From Wikipedia, the free encyclopedia
Chemical compound
Β-LGND2
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Other names | β-LGND2; ER-β-selective ligand 2 |
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Drug class |
Nonsteroidal estrogen; Selective ERβ agonist |
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4-bromo-6,8-dihydroxy-2-(4-hydroxyphenyl)isoquinolin-1-one
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CAS Number | |
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PubChem
CID | |
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Formula | C15H10BrNO4 |
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Molar mass | 348.152 g·mol−1 |
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3D model (
JSmol) | |
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C1=CC(=CC=C1N2C=C(C3=CC(=CC(=C3C2=O)O)O)Br)O
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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
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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 (
EC50Tooltip half-maximal effective concentration = 2 nM and 52 nM, respectively).
[3] β-LGND2 is an
isoquinolinone
derivative.
[2]
[5]
References
-
^
"Research programme: Estrogen receptor beta agonists - Oncternal Therapeutics - AdisInsight".
- ^
a
b Yepuru 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.
- ^
a
b Ponnusamy 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.
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^ 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.
- ^
a
b Paterni 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.
-
^ 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
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Mixed (
SERMsTooltip Selective estrogen receptor modulators) | |
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Antagonists |
- Coregulator-binding modulators:
ERX-11
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GPERTooltip G protein-coupled estrogen receptor | Agonists | |
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Antagonists | |
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Unknown | |
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