ReviewAdvances in pharmacology (San Diego, Calif.)2011
Pharmacological chaperones for misfolded gonadotropin-releasing hormone receptors.
Review in Advances in pharmacology (San Diego, Calif.), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 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
28 citing papers in PubMed.
- Folding, misfolding, and regulation of intracellular traffic of G protein-coupled receptors involved in the hypothalamic-pituitary-gonadal axis.Andrology · 2026Review
- Gonadotropin-Releasing Hormone Receptor (GnRHR) and Hypogonadotropic Hypogonadism.International journal of molecular sciences · 2023Review
- Spinocerebellar ataxia 38: structure-function analysis shows ELOVL5 G230V is proteotoxic, conformationally altered and a mutational hotspot.Human genetics · 2023Article
- Ligands for Melanocortin Receptors: Beyond Melanocyte-Stimulating Hormones and Adrenocorticotropin.Biomolecules · 2022Review
- Targeting trafficking as a therapeutic avenue for misfolded GPCRs leading to endocrine diseases.Frontiers in endocrinology · 2022Review
- Molecular basis for the evolved instability of a human G-protein coupled receptor.Cell reports · 2021Article
- Misfolded G Protein-Coupled Receptors and Endocrine Disease. Molecular Mechanisms and Therapeutic Prospects.International journal of molecular sciences · 2021Review
- Elagolix in the treatment of heavy menstrual bleeding associated with uterine fibroids in premenopausal women.Expert review of clinical pharmacology · 2021Review
- Folding and Misfolding of Human Membrane Proteins in Health and Disease: From Single Molecules to Cellular Proteostasis.Chemical reviews · 2019Article
- The melanocortin pathway and control of appetite-progress and therapeutic implications.The Journal of endocrinology · 2019Review
- Selective progesterone receptor modulators for fertility preservation in women with symptomatic uterine fibroids.Biology of reproduction · 2017Review
- Pharmacoperone rescue of vasopressin 2 receptor mutants reveals unexpected constitutive activity and coupling bias.PloS one · 2017Article
- Regulation of GPCR expression through an interaction with CCT7, a subunit of the CCT/TRiC complex.Molecular biology of the cell · 2016Article
- Pharmacological chaperoning: a primer on mechanism and pharmacology.Pharmacological research · 2014Review
- Using pharmacological chaperones to restore proteostasis.Pharmacological research · 2014Review
- Quality control autophagy degrades soluble ERAD-resistant conformers of the misfolded membrane protein GnRHR.Molecular cell · 2014Article
- Mutations in G protein-coupled receptors that impact receptor trafficking and reproductive function.Molecular and cellular endocrinology · 2014Review
- Ipsen 5i is a Novel Potent Pharmacoperone for Intracellularly Retained Melanocortin-4 Receptor Mutants.Frontiers in endocrinology · 2014Article
- A small molecule agonist THIQ as a novel pharmacoperone for intracellularly retained melanocortin-4 receptor mutants.International journal of biological sciences · 2014Article
- Current and future applications of GnRH, kisspeptin and neurokinin B analogues.Nature reviews. Endocrinology · 2013Review
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
Structural alterations provoked by mutations or genetic variations in the gene sequence of G protein-coupled receptors (GPCRs) may lead to abnormal function of the receptor molecule. Frequently, this leads to disease. While some mutations lead to changes in domains involved in agonist binding, receptor activation, or coupling to effectors, others may cause misfolding and lead to retention/degradation of the protein molecule by the quality control system of the cell. Several strategies, including genetic, chemical, and pharmacological approaches, have been shown to rescue function of trafficking-defective misfolded GPCRs. Among these, pharmacological strategies offer the most promising therapeutic tool to promote proper trafficking of misfolded proteins to the plasma membrane (PM). Pharmacological chaperones or "pharmacoperones" are small compounds that permeate the PM, enter cells, and bind selectively to misfolded proteins and correct folding allowing routing of the target protein to the PM, where the receptor may bind and respond to agonist stimulation. In this review, we describe new therapeutic opportunities based on mislocalization of otherwise functional human gonadotropin-releasing hormone receptors. This particular receptor is highly sensitive to single changes in chemical charge, and its intracellular traffic is delicately balanced between expression at the PM or retention/degradation in the endoplasmic reticulum; it is, therefore, a particularly instructive model to understand both the protein routing and the molecular mechanisms, whereby pharmacoperones rescue misfolded intermediates or conformationally defective receptors.
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