Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor
Publication type: Journal Article
Publication date: 2009-03-18
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
19296599
Drug Discovery
Molecular Medicine
Abstract
The luteinizing hormone (LH) receptor plays an important role in fertility and certain cancers. The endogenous ligands human chorionic gonadotropin (hCG) and LH bind to the large N terminal domain of the receptor. We recently reported on the first radiolabeled low molecular weight (LMW) agonist for this receptor, [(3)H]Org 43553, which was now used to screen for new LMW ligands. We identified a terphenyl derivative that inhibited [(3)H]Org 43553 binding to the receptor, which led us to synthesize a number of derivatives. The most potent compound of this terphenyl series, 24 (LUF5771), was able to increase the dissociation rate of [(3)H]Org 43553 by 3.3-fold (at 10 muM). In a functional assay, the presence of 24 resulted in a 2- to 3-fold lower potency of both Org 43553 and LH. Thus, the compounds presented in this paper are the first LMW ligands that allosterically inhibit the LH receptor.
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Total citations:
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Citations from 2024:
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(18%)
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Heitman L. H. et al. Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor // Journal of Medicinal Chemistry. 2009. Vol. 52. No. 7. pp. 2036-2042.
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Heitman L. H., Narlawar R., de Vries H., Willemsen M. N., Wolfram D., Brussee J., IJzerman A. P. Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor // Journal of Medicinal Chemistry. 2009. Vol. 52. No. 7. pp. 2036-2042.
Cite this
RIS
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TY - JOUR
DO - 10.1021/jm801561h
UR - https://doi.org/10.1021/jm801561h
TI - Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor
T2 - Journal of Medicinal Chemistry
AU - Heitman, Laura H.
AU - Narlawar, R.
AU - de Vries, Henk
AU - Willemsen, Milou N
AU - Wolfram, Dieter
AU - Brussee, Johannes
AU - IJzerman, Adriaan P.
PY - 2009
DA - 2009/03/18
PB - American Chemical Society (ACS)
SP - 2036-2042
IS - 7
VL - 52
PMID - 19296599
SN - 0022-2623
SN - 1520-4804
ER -
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@article{2009_Heitman,
author = {Laura H. Heitman and R. Narlawar and Henk de Vries and Milou N Willemsen and Dieter Wolfram and Johannes Brussee and Adriaan P. IJzerman},
title = {Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor},
journal = {Journal of Medicinal Chemistry},
year = {2009},
volume = {52},
publisher = {American Chemical Society (ACS)},
month = {mar},
url = {https://doi.org/10.1021/jm801561h},
number = {7},
pages = {2036--2042},
doi = {10.1021/jm801561h}
}
Cite this
MLA
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Heitman, Laura H., et al. “Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor.” Journal of Medicinal Chemistry, vol. 52, no. 7, Mar. 2009, pp. 2036-2042. https://doi.org/10.1021/jm801561h.