ReviewMolecular endocrinology (Baltimore, Md.)2010
Minireview: Not picking pockets: nuclear receptor alternate-site modulators (NRAMs).
Review in Molecular endocrinology (Baltimore, Md.), 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 52 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
52 citing papers in PubMed, 124 citations in OpenAlex.
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- Recent applications of computational methods to allosteric drug discovery.Frontiers in molecular biosciences · 2022Review
- ER/AR Multi-Conformational Docking Server: A Tool for Discovering and Studying Estrogen and Androgen Receptor Modulators.Frontiers in pharmacology · 2022Article
- Structure-Activity Relationship Studies of Trisubstituted Isoxazoles as Selective Allosteric Ligands for the Retinoic-Acid-Receptor-Related Orphan Receptor γt.Journal of medicinal chemistry · 2021Article
- Orthosteric and Allosteric Dual Targeting of the Nuclear Receptor RORγt with a Bitopic Ligand.ACS chemical biology · 2021Article
- Nuclear receptor crosstalk - defining the mechanisms for therapeutic innovation.Nature reviews. Endocrinology · 2020Review
- Article
- Strategies for developing pregnane X receptor antagonists: Implications from metabolism to cancer.Medicinal research reviews · 2020Review
- Elucidation of an Allosteric Mode of Action for a Thienopyrazole RORγt Inverse Agonist.ChemMedChem · 2020Article
- Computational Analysis of Crystallization Additives for the Identification of New Allosteric Sites.ACS omega · 2020Article
- Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists.Journal of medicinal chemistry · 2020Article
- Steroid receptor/coactivator binding inhibitors: An update.Molecular and cellular endocrinology · 2019Review
- Molecules targeting the androgen receptor (AR) signaling axis beyond the AR-Ligand binding domain.Medicinal research reviews · 2019Review
- Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARγ Drug Pioglitazone.Journal of medicinal chemistry · 2019Article
- Characteristics of Nur77 and its ligands as potential anticancer compounds (Review).Molecular medicine reports · 2018Review
- A Cell-Permeable Stapled Peptide Inhibitor of the Estrogen Receptor/Coactivator Interaction.ACS chemical biology · 2018Article
- Using TR-FRET to Investigate Protein-Protein Interactions: A Case Study of PXR-Coregulator Interaction.Advances in protein chemistry and structural biology · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Because of their central importance in gene regulation and mediating the actions of many hormones, the nuclear receptors (NRs) have long been recognized as very important biological and pharmaceutical targets. Of all the surfaces available on a given NR, the singular site for regulation of receptor activity has almost invariably been the ligand-binding pocket of the receptor, the site where agonists, antagonists, and selective NR modulators interact. With our increasing understanding of the multiple molecular components involved in NR action, researchers have recently begun to look to additional interaction sites on NRs for regulating their activities by novel mechanisms. The alternate NR-associated interaction sites that have been targeted include the coactivator-binding groove and allosteric sites in the ligand-binding domain, the zinc fingers of the DNA-binding domain, and the NR response element in DNA. The studies thus far have been performed with the estrogen receptors, the androgen receptor (AR), the thyroid hormone receptors, and the pregnane X receptor. Phenotypic and conformation-based screens have also identified small molecule modulators that are believed to function through the NRs but have, as yet, unknown sites and mechanisms of action. The rewards from investigation of these NR alternate-site modulators should be the discovery of new therapeutic approaches and novel agents for regulating the activities of these important NR proteins.
Indexed as
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.