Progesterone receptor blockers : historical perspective, mode of function and insights into clinical and scientific applications
Thieme. All rights reserved..
Antigestagens (antiprogestins) are functional competitors of progesterone (P4) that prevent P4 from mediating its biological functions either by suppressing its production or blocking its function. Among the latter are progesterone antagonists, competitors of P4 binding to its nuclear receptor PGR, which have found application in both human and veterinary medicine, in particular in small animal practice for the prevention of nidation and the interruption of pregnancy. Depending on their mode of action, progesterone receptor antagonists can be divided into 2 classes. Class I antagonists bind to the PGR but fail to induce its binding to promoters of target genes (competitive inhibitors). Class II antigestagens, including aglepristone used in veterinary medicine, bind to the PGR, activate its association with a promoter, but interfere with the downstream signalling cascades, e. g., by recruiting transcriptional repressors. They act thereby as transdominant repressors exerting negative effects on target gene expression. Importantly for experimental sciences, as active antagonists, class II antagonists do not require the presence of the natural ligand for their action. Besides their clinical application, antigestagens are used in research for investigating P4-dependent physiological and pathological processes. Here an overview of the history and the current usage of progesterone receptor antagonists in veterinary medicine and research is presented.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:48 |
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| Enthalten in: |
Tierarztliche Praxis. Ausgabe K, Kleintiere/Heimtiere - 48(2020), 6 vom: 11. Dez., Seite 433-440 |
| Sprache: |
Englisch |
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| Weiterer Titel: |
Progesteronrezeptorblocker: historische Perspektive, Funktionsweise und Einblicke in klinische und wissenschaftliche Anwendungen |
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| Beteiligte Personen: |
Kowalewski, Mariusz P [VerfasserIn] |
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| Links: |
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| Themen: |
Hormone Antagonists |
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| Anmerkungen: |
Date Completed 10.05.2021 Date Revised 10.05.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1055/a-1274-9290 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM318423952 |
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| 245 | 1 | 0 | |a Progesterone receptor blockers |b historical perspective, mode of function and insights into clinical and scientific applications |
| 246 | 3 | 3 | |a Progesteronrezeptorblocker: historische Perspektive, Funktionsweise und Einblicke in klinische und wissenschaftliche Anwendungen |
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| 500 | |a Date Completed 10.05.2021 | ||
| 500 | |a Date Revised 10.05.2021 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Thieme. All rights reserved. | ||
| 520 | |a Antigestagens (antiprogestins) are functional competitors of progesterone (P4) that prevent P4 from mediating its biological functions either by suppressing its production or blocking its function. Among the latter are progesterone antagonists, competitors of P4 binding to its nuclear receptor PGR, which have found application in both human and veterinary medicine, in particular in small animal practice for the prevention of nidation and the interruption of pregnancy. Depending on their mode of action, progesterone receptor antagonists can be divided into 2 classes. Class I antagonists bind to the PGR but fail to induce its binding to promoters of target genes (competitive inhibitors). Class II antigestagens, including aglepristone used in veterinary medicine, bind to the PGR, activate its association with a promoter, but interfere with the downstream signalling cascades, e. g., by recruiting transcriptional repressors. They act thereby as transdominant repressors exerting negative effects on target gene expression. Importantly for experimental sciences, as active antagonists, class II antagonists do not require the presence of the natural ligand for their action. Besides their clinical application, antigestagens are used in research for investigating P4-dependent physiological and pathological processes. Here an overview of the history and the current usage of progesterone receptor antagonists in veterinary medicine and research is presented | ||
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| 650 | 7 | |a Receptors, Progesterone |2 NLM | |
| 650 | 7 | |a Veterinary Drugs |2 NLM | |
| 700 | 1 | |a Pereira, Miguel Tavares |e verfasserin |4 aut | |
| 700 | 1 | |a Papa, Paula |e verfasserin |4 aut | |
| 700 | 1 | |a Gram, Aykut |e verfasserin |4 aut | |
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