., Greengard, P., & Brivanlou, A. H. (2004) · Nature Medicine · doi:10.1038/nm979 · Cited by 2,109
Self-citationGoessling, W., North, T. E., Loewer, S., Lord, A. M., Lee, S., Stoick-Cooper, C. L., Weidinger, G., Puder, M., Daley, G. Q., Moon, R. T., et al. (2009) · Cell · doi:10.1016/j.cell.2009.01.015 · Cited by 699
Wnt Signaling Requires Sequestration of Glycogen Synthase Kinase 3 inside Multivesicular Endosomes
Taelman, V. F., Dobrowolski, R., Plouhinec, J.-L., Fuentealba, L. C., Vorwald, P. P., Gumper, I., Sabatini, D. D., & De Robertis, E. M. (2010) · Cell · doi:10.1016/j.cell.2010.11.034 · Cited by 676
Metadata
- Authors
- Meijer, L., Skaltsounis, A.-L., Magiatis, P., Polychronopoulos, P., Knockaert, M., Leost, M., Ryan, X. P., Vonica, C. A., Brivanlou, A., Dajani, R., Crovace, C., Tarricone, C., Musacchio, A., Roe, S. M., Pearl, L., & Greengard, P.
- Venue
- Chemistry & Biology
- Publisher
- Elsevier BV
- Published
- 2003-12
- Volume
- 10
- Issue
- 12
- Pages
- 1255-1266
- ISSN
- 1074-5521 (ISSN-L)
- OpenAlex
- W1964378600
- Cited by
- 808
- References
- 3
- FWCI
- 8.26
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Meijer, L., Skaltsounis, A.-L., Magiatis, P., Polychronopoulos, P., Knockaert, M., Leost, M., Ryan, X. P., Vonica, C. A., Brivanlou, A., Dajani, R., Crovace, C., Tarricone, C., Musacchio, A., Roe, S. M., Pearl, L., & Greengard, P. (2003). GSK-3-Selective Inhibitors Derived from Tyrian Purple Indirubins. Chemistry & Biology. https://doi.org/10.1016/j.chembiol.2003.11.010
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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.
