Nuclear receptors are a pivotal family of 48 transcription factors in humans that orchestrate the regulation of gene networks integral to metabolism, inflammation, and circadian rhythm. Their multifaceted roles make them prime therapeutic targets for a spectrum of diseases, including metabolic disorders, inflammatory conditions, and cancers. Traditional drug development has predominantly focused on ligands, such as agonists and antagonists, to modulate these receptors. However, recent advancements have introduced innovative strategies like epigenetic modifications and PROTACs (Proteolysis Targeting Chimeras), underscoring the evolving landscape of this research domain. Despite these advancements, challenges persist, including limited clinical efficacy and potential side effects of drug candidates. Addressing these issues is crucial for advancing therapeutic interventions, and there is a pressing need for novel strategies and breakthroughs to enhance the efficacy and safety of nuclear receptor-targeted therapies.
This research topic aims to explore and reflect on the current status and recent progress in drug development strategies targeting nuclear receptors, particularly for metabolic diseases. The primary objective is to address the challenges of limited clinical efficacy and potential side effects by showcasing novel strategies and breakthroughs in the field. Specific questions include understanding the mechanisms underlying the limited transcriptional activity of certain nuclear receptors and exploring innovative approaches to enhance their therapeutic potential.
To gather further insights into the regulation and drug development of nuclear receptors, we welcome articles addressing, but not limited to, the following themes:
- Discovery or development of novel ligands targeting nuclear receptors, including agonists or antagonists from natural products or endogenous metabolites.
- Novel strategies targeting nuclear receptors, such as dual agonists and PROTACs.
- New functions and mechanisms of nuclear receptors in metabolic diseases.
- Non-genomic functions of nuclear receptors and their contribution to metabolic diseases.
- Mechanisms underlying the limited transcriptional activity and functions of nuclear receptors.
- Clinical trials detailing the efficacy, safety, and outcomes of candidates targeting nuclear receptors.
Keywords:
Nuclear receptors, regulation, drug development
Important Note:
All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.
Nuclear receptors are a pivotal family of 48 transcription factors in humans that orchestrate the regulation of gene networks integral to metabolism, inflammation, and circadian rhythm. Their multifaceted roles make them prime therapeutic targets for a spectrum of diseases, including metabolic disorders, inflammatory conditions, and cancers. Traditional drug development has predominantly focused on ligands, such as agonists and antagonists, to modulate these receptors. However, recent advancements have introduced innovative strategies like epigenetic modifications and PROTACs (Proteolysis Targeting Chimeras), underscoring the evolving landscape of this research domain. Despite these advancements, challenges persist, including limited clinical efficacy and potential side effects of drug candidates. Addressing these issues is crucial for advancing therapeutic interventions, and there is a pressing need for novel strategies and breakthroughs to enhance the efficacy and safety of nuclear receptor-targeted therapies.
This research topic aims to explore and reflect on the current status and recent progress in drug development strategies targeting nuclear receptors, particularly for metabolic diseases. The primary objective is to address the challenges of limited clinical efficacy and potential side effects by showcasing novel strategies and breakthroughs in the field. Specific questions include understanding the mechanisms underlying the limited transcriptional activity of certain nuclear receptors and exploring innovative approaches to enhance their therapeutic potential.
To gather further insights into the regulation and drug development of nuclear receptors, we welcome articles addressing, but not limited to, the following themes:
- Discovery or development of novel ligands targeting nuclear receptors, including agonists or antagonists from natural products or endogenous metabolites.
- Novel strategies targeting nuclear receptors, such as dual agonists and PROTACs.
- New functions and mechanisms of nuclear receptors in metabolic diseases.
- Non-genomic functions of nuclear receptors and their contribution to metabolic diseases.
- Mechanisms underlying the limited transcriptional activity and functions of nuclear receptors.
- Clinical trials detailing the efficacy, safety, and outcomes of candidates targeting nuclear receptors.
Keywords:
Nuclear receptors, regulation, drug development
Important Note:
All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.