ArticleACS chemical neuroscience2011
Benzothiophene Selective Estrogen Receptor Modulators Provide Neuroprotection by a novel GPR30-dependent Mechanism.
Article in ACS chemical neuroscience, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
36 citing papers in PubMed, 74 citations in OpenAlex.
- Strong protection by bazedoxifene against chemically-induced ferroptotic neuronal death in vitro and in vivo.Cell communication and signaling : CCS · 2025Article
- From Bones to Bugs: Structure-Based Development of Raloxifene-Derived Pathoblockers That Inhibit Pyocyanin Production inJournal of medicinal chemistry · 2025Article
- A framework for safe estradiol modulation in male bipolar disorder: theoretical justification for SERM-enabled adjunctive therapy.Frontiers in psychiatry · 2025Article
- Channeling Nicotinamide Phosphoribosyltransferase (NAMPT) to Address Life and Death.Journal of medicinal chemistry · 2024Review
- A Review on the Mechanism and Structure-activity Relationship of Resveratrol Heteroaryl Analogues.Combinatorial chemistry & high throughput screening · 2024Review
- Vanillin-Based Indolin-2-one Derivative Bearing a Pyridyl Moiety as a Promising Anti-Breast Cancer Agent via Anti-Estrogenic Activity.ACS omega · 2023Article
- The Role of Estrogen Receptors and Their Signaling across Psychiatric Disorders.International journal of molecular sciences · 2020Review
- Recent progress in selective estrogen receptor downregulators (SERDs) for the treatment of breast cancer.RSC medicinal chemistry · 2020Review
- Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.Journal of medicinal chemistry · 2019Article
- Neuroprotective Role of Hypothermia in Hypoxic-ischemic Brain Injury: Combined Therapies using Estrogen.Current neuropharmacology · 2019Review
- 17β-estradiol and tamoxifen protect mice from manganese-induced dopaminergic neurotoxicity.Neurotoxicology · 2018Article
- Effects of Ovariectomy in an hSOD1-G93A Transgenic Mouse Model of Amyotrophic Lateral Sclerosis (ALS).Medical science monitor : international medical journal of experimental and clinical research · 2018Article
- Translational Significance of Selective Estrogen Receptor Modulators in Psychiatric Disorders.International journal of endocrinology · 2018Review
- Effects of estrogen receptor modulators on cytoskeletal proteins in the central nervous system.Neural regeneration research · 2017Review
- Tamoxifen Provides Structural and Functional Rescue in Murine Models of Photoreceptor Degeneration.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2017Article
- Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.Journal of medicinal chemistry · 2017Article
- In Vitro Neuroprotective and Anti-Inflammatory Activities of Natural and Semi-Synthetic Spirosteroid Analogues.Molecules (Basel, Switzerland) · 2016Article
- International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators.Pharmacological reviews · 2015Review
- Emerging from the bottleneck: benefits of the comparative approach to modern neuroscience.Trends in neurosciences · 2015Review
- Article
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
Abstract
The clinical benzothiophene SERM (BT-SERM), raloxifene, was compared with estrogens in protection of primary rat neurons against oxygen-glucose deprivation (OGD). Structure-activity relationships for neuroprotection were determined for a family of BT-SERMs displaying a spectrum of ERα and ERβ binding affinity and agonist/antagonist activity, leading to discovery of a neuroprotective pharmacophore, present in the clinically relevant SERMS, raloxifene and desmethylarzoxifene (DMA), for which submicromolar potency was observed for neuroprotection. BT-SERM neuroprotection did not correlate with binding to ER nor classical ER activity, however, both the neuroprotective SERMs and estrogens were shown, using pharmacological probes, to activate the same kinase signaling cascades. The antiestrogen ICI 182,780 inhibited the actions of estrogens, but not those of BT-SERMs, whereas antagonism of the G-protein coupled receptor, GPR30, was effective for both SERMs and estrogens. Since SERMs have antioxidant activity, ER-independent mechanisms were studied using the classical phenolic antioxidants, BHT and Trolox, and the Nrf2-dependent cytoprotective electrophile, sulforaphane. However, neuroprotection by these agents was not sensitive to GPR30 antagonism. Collectively, these data indicate that the activity of neuroprotective BT-SERMs is GPR30-dependent and ER-independent and not mediated by antioxidant effects. Comparison of novel BT-SERM derivatives and analogs identified a neuroprotective pharmacophore of potential use in design of novel neuroprotective agents with a spectrum of ER activity.
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.