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Biomolecules
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Advances in β3-Adrenoceptor
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Advances in β3-Adrenoceptor

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Molecular Biology".

Deadline for manuscript submissions: 30 September 2024 | Viewed by 5861

Special Issue Editors

Dr. Alessandro Pini

E-Mail Website
Guest Editor
Department of Experimental and Clinical Medicine, Section of Anatomy and Histology, University of Florence, Viale Pieraccini, 6, 50139 Florence, Italy
Interests: β3-adrenoceptor; preterm delivery; fetus; cell differentiation; morphogenesis; hypoxia; diabetes; histamine; histology; tissue inflammation and remodelling; fibrosis
Dr. Luca Filippi

E-Mail Website
Guest Editor
Department of Clinical and Experimental Medicine, University of Pisa, Via Savi, 10, 56126 Pisa, Italy
Interests: β-adrenoceptors, hypoxia; preterm delivery; pregnancy; childbirth; postpartum period; cancer; retinopathy of prematurity; hemangiomas; propranolol; foetus

Special Issue Information

Dear Colleagues,

Since its discovery in 1989, β3-AR has been found to be abundantly expressed in restricted adult healthy human tissues, such as adipose tissue, the urinary tract, and the cardiovascular and nervous system. Ever since then, numerous studies have contributed to revealing, at least in part, the signalling pathways and the biological functions that β3-AR mediates. Its presence was also demonstrated during intrauterine life and in near-term myometrium, suggesting a role for β3-AR in morphogenesis and in the management of preterm labor. New aspects of β3-AR have recently been described, where it has been demonstrated to have neuroprotective properties and to be highly expressed in different malignant tumors. The involvement in cancer initiation/progression makes this receptor an intriguing target for novel antineoplastic approaches. Its restricted tissue presence and low tendency to desensitization appoint β3-AR as a therapeutic target for chronic treatments with low systemic off-target effects. However, maybe as a consequence of the interspecies differences, the role of β3-AR in humans and its clinical implications still remain controversial, limited to overactive bladder treatment. This Special Issue welcomes original research and reviews pertaining to all β3-AR aspects and represents a platform for researchers to contribute to the understanding of its biological effects and potential therapeutic applications.

Dr. Alessandro Pini
Dr. Luca Filippi
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Biomolecules is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • β3-adrenoceptor
  • cardiovascular diseases
  • cancer
  • prematurity
  • hypoxia/hyperoxia
  • neurodegenerative diseases
  • retinopathy

Published Papers (4 papers)

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Research

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17 pages, 3855 KiB  
Article
β3 Adrenoceptor Agonism Prevents Hyperoxia-Induced Colonic Alterations
by Luca Filippi, Patrizia Nardini, Virginia Zizi, Marta Molino, Camilla Fazi, Maura Calvani, Francesco Carrozzo, Giacomo Cavallaro, Giorgia Giuseppetti, Laura Calosi, Olivia Crociani and Alessandro Pini
Biomolecules 2023, 13(12), 1755; https://doi.org/10.3390/biom13121755 - 6 Dec 2023
Cited by 1 | Viewed by 941
Abstract
Oxygen level is a key regulator of organogenesis and its modification in postnatal life alters the maturation process of organs, including the intestine, which do not completely develop in utero. The β3-adrenoreceptor (β3-AR) is expressed in the colon and has an oxygen-dependent regulatory [...] Read more.
Oxygen level is a key regulator of organogenesis and its modification in postnatal life alters the maturation process of organs, including the intestine, which do not completely develop in utero. The β3-adrenoreceptor (β3-AR) is expressed in the colon and has an oxygen-dependent regulatory mechanism. This study shows the effects of the β3-AR agonist BRL37344 in a neonatal model of hyperoxia-driven colonic injury. For the first 14 days after birth, Sprague–Dawley rat pups were exposed to ambient oxygen levels (21%) or hyperoxia (85%) and treated daily with BRL37344 at 1, 3, 6 mg/kg or untreated. At the end of day 14, proximal colon samples were collected for analysis. Hyperoxia deeply influences the proximal colon development by reducing β3-AR-expressing cells (27%), colonic length (26%) and mucin production (47%), and altering the neuronal chemical coding in the myenteric plexus without changes in the neuron number. The administration of BRL37344 at 3 mg/kg, but not at 1 mg/kg, significantly prevented these alterations. Conversely, it was ineffective in preventing hyperoxia-induced body weight loss. BRL37344 at 6 mg/kg was toxic. These findings pave the way for β3-AR pharmacological targeting as a therapeutic option for diseases caused by hyperoxia-impaired development, typical prematurity disorders. Full article
(This article belongs to the Special Issue Advances in β3-Adrenoceptor)
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Review

