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Transporters in Health and Disease
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Transporters in Health and Disease

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Biology".

Deadline for manuscript submissions: 20 July 2025 | Viewed by 4211

Special Issue Editor

Prof. Dr. Giuliano Ciarimboli

E-Mail Website
Guest Editor
Experimental Nephrology, Department of Internal Medicine D, University Hospital Münster, 48149 Münster, Germany
Interests: transporters; regulation; kidneys; drugs; toxicity; physiology; polarity; chemotherapeutics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Transporter proteins play a crucial role in maintaining cellular physiology, metabolism, and signaling by facilitating the movement of water and various solutes, such as inorganic and organic ions, hormones, amino acids, sugars, and other substances, across biological membranes. Additionally, they can mediate the transport of environmental toxins, xenobiotics, and drugs across the plasma membrane. This is particularly important for hydrophilic drugs, which often rely on transporters to reach their target sites or be effectively cleared from the body. Alterations in the function or expression of these transporters can lead to cellular dysfunction and contribute to the development of diseases. Conversely, the presence of disease can also impact the expression and function of transporters. For instance, the dysregulation of the renal epithelial sodium channel can increase sodium and water reabsorption in the kidneys, leading to hypertension, as observed in Liddle's syndrome, while changes in transporter expression can affect drug pharmacokinetics and toxicity.

This Special Issue will compile the latest insights into the role of transporters in health and disease and their pharmacological and toxicological implications. We invite submissions of original research articles and reviews.

Prof. Dr. Giuliano Ciarimboli
Guest Editor

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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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

  • transporters
  • disease
  • regulation
  • drugs
  • toxicity
  • signaling

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Published Papers (3 papers)

