Third- and Fourth-Generation SERMs

Labrie, Fernand; Labrie, Claude; Bélanger, Alain; Simard, Jacques

doi:10.1007/978-1-59259-157-2_9

Cited by 5 publications

(5 citation statements)

References 81 publications

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“…Serum samples were drawn in the morning (before 10 AM; 69% of the cohort) or around noon (between 10 AM and 3 PM, average 1 PM; 31% (27)(28)(29) was used to analyze DHEA (limit of detection, 0.20 ng/ml; intra-assay CV, 2.0%; interassay CV, 1.9%), testosterone (limit of detection, 0.05 ng/ml; intra-assay CV, 2.9%; interassay CV, 3.4%), and estradiol (limit of detection, 2.00 pg/ml; intra-assay CV, 1.5%; interassay CV, 2.7%) using a 50% phenyl-methyl polysiloxane (DB-17HT) capillary column (30-m Â 0.25-mm internal diameter; 0.15-mm film thickness) with helium as the carrier gas.…”

Section: Methods Study Population the Multicenter Mros (Osteoporoticmentioning

confidence: 99%

“…DHEA-S (limit of detection, 0.075 mg/ml; intra-assay CV, 5.2%; interassay CV, 6.3%) was analyzed by a validated liquid chromatography-tandem mass spectroscopy method using turbo ion spray, as previously described (27). To measure the serum sex hormonebinding globulin, we used an immunoradiometric assay (Orion Diagnostics, Espoo, Finland; limit of detection, 1.3 nmol/l; intra-assay CV, 3%; interassay CV, 7%).…”

Section: Methods Study Population the Multicenter Mros (Osteoporoticmentioning

confidence: 99%

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Dehydroepiandrosterone and its Sulfate Predict the 5-Year Risk of Coronary Heart Disease Events in Elderly Men

Tivesten

Vandenput

Carlzon

et al. 2014

Journal of the American College of Cardiology

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Section: Methods Study Population the Multicenter Mros (Osteoporoticmentioning

confidence: 99%

Section: Methods Study Population the Multicenter Mros (Osteoporoticmentioning

confidence: 99%

Dehydroepiandrosterone and its Sulfate Predict the 5-Year Risk of Coronary Heart Disease Events in Elderly Men

Tivesten

Vandenput

Carlzon

et al. 2014

Journal of the American College of Cardiology

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“…Compounds with agonistic activity were usually classified into three groups, normal agonist, partial agonist, or superagonist, based on their maximum efficacy ( E max ) of cell proliferation. The interesting activities are seen in series I. Conjugates possessing a para -SAHA group at the phenyl sulfonate unit are potent and highly efficacious ERα and ERβ antagonists; yet most benzothiophene scaffold-based hybrid HDAC inhibitors (termed SERMostats), developed by Thatcher et al, showed little effect on transcriptional activity, and ethynylestradiol-HDACi conjugates (EED-HDACi) developed by Oyelere et al retained the ERα agonist activity of their parent compound EED .…”

Section: Resultsmentioning

confidence: 99%

Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer

Tang

Zhang

et al. 2015

J. Med. Chem.

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A strategy to develop chemotherapeutic agents by combining several active groups into a single molecule as a conjugate that can modulate multiple cellular pathways may produce compounds having higher efficacy compared to that of single-target drugs. In this article, we describe the synthesis and evaluation of an array of dual-acting ER and histone deacetylase inhibitors. These novel hybrid compounds combine an indirect antagonism structure motif of ER (OBHS, oxabicycloheptene sulfonate) with the HDAC inhibitor suberoylanilide hydroxamic acid (SAHA). These OBHS-HDACi conjugates exhibited good ER binding affinity and excellent ERα antagonistic activity, and they also exhibited potent inhibitory activities against HDACs. Compared with the approved drug tamoxifen, these conjugates exhibited higher antitumor potency in ERα-positive breast cancer cells (MCF-7). Moreover, these conjugates not only showed selective anticancer activity that was more potent against MCF-7 cells than DU 145 (prostate cancer), but they had no toxicity toward normal cells.

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“…It exhibits potent inhibitory activity on both ERα and ERβ. It inhibits both the AF1 and AF2 functions of the ERα and ERβ [232][233][234]. The effects of EM-800 and cyclophosphamide (drugs with different mechanisms of action ) alone and in combination was investigated on the growth of human breast cancer tumour ZR-75-1in nude mice.…”

Section: Phytoestrogens and Compounds Structurally Related To Flavonomentioning

confidence: 99%

Advances in the Science of Estrogen Receptor Modulation

Mj¹,

Dg²

2003

CMC

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This work details recent advances in the science of estrogen receptor (ER) modulation, with emphasis on the discovery of novel ligands for the ER ligand binding domain (LBD). A detailed examination of structural studies of the ERs is presented with analysis of the impact of such works on contemporary ligand design and the molecular pharmacology of the ER. The various classes of ER modulators are discussed on the basis of stuctural similarities including selective estrogen receptor modulators (SERMs) and 'pure' non-steroidal antiestrogens. Additionally we review the emergence of a novel selective class of modulator which we have termed the selective estrogen receptor subtype modulators (SERSMs) and, in a departure from LBD strategies we examine the discovery of novel peptide inhibitors of the ER which inhibit transcriptional activiation of agonist liganded receptor through interaction with coactivator recruitment proteins, and offer unique insight to the mechanism of action of all classes of ER modulators. Through examination of patent and classical literature we present a thorough and informative cross-section of the contemporary state of the art in this exciting field of pharmaceutical research.

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Third- and Fourth-Generation SERMs

Cited by 5 publications

References 81 publications

Dehydroepiandrosterone and its Sulfate Predict the 5-Year Risk of Coronary Heart Disease Events in Elderly Men

Dehydroepiandrosterone and its Sulfate Predict the 5-Year Risk of Coronary Heart Disease Events in Elderly Men

Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer

Advances in the Science of Estrogen Receptor Modulation

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