Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRβ and ERRγ

William J. Zuercher; Stéphanie Gaillard; Lisa A. Orband-Miller; Esther Y.H. Chao; Barry G. Shearer; David G. Jones; Aaron B. Miller; Jon L. Collins; Donald P. McDonnell; Timothy M. Willson

doi:10.1021/jm050161j

Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRβ and ERRγ

William J. Zuercher, Stéphanie Gaillard, Lisa A. Orband-Miller, Esther Y.H. Chao, Barry G. Shearer, David G. Jones, Aaron B. Miller, Jon L. Collins, Donald P. McDonnell, Timothy M. Willson

Research output: Contribution to journal › Article › peer-review

79 Scopus citations

Abstract

The first small molecule agonists of the estrogen-related receptors have been identified. GSK4716 (3) and GSK9089 (4) show binding to ERRγ with remarkable selectivity over the classical estrogen receptors. Notably, in cell-based reporter assays, 3 mimics the protein ligand PGC-1α in activation of human ERRβ and ERRγ.

Original language	English (US)
Pages (from-to)	3107-3109
Number of pages	3
Journal	Journal of medicinal chemistry
Volume	48
Issue number	9
DOIs	https://doi.org/10.1021/jm050161j
State	Published - May 5 2005
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

Access to Document

10.1021/jm050161j

Cite this

Zuercher, W. J., Gaillard, S., Orband-Miller, L. A., Chao, E. Y. H., Shearer, B. G., Jones, D. G., Miller, A. B., Collins, J. L., McDonnell, D. P., & Willson, T. M. (2005). Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRβ and ERRγ. Journal of medicinal chemistry, 48(9), 3107-3109. https://doi.org/10.1021/jm050161j

Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRβ and ERRγ. / Zuercher, William J.; Gaillard, Stéphanie; Orband-Miller, Lisa A. et al.
In: Journal of medicinal chemistry, Vol. 48, No. 9, 05.05.2005, p. 3107-3109.

Research output: Contribution to journal › Article › peer-review

Zuercher, WJ, Gaillard, S, Orband-Miller, LA, Chao, EYH, Shearer, BG, Jones, DG, Miller, AB, Collins, JL, McDonnell, DP & Willson, TM 2005, 'Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRβ and ERRγ', Journal of medicinal chemistry, vol. 48, no. 9, pp. 3107-3109. https://doi.org/10.1021/jm050161j

@article{d8a36b9a21b94560a48ee498302e19f4,

title = "Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRβ and ERRγ",

abstract = "The first small molecule agonists of the estrogen-related receptors have been identified. GSK4716 (3) and GSK9089 (4) show binding to ERRγ with remarkable selectivity over the classical estrogen receptors. Notably, in cell-based reporter assays, 3 mimics the protein ligand PGC-1α in activation of human ERRβ and ERRγ.",

author = "Zuercher, {William J.} and St{\'e}phanie Gaillard and Orband-Miller, {Lisa A.} and Chao, {Esther Y.H.} and Shearer, {Barry G.} and Jones, {David G.} and Miller, {Aaron B.} and Collins, {Jon L.} and McDonnell, {Donald P.} and Willson, {Timothy M.}",

year = "2005",

month = may,

day = "5",

doi = "10.1021/jm050161j",

language = "English (US)",

volume = "48",

pages = "3107--3109",

journal = "Journal of medicinal chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "9",

}

TY - JOUR

T1 - Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRβ and ERRγ

AU - Zuercher, William J.

AU - Gaillard, Stéphanie

AU - Orband-Miller, Lisa A.

AU - Chao, Esther Y.H.

AU - Shearer, Barry G.

AU - Jones, David G.

AU - Miller, Aaron B.

AU - Collins, Jon L.

AU - McDonnell, Donald P.

AU - Willson, Timothy M.

PY - 2005/5/5

Y1 - 2005/5/5

N2 - The first small molecule agonists of the estrogen-related receptors have been identified. GSK4716 (3) and GSK9089 (4) show binding to ERRγ with remarkable selectivity over the classical estrogen receptors. Notably, in cell-based reporter assays, 3 mimics the protein ligand PGC-1α in activation of human ERRβ and ERRγ.

AB - The first small molecule agonists of the estrogen-related receptors have been identified. GSK4716 (3) and GSK9089 (4) show binding to ERRγ with remarkable selectivity over the classical estrogen receptors. Notably, in cell-based reporter assays, 3 mimics the protein ligand PGC-1α in activation of human ERRβ and ERRγ.

UR - http://www.scopus.com/inward/record.url?scp=20944432239&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=20944432239&partnerID=8YFLogxK

U2 - 10.1021/jm050161j

DO - 10.1021/jm050161j

M3 - Article

C2 - 15857113

AN - SCOPUS:20944432239

SN - 0022-2623

VL - 48

SP - 3107

EP - 3109

JO - Journal of medicinal chemistry

JF - Journal of medicinal chemistry

IS - 9

ER -

Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRβ and ERRγ

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this