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12 pages, 5236 KiB  
Article
Are Δ9-Tetrahydrocannabinol and Its Major Metabolites Substrates or Inhibitors of Placental or Human Hepatic Drug Solute-Carrier Transporters?
by Xin Chen, Zsuzsanna Gáborik, Qingcheng Mao and Jashvant D. Unadkat
Int. J. Mol. Sci. 2024, 25(22), 12036; https://doi.org/10.3390/ijms252212036 - 9 Nov 2024
Viewed by 1075
Abstract
Δ9-Tetrahydrocannabinol (THC) is the primary psychoactive component of cannabis which is being increasingly consumed by pregnant people. In humans, THC is sequentially metabolized in the liver to its circulating metabolites 11-hydroxy-THC (11-OH-THC, psychoactive) and 11-nor-9-carboxy-THC (THC-COOH, non-psychoactive). Human and [...] Read more.
Δ9-Tetrahydrocannabinol (THC) is the primary psychoactive component of cannabis which is being increasingly consumed by pregnant people. In humans, THC is sequentially metabolized in the liver to its circulating metabolites 11-hydroxy-THC (11-OH-THC, psychoactive) and 11-nor-9-carboxy-THC (THC-COOH, non-psychoactive). Human and macaque data show that fetal exposure to THC is considerably lower than the corresponding maternal exposure. Through perfused human placenta studies, we showed that this is due to the active efflux of THC (fetal-to-maternal) by a placental transporter(s) other than P-glycoprotein or breast cancer resistance protein. The identity of this placental transporter(s) as well as whether THC or its metabolites are substrates or inhibitors of hepatic solute carrier transporters is unknown. Therefore, we investigated whether 5 μM THC, 0.3 μM 11-OH-THC, and 2.5 μM THC-COOH are substrates and/or inhibitors of placental or hepatic solute carrier transporters at their pharmacologically relevant concentrations. Using HEK cells overexpressing human OATP1B1, OATP1B3, OATP2B1, OCT1, OCT3, OAT2, OAT4, or NTCP, and prototypic substrates/inhibitors of these transporters, we found that THC and THC-COOH were substrates but not inhibitors of OCT1. THC-COOH was a weak substrate of OCT3 and a weak inhibitor of OAT4. THC, 11-OH-THC, and THC-COOH were found not to be substrates/inhibitors of the remaining transporters investigated. Full article
(This article belongs to the Special Issue Transporters in Health and Disease)
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12 pages, 3594 KiB  
Article
Impairment of Skeletal Muscle Contraction by Inhibitors of GABA Transporters
by Nikita S. Fedorov, Guzel V. Sibgatullina and Artem I. Malomouzh
Int. J. Mol. Sci. 2024, 25(23), 12510; https://doi.org/10.3390/ijms252312510 - 21 Nov 2024
Viewed by 1233
Abstract
γ-Aminobutyric acid (GABA) has a significant impact on the functioning of not only the central but also the peripheral part of the nervous system. Recently, various elements of the GABAergic signaling system have been discovered in the area of the neuromuscular junction of [...] Read more.
γ-Aminobutyric acid (GABA) has a significant impact on the functioning of not only the central but also the peripheral part of the nervous system. Recently, various elements of the GABAergic signaling system have been discovered in the area of the neuromuscular junction of mammals. At the same time, the functional activity of membrane-bound GABA transporters (GATs) and their role in neuromuscular transmission have not been identified. In the present study, performed on a neuromuscular preparation of the mouse diaphragm, the effect of GABA transporter inhibitors (nipecotic acid and β-alanine) on the force of muscle contraction was assessed. It was found that in the presence of both compounds in the bathing solution, the force of contractions caused by stimulation of the motor nerve dropped by 30–50%. However, when the muscle was stimulated directly, no effect of GABA transporter inhibitors on the contractile force was observed. The depressant effect of β-alanine induced by nerve stimulation was completely abolished by the GABAB receptor blocker CGP 55845. GABA transporters were detected at the neuromuscular junction using immunohistochemistry. Thus, our results indicate that GABA transporters are localized in the area of the neuromuscular junction, and their activity affects the muscle contraction force. This influence is most likely due to the removal of GABA released during nerve stimulation and activating GABA receptors, which leads to a decrease in the contraction force of the striated muscles. Full article
(This article belongs to the Special Issue Transporters in Health and Disease)
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17 pages, 1741 KiB  
Article
Effect of Organic Anion Transporting Polypeptide 1B1 on Plasma Concentration Dynamics of Clozapine in Patients with Treatment-Resistant Schizophrenia
by Toshihiro Sato, Takeshi Kawabata, Masaki Kumondai, Nagomi Hayashi, Hiroshi Komatsu, Yuki Kikuchi, Go Onoguchi, Yu Sato, Kei Nanatani, Masahiro Hiratsuka, Masamitsu Maekawa, Hiroaki Yamaguchi, Takaaki Abe, Hiroaki Tomita and Nariyasu Mano
Int. J. Mol. Sci. 2024, 25(23), 13228; https://doi.org/10.3390/ijms252313228 - 9 Dec 2024
Viewed by 1431
Abstract
The involvement of drug-metabolizing enzymes and transporters in plasma clozapine (CLZ) dynamics has not been well examined in Japanese patients with treatment-resistant schizophrenia (TRS). Therefore, this clinical study investigated the relationship between single nucleotide polymorphisms (SNPs) of various pharmacokinetic factors (drug-metabolizing enzymes and [...] Read more.
The involvement of drug-metabolizing enzymes and transporters in plasma clozapine (CLZ) dynamics has not been well examined in Japanese patients with treatment-resistant schizophrenia (TRS). Therefore, this clinical study investigated the relationship between single nucleotide polymorphisms (SNPs) of various pharmacokinetic factors (drug-metabolizing enzymes and transporters) and dynamic changes in CLZ. Additionally, we aimed to determine whether CLZ acts as a substrate for pharmacokinetic factors using in vitro assays and molecular docking calculations. We found that 6 out of 10 patients with TRS and with multiple organic anion transporting polypeptide (OATP) variants (OATP1B1: *1b, *15; OATP1B3: 334T>G, 699G>A; and OATP2B1: *3, 935G>A, 601G>A, 76_84del) seemed to be highly exposed to CLZ and/or N-desmethyl CLZ. A CLZ uptake study using OATP-expressing HEK293 cells showed that CLZ was a substrate of OATP1B1 with Km and Vmax values of 38.9 µM and 2752 pmol/mg protein/10 min, respectively. The results of molecular docking calculations supported the differences in CLZ uptake among OATP molecules and the weak inhibitory effect of cyclosporine A, which is a strong inhibitor of OATPs, on CLZ uptake via OATP1B1. This is the first study to show that CLZ is an OATP1B1 substrate and that the presence of SNPs in OATPs potentially alters CLZ pharmacokinetic parameters. Full article
(This article belongs to the Special Issue Transporters in Health and Disease)
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