The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation
Open accessAbstract
Autotaxin (ATX) is a secreted nucleotide pyrophosphatase/phosphodiesterase that functions as a lysophospholipase D to produce the lipid mediator lysophosphatidic acid (LPA), a mitogen, chemoattractant, and survival factor for many cell types. The ATX-LPA signaling axis has been implicated in angiogenesis, chronic inflammation, fibrotic diseases and tumor progression, making this system an attractive target for therapy. However, potent and selective nonlipid inhibitors of ATX are currently not available. By screening a chemical library, we have identified thiazolidinediones that selectively inhibit ATX-mediated LPA production both in vitro and in vivo. Inhibitor potency was approximately 100-fold increased (IC 50 ∼ 30 nM) after the incorporation of a boronic acid moiety, designed to target the active-site threonine (T210) in ATX. Intravenous injection of this inhibitor into mice resulted in a surprisingly rapid decrease in plasma LPA levels, indicating that turnover of LPA in the circulation is much more dynamic than previously appreciated. Thus, boronic acid-based small molecules hold promise as candidate drugs to target ATX.
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Tager, A. M., LaCamera, P., Shea, B. S., Campanella, G. S., Selman, M., Zhao, Z., Polosukhin, V., Wain, J., Karimi-Shah, B. A., Kim, N. D., et al. (2008) · Nature Medicine · doi:10.1038/nm1685 · Cited by 823
Potent and selective inhibitors of the proteasome: Dipeptidyl boronic acids
Adams, J., Behnke, M., Chen, S., Cruickshank, A. A., Dick, L. R., Grenier, L., Klunder, J. M., Ma, Y.-T., Plamondon, L., & Stein, R. L. (1998) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(98)00029-8 · Cited by 685
Cited by
Boron Chemicals in Diagnosis and Therapeutics
Das, B. C., Thapa, P., Karki, R., Schinke, C., Das, S., Kambhampati, S., Banerjee, S. K., Van Veldhuizen, P., Verma, A., Weiss, L. M., et al. (2013) · Future Medicinal Chemistry · doi:10.4155/fmc.13.38 · Cited by 279
Design and discovery of boronic acid drugs
Plescia, J., & Moitessier, N. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112270 · Cited by 201
Docosatetraenoyl LPA is elevated in exhaled breath condensate in idiopathic pulmonary fibrosis
Montesi, S. B., Mathai, S. K., Brenner, L. N., Gorshkova, I. A., Berdyshev, E. V., Tager, A. M., & Shea, B. S. (2014) · BMC Pulmonary Medicine · doi:10.1186/1471-2466-14-5 · Cited by 66
Metadata
- Authors
- Albers, H. M. H. G., Dong, A., van Meeteren, L. A., Egan, D. A., Sunkara, M., van Tilburg, E. W., Schuurman, K., van Tellingen, O., Morris, A. J., Smyth, S. S., Moolenaar, W. H., & Ovaa, H.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2010-04
- Volume
- 107
- Issue
- 16
- Pages
- 7257-7262
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2145179793
- Cited by
- 204
- References
- 2
- FWCI
- 10.04
- Type
- journal article
- Language
- en
- Open access
- green
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- Albers, H. M. H. G., Dong, A., van Meeteren, L. A., Egan, D. A., Sunkara, M., van Tilburg, E. W., Schuurman, K., van Tellingen, O., Morris, A. J., Smyth, S. S., Moolenaar, W. H., & Ovaa, H. (2010). Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.1001529107
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