Β-LGND2 explained
β-LGND2, also known as ERβ-selective ligand 2 or as GTx-878, is a synthetic nonsteroidal estrogen and selective ERβ agonist which was under development by GTx for the treatment of benign prostatic hyperplasia, prostatitis, and rheumatoid arthritis but was never marketed.[1] [2] [3] [4] [5] [6] It shows approximately 25-fold selectivity for activation of the ERβ over the ERα (= 2 nM and 52 nM, respectively). β-LGND2 is an isoquinolinone derivative.
External links
Notes and References
- Web site: Research programme: Estrogen receptor beta agonists - Oncternal Therapeutics - AdisInsight.
- Yepuru M, Eswaraka J, Kearbey JD, Barrett CM, Raghow S, Veverka KA, Miller DD, Dalton JT, Narayanan R . Estrogen receptor--selective ligands alleviate high-fat diet- and ovariectomy-induced obesity in mice . J. Biol. Chem. . 285 . 41 . 31292–303 . October 2010 . 20657011 . 2951204 . 10.1074/jbc.M110.147850 . free .
- Ponnusamy S, Tran QT, Harvey I, Smallwood HS, Thiyagarajan T, Banerjee S, Johnson DL, Dalton JT, Sullivan RD, Miller DD, Bridges D, Narayanan R . Pharmacologic activation of estrogen receptor β increases mitochondrial function, energy expenditure, and brown adipose tissue . FASEB J. . 31 . 1 . 266–281 . January 2017 . 27733447 . 5161516 . 10.1096/fj.201600787RR . free . 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..
- Giddabasappa A, Eswaraka JR, Barrett CM, Bauler MN, Wu Z, Yepuru M, Miller DD, Dalton JT . β-LGND2, an ERβ selective agonist, inhibits pathologic retinal neovascularization . Invest. Ophthalmol. Vis. Sci. . 53 . 8 . 5066–75 . July 2012 . 22714897 . 10.1167/iovs.12-9627 . free .
- Paterni I, Granchi C, Katzenellenbogen JA, Minutolo F . Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential . Steroids . 90 . 13–29 . November 2014 . 24971815 . 4192010 . 10.1016/j.steroids.2014.06.012 .
- Mohler ML, Narayanan R, Coss CC, Hu K, He Y, Wu Z, Hong SS, Hwang DJ, Miller DD, Dalton JT . Estrogen receptor beta selective nonsteroidal estrogens: seeking clinical indications . Expert Opin Ther Pat . 20 . 4 . 507–34 . April 2010 . 20302450 . 10.1517/13543771003657164 . 314347 .
