Chemistry:LE135
From HandWiki
LE135 is a drug which acts as a selective retinoic acid receptor β (RARβ) antagonist. It was developed in the 1990s and has been widely used for research into the function of RARβ especially its roles in cell differentiation during growth, tissue repair and embryonic development, regulation of immune system function, and development of certain forms of cancer.[1][2][3][4][5][6][7][8][9][10][11][12][13] However, it has also been shown to act as a potent activator of the cation channels TRPV1 and TRPA1, which means caution must be applied when interpreting results which assume that it is only acting by blocking RARβ.[14]
References
- ↑ "Regulation of retinoidal actions by diazepinylbenzoic acids". Retinoid Synergists Which Activate the RXR-RAR Heterodimers. J Med Chem 40 (26): 4222–4234. 19 December 1997. doi:10.1021/jm9704309. PMID 9435893.
- ↑ "Inhibition of IL-1-induced IL-6 production by synthetic retinoids". Biochemical and Biophysical Research Communications 231 (2): 243–248. 13 February 1997. doi:10.1006/bbrc.1997.6087. PMID 9070257.
- ↑ "Effect of retinoic acid on morphological changes of human pancreatic cancer cells on collagen gels: a possible association with the metastatic potentials". Oncology Research 10 (1): 7–14. 1998. PMID 9613452.
- ↑ "Novel synthetic retinoids and separation of the pleiotropic retinoidal activities". Current Medicinal Chemistry 9 (5): 591–608. March 2002. doi:10.2174/0929867024606975. PMID 11945126.
- ↑ "Retinoic acids exert direct effects on T cells to suppress Th1 development and enhance Th2 development via retinoic acid receptors". International Immunology 15 (8): 1017–1025. August 2003. doi:10.1093/intimm/dxg101. PMID 12882839.
- ↑ "Pharmacological regulation of adult stem cells: chondrogenesis can be induced using a synthetic inhibitor of the retinoic acid receptor". Stem Cells (Dayton, Ohio) 25 (10): 2460–2468. October 2007. doi:10.1634/stemcells.2007-0059. PMID 17615267.
- ↑ "Retinoic acid receptor beta mediates all-trans retinoic acid facilitation of mesenchymal stem cells neuronal differentiation". The International Journal of Biochemistry & Cell Biology 45 (4): 866–875. April 2013. doi:10.1016/j.biocel.2013.01.002. PMID 23318218.
- ↑ "Retinoid signaling is necessary for, and promotes long-term memory formation following operant conditioning". Neurobiology of Learning and Memory 114: 127–140. October 2014. doi:10.1016/j.nlm.2014.05.010. PMID 24925874.
- ↑ "Cilostazol suppresses β-amyloid production by activating a disintegrin and metalloproteinase 10 via the upregulation of SIRT1-coupled retinoic acid receptor-β". Journal of Neuroscience Research 92 (11): 1581–1590. November 2014. doi:10.1002/jnr.23421. PMID 24903973.
- ↑ "The Expression of Bone Morphogenetic Protein 2 and Matrix Metalloproteinase 2 through Retinoic Acid Receptor Beta Induced by All-Trans Retinoic Acid in Cultured ARPE-19 Cells". PLOS ONE 11 (3). 11 March 2016. doi:10.1371/journal.pone.0150831. PMID 26967733.
- ↑ "Regulation of RXR-RAR Heterodimers by RXR- and RAR-Specific Ligands and Their Combinations". Cells 8 (11): 1392. 5 November 2019. doi:10.3390/cells8111392. PMID 31694317.
- ↑ "The Antagonist of Retinoic Acid Receptor α, ER-50891 Antagonizes the Inhibitive Effect of All-Trans Retinoic Acid and Rescues Bone Morphogenetic Protein 2-Induced Osteoblastogenic Differentiation". Drug Design, Development and Therapy 14: 297–308. 22 January 2020. doi:10.2147/DDDT.S215786. PMID 32158187.
- ↑ "Adapalene, an RAR agonist, exerts anti-inflammatory effects by regulating macrophage polarization through RAR-mediated signaling pathways". Scientific Reports 16 (1). 26 March 2026. doi:10.1038/s41598-026-44454-z. PMID 41888273.
- ↑ "LE135, a retinoid acid receptor antagonist, produces pain through direct activation of TRP channels". British Journal of Pharmacology 171 (6): 1510–1520. March 2014. doi:10.1111/bph.12543. PMID 24308840.
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