A Small‐Molecule Agonist of the Wnt Signaling Pathway
Abstract
A new tool for developmental biology: A screen of combinatorial chemical libraries identified the 2-amino-4,6-disubstituted pyrimidine 1 as a dose-dependent agonist of Wnt signaling. Tadpoles that developed from embryos treated with 1 had substantial head defects (see right-hand image; left=control). Compound 1 appears to mimic the effects of a Wnt ligand in a Xenopus model and may be a useful tool in the study of physiological processes that involve the Wnt pathway.
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BML-284 is an agonist of Wnt/β-catenin signaling with an EC50 of 0.7 μM of Wnt reporter activity in HEK293 cells.
“BML-284 is an agonist of Wnt/β-catenin signaling with an EC50 of 0.7 µM of Wnt reporter activity in HEK293 cells [41].”
From CI-994 is a dual modulator of class I HDACs and Wnt/β-catenin signaling for the treatment of Alzheimer's disease (2026) · cites this paper as [41]
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Wnt signaling promotes regeneration in the retina of adult mammals
Osakada, F., Ooto, S., Akagi, T., Mandai, M., Akaike, A., & Takahashi, M. (2007) · The Journal of Neuroscience · doi:10.1523/jneurosci.4193-06.2007 · Cited by 322 · see citing works
Lu, W., Kawatani, K., Ren, Y., Nambara, T., Jia, L., Jeevaratnam, S., Lee, E., Martinez, P. R., Izhar, T., Wang, N., et al. (2026) · Alzheimer's Research & Therapy · doi:10.1186/s13195-026-01982-0 · Cited by 4 · see citing works
- Authors
- Liu, J., Wu, X., Mitchell, B., Kintner, C., Ding, S., & Schultz, P. G.
- Affiliations
- Scripps Research Institute (US)
- Salk Institute for Biological Studies (US)
- Corresponding author
- Ding, Sheng
- Schultz, Peter G.
- Venue
- Angewandte Chemie International Edition
- Publisher
- Wiley
- Published
- 2005-03-16
- Volume
- 44
- Issue
- 13
- Pages
- 1987-1990
- ISSN
- 1433-7851 (ISSN-L)
- 1521-3773
- OpenAlex
- W2125789563
- Cited by
- 142
- References
- 0
- Citations by year
- 2026: 6 · 2025: 9 · 2024: 8 · 2023: 5 · 2022: 5 · 2021: 9 · 2020: 5 · 2019: 6 · 2018: 6 · 2017: 7 · 2016: 4 · 2015: 5 · 2014: 7 · 2013: 7 · 2012: 6
- FWCI
- 3.64
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Angewandte Chemie International Edition (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Wnt/β-catenin signaling in development and cancer
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Hedgehog Signaling Pathway Studies
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Developmental Biology and Gene Regulation
- Keywords
- Wnt signaling, small molecule agonists, Xenopus tadpoles
- MeSH terms
- Animals, Cells, Cultured, Dimethyl Sulfoxide, Embryo, Nonmammalian, Xenopus laevis, Signal Transduction, Xenopus Proteins, Wnt Proteins, beta Catenin, TCF Transcription Factors, Transcription Factor 7-Like 2 Protein
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