The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Design and Synthesis of Potent Retinoid X Receptor Selective Ligands That Induce Apoptosis in Leukemia Cells
Open accessAbstract
Structural modifications of the retinoid X receptor (RXR) selective compound 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2- naphthyl)ethenyl]benzoic acid (LGD1069), which is currently in phase I/IIA clinical trials for cancer and dermatological indications, have resulted in the identification of increasingly potent retinoids with > 1000-fold selectivity for the RXRs. This paper describes the design and preparation of a series of RXR selective retinoids as well as the biological data obtained from cotransfection and competitive binding assays which were used to evaluate their potency and selectivity. The most potent and selective of the analogs is 6-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2- yl)cyclopropyl]nicotinic acid (12d; LG100268). This compound has proven useful for investigating RXR dependent biological pathways including the induction of programmed cell death (PCD) and transglutaminase (TGase) activity. Our studies indicate that the induction of PCD and TGase in human leukemic myeloid cells is dependent upon activation of RXR-mediated pathways.
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Cites
Yung-Chi, C., & Prusoff, W. H. (1973) · Biochemical Pharmacology · doi:10.1016/0006-2952(73)90196-2 · Cited by 12,922
9-cis retinoic acid is a high affinity ligand for the retinoid X receptor
Heyman, R. A., Mangelsdorf, D. J., Dyck, J. A., Stein, R. B., Eichele, G., Evans, R. M., & Thaller, C. (1992) · Cell · doi:10.1016/0092-8674(92)90479-v · Cited by 1,780
Self-citationMultiplicity generates diversity in the retinoic acid signalling pathways
Leid, M., Kastner, P., & Chambon, P. (1992) · Trends in Biochemical Sciences · doi:10.1016/0968-0004(92)90014-z · Cited by 821
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Endogenous Bile Acids Are Ligands for the Nuclear Receptor FXR/BAR
Wang, H., Chen, J., Hollister, K., Sowers, L. C., & Forman, B. M. (1999) · Molecular Cell · doi:10.1016/s1097-2765(00)80348-2 · Cited by 1,636
Regulation of Absorption and ABC1-Mediated Efflux of Cholesterol by RXR Heterodimers
Repa, J. J., Turley, S. D., Lobaccaro, J.-M. A., Medina, J., Li, L., Lustig, K., Shan, B., Heyman, R. A., Dietschy, J. M., & Mangelsdorf, D. J. (2000) · Science · doi:10.1126/science.289.5484.1524 · Cited by 1,301
Self-citationRepa, J. J., Berge, K. E., Pomajzl, C., Richardson, J. A., Hobbs, H., & Mangelsdorf, D. J. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m109927200 · Cited by 852
Duvic, M., Hymes, K., Heald, P., Breneman, D., Martin, A. G., Myskowski, P., Crowley, C., Yocum, R. C., & for Members of the Bexarotene Worldwide Study Group (2001) · Journal of Clinical Oncology · doi:10.1200/jco.2001.19.9.2456 · Cited by 706
Triterpenoids and rexinoids as multifunctional agents for the prevention and treatment of cancer
Liby, K. T., Yore, M. M., & Sporn, M. B. (2007) · Nature Reviews Cancer · doi:10.1038/nrc2129 · Cited by 637
Metadata
- Authors
- Boehm, M. F., Zhang, L., Zhi, L., McClurg, M. R., Berger, E., Wagoner, M., Mais, D. E., Suto, C. M., Davies, P. J. A., Heyman, R. A., & Nadzan, A. M.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1995-08-01
- Volume
- 38
- Issue
- 16
- Pages
- 3146-3155
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2951765624
- Cited by
- 335
- References
- 3
- FWCI
- 4.62
- Type
- journal article
- Language
- en
- Open access
- green
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- The paper
- Boehm, M. F., Zhang, L., Zhi, L., McClurg, M. R., Berger, E., Wagoner, M., Mais, D. E., Suto, C. M., Davies, P. J. A., Heyman, R. A., & Nadzan, A. M. (1995). Design and Synthesis of Potent Retinoid X Receptor Selective Ligands That Induce Apoptosis in Leukemia Cells. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm00016a018
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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.
