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β-LGND2

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
Β-LGND2
Clinical data
Other namesβ-LGND2; ER-β-selective ligand 2
Drug classNonsteroidal estrogen; Selective ERβ agonist
Identifiers
  • 4-bromo-6,8-dihydroxy-2-(4-hydroxyphenyl)isoquinolin-1-one
CAS Number
PubChemCID
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC15H10BrNO4
Molar mass348.152 g·mol−1
3D model (JSmol)
  • C1=CC(=CC=C1N2C=C(C3=CC(=CC(=C3C2=O)O)O)Br)O
  • InChI=1S/C15H10BrNO4/c16-12-7-17(8-1-3-9(18)4-2-8)15(21)14-11(12)5-10(19)6-13(14)20/h1-7,18-20H
  • Key:GLVQMSCCFOGRRG-UHFFFAOYSA-N

β-LGND2, also known asERβ-selective ligand 2 or asGTx-878, is asyntheticnonsteroidal estrogen andselectiveERβagonist which was under development byGTx for the treatment ofbenign prostatic hyperplasia,prostatitis, andrheumatoid arthritis but was never marketed.[1][2][3][4][5][6] It shows approximately 25-foldselectivity for activation of the ERβ over theERα (EC50Tooltip half-maximal effective concentration = 2 nM and 52 nM, respectively).[3] β-LGND2 is anisoquinolinonederivative.[2][5]

References

[edit]
  1. ^"Research programme: Estrogen receptor beta agonists - Oncternal Therapeutics - AdisInsight".
  2. ^abYepuru M, Eswaraka J, Kearbey JD, Barrett CM, Raghow S, Veverka KA, Miller DD, Dalton JT, Narayanan R (October 2010)."Estrogen receptor-{beta}-selective ligands alleviate high-fat diet- and ovariectomy-induced obesity in mice".J. Biol. Chem.285 (41):31292–303.doi:10.1074/jbc.M110.147850.PMC 2951204.PMID 20657011.
  3. ^abPonnusamy S, Tran QT, Harvey I, Smallwood HS, Thiyagarajan T, Banerjee S, Johnson DL, Dalton JT, Sullivan RD, Miller DD, Bridges D, Narayanan R (January 2017)."Pharmacologic activation of estrogen receptor β increases mitochondrial function, energy expenditure, and brown adipose tissue".FASEB J.31 (1):266–281.doi:10.1096/fj.201600787RR.PMC 5161516.PMID 27733447.We found that β-LGND2, also known as GTx-878 (GTx, Inc. (31)), reduces body weight and fat mass without altering feed consumption of high-fat diet (HFD)-fed WT, but not ER-βKO, mice.
  4. ^Giddabasappa A, Eswaraka JR, Barrett CM, Bauler MN, Wu Z, Yepuru M, Miller DD, Dalton JT (July 2012)."β-LGND2, an ERβ selective agonist, inhibits pathologic retinal neovascularization".Invest. Ophthalmol. Vis. Sci.53 (8):5066–75.doi:10.1167/iovs.12-9627.PMID 22714897.
  5. ^abPaterni I, Granchi C, Katzenellenbogen JA, Minutolo F (November 2014)."Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential".Steroids.90:13–29.doi:10.1016/j.steroids.2014.06.012.PMC 4192010.PMID 24971815.
  6. ^Mohler ML, Narayanan R, Coss CC, Hu K, He Y, Wu Z, Hong SS, Hwang DJ, Miller DD, Dalton JT (April 2010). "Estrogen receptor beta selective nonsteroidal estrogens: seeking clinical indications".Expert Opin Ther Pat.20 (4):507–34.doi:10.1517/13543771003657164.PMID 20302450.S2CID 314347.

External links

[edit]


ERTooltip Estrogen receptor
Agonists
Mixed
(SERMsTooltip Selective estrogen receptor modulators)
Antagonists
GPERTooltip G protein-coupled estrogen receptor
Agonists
Antagonists
Unknown
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