Biology:Retinoic acid receptor gamma
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Short description: Protein-coding gene in the species Homo sapiens
 Generic protein structure example |
Retinoic acid receptor gamma (RAR-γ), also known as NR1B3 (nuclear receptor subfamily 1, group B, member 3) is a nuclear receptor encoded by the RARG gene.[1][2] Adapalene selectively targets retinoic acid receptor beta and retinoic acid receptor gamma[3] and its agonism of the gamma subtype is largely responsible for adapalene's observed effects.[4]
Interactions
Retinoic acid receptor gamma has been shown to interact with NCOR1.[5]
Ligands
- Agonists
- Adapalene (also agonist at RARβ and weakly at RARα)
- CD1530 [6]
- Tazarotene (mixed RARβ/RARγ agonist, selective over RARα)
- Trifarotene (RARγ selective)
- Antagonists
See also
References
- ↑ "Entrez Gene: RARG retinoic acid receptor, gamma". https://www.ncbi.nlm.nih.gov/gene?Db=gene&Cmd=ShowDetailView&TermToSearch=5916.
- ↑ "Genomic organization of the retinoic acid receptor gamma gene". Nucleic Acids Research 19 (3): 573–8. Feb 1991. doi:10.1093/nar/19.3.573. PMID 1849262.
- ↑ "Retinoids in the treatment of skin aging: an overview of clinical efficacy and safety". Clinical Interventions in Aging 1 (4): 327–48. 2006. doi:10.2147/ciia.2006.1.4.327. PMID 18046911.
- ↑ "Pharmacology of adapalene". The British Journal of Dermatology 139 (Suppl 52): 3–7. October 1998. doi:10.1046/j.1365-2133.1998.1390s2003.x. PMID 9990413.
- ↑ "Identification of nuclear receptor corepressor as a peroxisome proliferator-activated receptor alpha interacting protein". The Journal of Biological Chemistry 274 (22): 15901–7. May 1999. doi:10.1074/jbc.274.22.15901. PMID 10336495.
- ↑ Yimiti D, Uchibe K, Toriyama M, Hayashi Y, Ikuta Y, Nakasa T, Akiyama H, Watanabe H, Kondoh G, Takimoto A, Shukunami C, Adachi N, Miyaki S. CD1530, selective RARγ agonist, facilitates Achilles tendon healing by modulating the healing environment including less chondrification in a mouse model. J Orthop Res. 2025 Feb;43(2):273-284. doi:10.1002/jor.26006 PMID 39513493
- ↑ Hughes NE, Bleisch TJ, Jones SA, Richardson TI, Doti RA, Wang Y, Stout SL, Durst GL, Chambers MG, Oskins JL, Lin C, Adams LA, Page TJ, Barr RJ, Zink RW, Osborne H, Montrose-Rafizadeh C, Norman BH. Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3274-3277. doi:10.1016/j.bmcl.2016.05.056 PMID 27261179
- ↑ Holmes WF, Dawson MI, Soprano RD, Soprano KJ. Induction of apoptosis in ovarian carcinoma cells by AHPN/CD437 is mediated by retinoic acid receptors. J Cell Physiol. 2000 Oct;185(1):61-7. doi:10.1002/1097-4652(200010)185:1<61::AID-JCP5>3.0.CO;2-0 PMID 10942519
Further reading
- "Purification, cloning, and RXR identity of the HeLa cell factor with which RAR or TR heterodimerizes to bind target sequences efficiently". Cell 68 (2): 377–95. Jan 1992. doi:10.1016/0092-8674(92)90478-U. PMID 1310259.
- "Retinoic acid receptors as regulators of human epidermal keratinocyte differentiation". Molecular Endocrinology 6 (5): 667–76. May 1992. doi:10.1210/mend.6.5.1318502. PMID 1318502.
- "RAR gamma 2 expression is regulated through a retinoic acid response element embedded in Sp1 sites". Molecular and Cellular Biology 12 (7): 2976–85. Jul 1992. doi:10.1128/mcb.12.7.2976. PMID 1320193.
