Abstract
The progesterone receptor (PR) is a ligand-activated steroid receptor in the nuclear receptor (NR) superfamily of transcription factor. Besides gynecological and obstetrical indications, the involvement/mechanism of PR in many other diseases, such as oncology, neurology, immunology, etc. has been revealed and studied in recent decades. Therapeutic agents that selectively activate or inhibit PR have been developed. PR agonists have generally been used in oral contraception and postmenopausal hormone replacement therapy (HRT), typically in combination with estrogens. PR antagonists and selective PR modulators (SPRMs) can be useful therapies for hormone dependent breast and prostate cancers, nonmalignant chronic conditions such as fibroids, and endometriosis. This review provides an overview and detailed discussions about the recent development of chemical structures of the PR ligands, their structural characteristics (particularly those contributing to their activity and selectivity), in vitro/in vivo studies and clinical trial outcomes, and the synthetic methodologies.
Keywords: Agonist, Antagonist, Ligand, Modulator, Nonsteroid, Progesterone receptor, Steroid.
Current Medicinal Chemistry
Title:Current Progresses and Trends in the Development of Progesterone Receptor Modulators
Volume: 23 Issue: 23
Author(s): Wenlu Li, Xi Li, Bin Zhang, Chunmei Gao, Yuzong Chen and Yuyang Jiang
Affiliation:
Keywords: Agonist, Antagonist, Ligand, Modulator, Nonsteroid, Progesterone receptor, Steroid.
Abstract: The progesterone receptor (PR) is a ligand-activated steroid receptor in the nuclear receptor (NR) superfamily of transcription factor. Besides gynecological and obstetrical indications, the involvement/mechanism of PR in many other diseases, such as oncology, neurology, immunology, etc. has been revealed and studied in recent decades. Therapeutic agents that selectively activate or inhibit PR have been developed. PR agonists have generally been used in oral contraception and postmenopausal hormone replacement therapy (HRT), typically in combination with estrogens. PR antagonists and selective PR modulators (SPRMs) can be useful therapies for hormone dependent breast and prostate cancers, nonmalignant chronic conditions such as fibroids, and endometriosis. This review provides an overview and detailed discussions about the recent development of chemical structures of the PR ligands, their structural characteristics (particularly those contributing to their activity and selectivity), in vitro/in vivo studies and clinical trial outcomes, and the synthetic methodologies.
Export Options
About this article
Cite this article as:
Li Wenlu, Li Xi, Zhang Bin, Gao Chunmei, Chen Yuzong and Jiang Yuyang, Current Progresses and Trends in the Development of Progesterone Receptor Modulators, Current Medicinal Chemistry 2016; 23 (23) . https://dx.doi.org/10.2174/0929867323666160428105310
DOI https://dx.doi.org/10.2174/0929867323666160428105310 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Oncogenomic Approaches in Exploring Gain of Function of Mutant p53
Current Genomics Tumor Biomarkers: Clinical Utility, Promises and Problems
Applied Clinical Research, Clinical Trials and Regulatory Affairs Pain and Child: A Translational Hypothesis on the Pathophysiology of a Mild Type-2 Diabetes Model
Endocrine, Metabolic & Immune Disorders - Drug Targets Cell Cycle Inhibition in Malignant Lymphoma: Disease Control by Attacking the Cellular Proliferation Machinery
Current Drug Targets Pathophysiology of Metastatic Bone Disease and the Role of the Second Generation of Bisphosphonates: From Basic Science to Medicine
Current Pharmaceutical Design Meet Our Editorial Board Member
Current Cancer Therapy Reviews Patented Biomarkers for the Early Detection of Ovarian Cancer
Recent Patents on Biomarkers 25-hydroxyvitamin D Correlation with Prolactin Levels and Adenoma Size in Female Patients with Newly Diagnosed Prolactin Secreting Adenoma
Endocrine, Metabolic & Immune Disorders - Drug Targets Fragment-Based Discovery of Inhibitors of Protein Kinase B
Current Topics in Medicinal Chemistry <i>Propionibacterium acnes</i> in the Pathogenesis and Immunotherapy of Acne Vulgaris
Current Drug Metabolism Lectin Glycoarray Technologies for Nanoscale Biomedical Detection
Protein & Peptide Letters DNA-Binding Properties of Poly(ADP-Ribose) Polymerase: A Target for Anti-Cancer Therapy
Current Drug Targets AKT Signaling in Regulating Angiogenesis
Current Cancer Drug Targets Anti-inflammatory Property of AMP-activated Protein Kinase
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Drugs of Abuse and Oxidative Stress in the Brain: From Animal Models to Human Evidence
Mini-Reviews in Organic Chemistry Recent Development in Targeting PI3K-Akt-mTOR Signaling for Anticancer Therapeutic Strategies
Anti-Cancer Agents in Medicinal Chemistry Anti-inflammatory Phytochemicals for Chemoprevention of Colon Cancer
Current Cancer Drug Targets Viruses in Semen and Male Genital Tissues - Consequences for the Reproductive System and Therapeutic Perspectives
Current Pharmaceutical Design Synthesis of Novel Steroid Derivatives Derived from Dehydroepiandrosterone as Potential Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry The Impact of the Theory-Based Training on Beliefs of Women towards Breast Cancer Screening Behaviors
Current Women`s Health Reviews