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29 pages, 1514 KiB  
Review
Inside the Biology of the β3-Adrenoceptor
by Amada Pasha, Annalisa Tondo, Claudio Favre and Maura Calvani
Biomolecules 2024, 14(2), 159; https://doi.org/10.3390/biom14020159 - 29 Jan 2024
Viewed by 1443
Abstract
Since the first discovery in 1989, the β3-adrenoceptor (β3-AR) has gained great attention because it showed the ability to regulate many physiologic and metabolic activities, such as thermogenesis and lipolysis in brown and white adipose tissue, respectively (BAT, WAT), negative inotropic effects in [...] Read more.
Since the first discovery in 1989, the β3-adrenoceptor (β3-AR) has gained great attention because it showed the ability to regulate many physiologic and metabolic activities, such as thermogenesis and lipolysis in brown and white adipose tissue, respectively (BAT, WAT), negative inotropic effects in cardiomyocytes, and relaxation of the blood vessels and the urinary bladder. The β3-AR has been suggested as a potential target for cancer treatment, both in adult and pediatric tumors, since under hypoxia its upregulation in the tumor microenvironment (TME) regulates stromal cell differentiation, tumor growth and metastases, signifying that its agonism/antagonism could be useful for clinical benefits. Promising results in cancer research have proposed the β3-AR being targeted for the treatment of many conditions, with some drugs, at present, undergoing phase II and III clinical trials. In this review, we report the scientific journey followed by the research from the β3-Ars’ discovery, with focus on the β3-Ars’ role in cancer initiation and progression that elects it an intriguing target for novel antineoplastic approaches. The overview highlights the great potential of the β3-AR, both in physiologic and pathologic conditions, with the intention to display the possible benefits of β3-AR modulation in cancer reality. Full article
(This article belongs to the Special Issue Advances in β3-Adrenoceptor)
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24 pages, 993 KiB  
Review
Is the β3-Adrenoceptor a Valid Target for the Treatment of Obesity and/or Type 2 Diabetes?
by Haneen S. Dwaib and Martin C. Michel
Biomolecules 2023, 13(12), 1714; https://doi.org/10.3390/biom13121714 - 28 Nov 2023
Viewed by 1611
Abstract
β3-Adrenoceptors mediate several functions in rodents that could be beneficial for the treatment of obesity and type 2 diabetes. This includes promotion of insulin release from the pancreas, cellular glucose uptake, lipolysis, and thermogenesis in brown adipose tissue. In combination, they [...] Read more.
β3-Adrenoceptors mediate several functions in rodents that could be beneficial for the treatment of obesity and type 2 diabetes. This includes promotion of insulin release from the pancreas, cellular glucose uptake, lipolysis, and thermogenesis in brown adipose tissue. In combination, they lead to a reduction of body weight in several rodent models including ob/ob mice and Zucker diabetic fatty rats. These findings stimulated drug development programs in various pharmaceutical companies, and at least nine β3-adrenoceptor agonists have been tested in clinical trials. However, all of these projects were discontinued due to the lack of clinically relevant changes in body weight. Following a concise historical account of discoveries leading to such drug development programs we discuss species differences that explain why β3-adrenoceptors are not a meaningful drug target for the treatment of obesity and type 2 diabetes in humans. Full article
(This article belongs to the Special Issue Advances in β3-Adrenoceptor)
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13 pages, 870 KiB  
Review
β3 Receptor Signaling in Pregnant Human Myometrium Suggests a Role for β3 Agonists as Tocolytics
by Iain L. O. Buxton, Hazik Asif and Scott D. Barnett
Biomolecules 2023, 13(6), 1005; https://doi.org/10.3390/biom13061005 - 17 Jun 2023
Cited by 1 | Viewed by 1518
Abstract
Preterm labor leading to preterm birth is the leading cause of infant morbidity and mortality. At the present time, nothing can reliably halt labor once it begins. The knowledge that agonists of the β2 adrenergic receptor relax airway smooth muscle and are effective [...] Read more.
Preterm labor leading to preterm birth is the leading cause of infant morbidity and mortality. At the present time, nothing can reliably halt labor once it begins. The knowledge that agonists of the β2 adrenergic receptor relax airway smooth muscle and are effective in the treatment of asthma led to the notion that β2 mimetics would prevent preterm birth by relaxing uterine smooth muscle. The activation of cAMP-dependent protein kinase by β2 receptors is unable to provide meaningful tocolysis. The failure of β2 agonists such as ritodrine and terbutaline to prevent preterm birth suggests that the regulation of uterine smooth muscle is disparate from that of airway. Other smooth muscle quiescent-mediating molecules, such as nitric oxide, relax vascular smooth muscle in a cGMP-protein kinase G-dependent manner; however, nitric oxide activation of protein kinase G fails to explain the relaxation of the myometrium to nitric oxide. Moreover, nitric oxide-mediated relaxation is blunted in preterm labor, and thus, for this reason and because of the fall in maternal blood pressure, nitric oxide cannot be employed as a tocolytic. The β3 adrenergic receptor-mediated relaxation of the human myometrium is claimed to be cAMP-dependent protein kinase-dependent. This is scientifically displeasing given the failure of β2 agonists as tocolytics and suggests a non-canonical signaling role for β3AR in myometrium. The addition of the β3 agonist mirabegron to pregnant human myometrial strips in the tissue bath relaxes oxytocin-induced contractions. Mirabegron stimulates nitric oxide production in myometrial microvascular endothelial cells, and the relaxation of uterine tissue in vitro is partially blocked by the addition of the endothelial nitric oxide synthase blocker Nω-Nitro-L-arginine. Recent data suggest that both endothelial and smooth muscle cells respond to β3 stimulation and contribute to relaxation through disparate signaling pathways. The repurposing of approved medications such as mirabegron (Mybetriq™) tested in human myometrium as uterine tocolytics can advance the prevention of preterm birth. Full article
(This article belongs to the Special Issue Advances in β3-Adrenoceptor)
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