The DOI matches its Crossref record; 6 of the 6 references it cites were found in a registry or an index.
Identification of small-molecule antagonists that inhibit an activator:coactivator interaction
Open accessAbstract
Phosphorylation of the cAMP response element binding protein (CREB) at Ser-133 in response to hormonal stimuli triggers cellular gene expression via the recruitment of the histone acetylase coactivator paralogs CREB binding protein (CBP) and p300 to the promoter. The NMR structure of the CREB:CBP complex, using relevant interaction domains called KID and KIX, respectively, reveals a shallow hydrophobic groove on the surface of KIX that accommodates an amphipathic helix in phospho (Ser-133) KID. Using an NMR-based screening approach on a preselected small-molecule library, we identified several compounds that bind to different surfaces on KIX. One of these, KG-501 (2-naphthol-AS-E-phosphate), targeted a surface distal to the CREB binding groove that includes Arg-600, a residue that is required for the CREB:CBP interaction. When added to live cells, KG-501 disrupted the CREB: CBP complex and attenuated target gene induction in response to cAMP agonist. These results demonstrate the ability of small molecules to interfere with second-messenger signaling cascades by inhibiting specific protein–protein interactions in the nucleus.
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Cites
In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2
Vassilev, L. T., Vu, B. T., Graves, B., Carvajal, D., Podlaski, F., Filipovic, Z., Kong, N., Kammlott, U., Lukacs, C., Klein, C., et al. (2004) · Science · doi:10.1126/science.1092472 · Cited by 4,661
Control of hepatic gluconeogenesis through the transcriptional coactivator PGC-1
Yoon, J. C., Puigserver, P., Chen, G., Donovan, J., Wu, Z., Rhee, J., Adelmant, G., Stafford, J., Kahn, C. R., Granner, D. K., et al. (2001) · Nature · doi:10.1038/35093050 · Cited by 1,821
Transcriptional activation by recruitment
Ptashne, M., & Gann, A. (1997) · Nature · doi:10.1038/386569a0 · Cited by 1,158
Radhakrishnan, I., Pérez-Alvarado, G. C., Parker, D., Dyson, H. J., Montminy, M. R., & Wright, P. E. (1997) · Cell · doi:10.1016/s0092-8674(00)80463-8 · Cited by 728
Self-citationParker, D., Ferreri, K., Nakajima, T., Lamorte, V. J., Evans, R., Koerber, S. C., Hoeger, C., & Montminy, M. R. (1996) · Molecular and Cellular Biology · doi:10.1128/mcb.16.2.694 · Cited by 408
Self-citationCooperativity in Transcription Factor Binding to the Coactivator CREB-binding Protein (CBP)
Goto, N. K., Zor, T., Martinez-Yamout, M., Dyson, H. J., & Wright, P. E. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m207660200 · Cited by 177
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Cited by
CREB and the CRTC co-activators: sensors for hormonal and metabolic signals
Altarejos, J. Y., & Montminy, M. (2011) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm3072 · Cited by 1,040
Self-citationTargeting hepatic glucose metabolism in the treatment of type 2 diabetes
Rines, A. K., Sharabi, K., Tavares, C. D. J., & Puigserver, P. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.151 · Cited by 375
A complex task? Direct modulation of transcription factors with small molecules
Koehler, A. N. (2010) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2010.03.022 · Cited by 189
Ghiboub, M., Elfiky, A. M. I., de Winther, M. P. J., Harker, N. R., Tough, D. F., & de Jonge, W. J. (2021) · Journal of Personalized Medicine · doi:10.3390/jpm11050336 · Cited by 28
Metadata
- Authors
- Best, J. L., Amezcua, C. A., Mayr, B., Flechner, L., Murawsky, C. M., Emerson, B., Zor, T., Gardner, K. H., & Montminy, M.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2004-12-07
- Volume
- 101
- Issue
- 51
- Pages
- 17622-17627
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2164208610
- Cited by
- 207
- References
- 6
- FWCI
- 1.53
- Type
- journal article
- Language
- en
- Open access
- green
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- Best, J. L., Amezcua, C. A., Mayr, B., Flechner, L., Murawsky, C. M., Emerson, B., Zor, T., Gardner, K. H., & Montminy, M. (2004). Identification of small-molecule antagonists that inhibit an activator:coactivator interaction. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.0406374101
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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.
