Therapeutic approaches targeting the neurotensin receptors
العنوان: | Therapeutic approaches targeting the neurotensin receptors |
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المؤلفون: | George Kunos, Malliga R. Iyer |
المصدر: | Expert Opinion on Therapeutic Patents. 31:361-386 |
بيانات النشر: | Informa UK Limited, 2021. |
سنة النشر: | 2021 |
مصطلحات موضوعية: | Neurotensin receptor 1, Neurotensin receptor 2, Neuropeptide, Biology, 01 natural sciences, Patents as Topic, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Drug Discovery, Animals, Humans, Receptors, Neurotensin, Molecular Targeted Therapy, Receptor, Neurotransmitter, Neurotensin, Pharmacology, Drug discovery, Translation (biology), Receptor Cross-Talk, General Medicine, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, chemistry, 030220 oncology & carcinogenesis, Neuroscience |
الوصف: | Introduction: Neurotensin is a gut-brain peptide hormone, a 13 amino acid neuropeptide found in the central nervous system and in the GI tract. The neurotensinergic system is implicated in various physiological and pathological processes related to neuropsychiatric and metabolic machineries, cancer growth, food, and drug intake. NT mediates its functions through its two G protein-coupled receptors: neurotensin receptor 1 (NTS1/NTSR1) and neurotensin receptor 2 (NTS2/NTSR2). Over the past decade, the role of NTS3/NTSR3/sortilin has also gained importance in human pathologies. Several approaches have appeared dealing with the discovery of compounds able to modulate the functions of this neuropeptide through its receptors for therapeutic gain.Areas covered: The article provides an overview of over four decades of research and details the drug discovery approaches and patented strategies targeting NTSR in the past decade.Expert opinion: Neurotensin is an important neurotransmitter that enables crosstalk with various neurotransmitter and neuroendocrine systems. While significant efforts have been made that have led to selective agonists and antagonists with promising in vitro and in vivo activities, the therapeutic potential of compounds targeting the neurotensinergic system is still to be fully harnessed for successful clinical translation of compounds for the treatment of several pathologies. |
تدمد: | 1744-7674 1354-3776 |
URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6a7ca5b615dc3afa4c2aa6b9f3b5ffb https://doi.org/10.1080/13543776.2021.1866539 |
رقم الأكسشن: | edsair.doi.dedup.....f6a7ca5b615dc3afa4c2aa6b9f3b5ffb |
قاعدة البيانات: | OpenAIRE |
تدمد: | 17447674 13543776 |
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