- "Chromosomal assignment of retinoic acid receptor (RAR) genes in the human, mouse, and rat genomes". Genomics 10 (4): 1061–9. Aug 1991. doi:10.1016/0888-7543(91)90199-O. PMID 1655630. https://dipot.ulb.ac.be/dspace/bitstream/2013/188897/1/Elsevier_172524.pdf.
- "Murine isoforms of retinoic acid receptor gamma with specific patterns of expression". Proceedings of the National Academy of Sciences of the United States of America 87 (7): 2700–4. Apr 1990. doi:10.1073/pnas.87.7.2700. PMID 2157210. Bibcode: 1990PNAS...87.2700K.
- "Identification of a novel isoform of the retinoic acid receptor gamma expressed in the mouse embryo". Molecular and Cellular Biology 10 (5): 2335–40. May 1990. doi:10.1128/mcb.10.5.2335. PMID 2157970.
- "A functional retinoic acid receptor encoded by the gene on human chromosome 12". Molecular Endocrinology 4 (6): 837–44. Jun 1990. doi:10.1210/mend-4-6-837. PMID 2172793.
- "A third human retinoic acid receptor, hRAR-gamma". Proceedings of the National Academy of Sciences of the United States of America 86 (14): 5310–4. Jul 1989. doi:10.1073/pnas.86.14.5310. PMID 2546152. Bibcode: 1989PNAS...86.5310K.
- "Crystal structure of the RAR-gamma ligand-binding domain bound to all-trans retinoic acid". Nature 378 (6558): 681–9. Dec 1995. doi:10.1038/378681a0. PMID 7501014. Bibcode: 1995Natur.378..681R.
- "A human retinoic acid receptor gamma isoform is homologous to the murine retinoic acid receptor gamma 7". Nucleic Acids Research 21 (10): 2520. May 1993. doi:10.1093/nar/21.10.2520. PMID 7685085.
- "Retinoic acid inhibition of IL-1-induced IL-6 production by human lung fibroblasts". Journal of Immunology 152 (3): 1419–27. Feb 1994. doi:10.4049/jimmunol.152.3.1419. PMID 8301142.
- "Retinoic acid receptor/retinoid X receptor heterodimers can be activated through both subunits providing a basis for synergistic transactivation and cellular differentiation". The Journal of Biological Chemistry 272 (14): 9443–9. Apr 1997. doi:10.1074/jbc.272.14.9443. PMID 9083083.
- "RAR-, not RXR, ligands inhibit cell activation and prevent apoptosis in B-lymphocytes". Journal of Cellular Physiology 175 (1): 68–77. Apr 1998. doi:10.1002/(SICI)1097-4652(199804)175:1<68::AID-JCP8>3.0.CO;2-A. PMID 9491782.
- "Conformational adaptation of agonists to the human nuclear receptor RAR gamma". Nature Structural Biology 5 (3): 199–202. Mar 1998. doi:10.1038/nsb0398-199. PMID 9501913.
- "Arg278, but not Lys229 or Lys236, plays an important role in the binding of retinoic acid by retinoic acid receptor gamma". The Journal of Biological Chemistry 273 (51): 34016–21. Dec 1998. doi:10.1074/jbc.273.51.34016. PMID 9852056.
- "Modulation of aromatase expression in the breast tissue by ERR alpha-1 orphan receptor". Cancer Research 58 (24): 5695–700. Dec 1998. PMID 9865725.
- "Retinoid-dependent recruitment of a histone H1 displacement activity by retinoic acid receptor". The Journal of Biological Chemistry 274 (32): 22563–8. Aug 1999. doi:10.1074/jbc.274.32.22563. PMID 10428834.
- "Crystal structure of the human RXRalpha ligand-binding domain bound to its natural ligand: 9-cis retinoic acid". The EMBO Journal 19 (11): 2592–601. Jun 2000. doi:10.1093/emboj/19.11.2592. PMID 10835357.
- "Retinoid signaling is attenuated by proteasome-mediated degradation of retinoid receptors in human keratinocyte HaCaT cells". Experimental Cell Research 274 (1): 130–7. Mar 2002. doi:10.1006/excr.2001.5450. PMID 11855864.
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