CGP 52608 explained

CGP 52608 is a selective ligand of the RAR-related orphan receptor alpha.[1] It has been used as a biochemical tool to investigate nuclear and membrane signaling of melatonin.[1] CGP 52608 has also been reported to possess antiarthritic activity.[2] The pharmaceutical company Novartis brought it to clinical trials for rheumatoid arthritis, but development was discontinued in 2006.[3]

CGP 52608 contains a thiazolinidinedione group.[4]

Notes and References

  1. Wiesenberg I, Missbach M, Kahlen JP, Schräder M, Carlberg C . Transcriptional activation of the nuclear receptor RZR alpha by the pineal gland hormone melatonin and identification of CGP 52608 as a synthetic ligand . Nucleic Acids Res. . 23 . 3 . 327–33 . February 1995 . 7885826 . 306679 . 10.1093/nar/23.3.327 .
  2. Missbach M, Jagher B, Sigg I, Nayeri S, Carlberg C, Wiesenberg I . Thiazolidine diones, specific ligands of the nuclear receptor retinoid Z receptor/retinoid acid receptor-related orphan receptor alpha with potent antiarthritic activity . J. Biol. Chem. . 271 . 23 . 13515–22 . June 1996 . 8662835 . 10.1074/jbc.271.23.13515 . free .
  3. Web site: CGP 52608 . Adis Insight .
  4. Melatonin and RZR/ROR receptor ligand CGP 52608 induce apoptosis in the murine colonic cancer. Winczyk . K. Pawlikowski . M. Karasek . M. J Pineal Res. Sep 2001 . 31. 2. 179–82. 10.1034/j.1600-079x.2001.310213.x . 11555175 . 6461798 .

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