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Latest Review Papers in Molecular Pharmacology 2023

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

Deadline for manuscript submissions: closed (31 March 2023) | Viewed by 74053

Special Issue Editor

Dr. Anastasios Lymperopoulos

E-Mail Website
Guest Editor
Laboratory for the Study of Neurohormonal Control of the Circulation, Department of Pharmaceutical Sciences, Nova Southeastern University, Fort Lauderdale, FL 33328-2018, USA
Interests: cardiovascular G protein-coupled receptors (GPCRs); heart failure; autonomic control of the circulation; adrenal physiology and pharmacology; adrenergic receptors; angiotensin receptors; signal transduction; gene therapy; aldosterone pharmacology; GPCR-Kinases; arrestins; G protein signaling
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Dear Colleagues, 

This Special Issue aims to collect high quality review papers in all topics of molecular pharmacology. We encourage researchers from related fields to contribute review papers highlighting the latest developments in molecular pharmacology, or to invite relevant experts and colleagues to do so. Comprehensive, authoritative reviews are strongly encouraged.

Dr. Anastasios Lymperopoulos
Guest Editor

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Published Papers (15 papers)

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Review

22 pages, 1541 KiB  
Review
Medicinally Privileged Natural Chalcones: Abundance, Mechanisms of Action, and Clinical Trials
by Sophia M. Villa, Justin Heckman and Debasish Bandyopadhyay
Int. J. Mol. Sci. 2024, 25(17), 9623; https://doi.org/10.3390/ijms25179623 - 5 Sep 2024
Viewed by 1162
Abstract
Chalcones have been utilized for centuries as foods and medicines across various cultures and traditions worldwide. This paper concisely overviews their biosynthesis as specialized metabolites in plants and their significance, potential, efficacy, and possibility as future medicines. This is followed by a more [...] Read more.
Chalcones have been utilized for centuries as foods and medicines across various cultures and traditions worldwide. This paper concisely overviews their biosynthesis as specialized metabolites in plants and their significance, potential, efficacy, and possibility as future medicines. This is followed by a more in-depth exploration of naturally occurring chalcones and their corresponding mechanisms of action in human bodies. Based on their mechanisms of action, chalcones exhibit many pharmacological properties, including antioxidant, anti-inflammatory, anticancer, antimalarial, antiviral, and antibacterial properties. Novel naturally occurring chalcones are also recognized as potential antidiabetic drugs, and their effect on the GLUT-4 transporter is investigated. In addition, they are examined for their anti-inflammatory effects, focusing on chalcones used for future pharmaceutical utilization. Chalcones also bind to specific receptors and toxins that prevent bacterial and viral infections. Chalcones exhibit physiological protective effects on the biological degradation of different systems, including demyelinating neurodegenerative diseases and preventing hypertension or hyperlipidemia. Chalcones that are/were in clinical trials have been included as a separate section. By revealing the many biological roles of chalcones and their impact on medicine, this paper underlines the significance of naturally occurring chalcones and their extension to patient care, providing the audience with an index of topic-relevant information. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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42 pages, 12328 KiB  
Review
Iron–Imine Cocktail in Drug Development: A Contemporary Update
by Judith Anane, Esther Owusu, Gildardo Rivera and Debasish Bandyopadhyay
Int. J. Mol. Sci. 2024, 25(4), 2263; https://doi.org/10.3390/ijms25042263 - 13 Feb 2024
Viewed by 1769
Abstract
Organometallic drug development is still in its early stage, but recent studies show that organometallics having iron as the central atom have the possibility of becoming good drug candidates because iron is an important micro-nutrient, and it is compatible with many biological systems, [...] Read more.
Organometallic drug development is still in its early stage, but recent studies show that organometallics having iron as the central atom have the possibility of becoming good drug candidates because iron is an important micro-nutrient, and it is compatible with many biological systems, including the human body. Being an eco-friendly Lewis acid, iron can accept the lone pair of electrons from imino(sp2)-nitrogen, and the resultant iron–imine complexes with iron as a central atom have the possibility of interacting with several proteins and enzymes in humans. Iron–imine complexes have demonstrated significant potential with anticancer, bactericidal, fungicidal, and other medicinal activities in recent years. This article systematically discusses major synthetic methods and pharmacological potentials of iron–imine complexes having in vitro activity to significant clinical performance from 2016 to date. In a nutshell, this manuscript offers a simplistic view of iron complexes in medicinal inorganic chemistry: for instance, iron is presented as an “eco-friendly non-toxic” metal (as opposed to platinum) that will lead to non-toxic pharmaceuticals. The abundant literature on iron chelators shows that many iron complexes, particularly if redox-active in cells, can be quite cytotoxic, which can be beneficial for future targeted therapies. While we made every effort to include all the related papers, any omission is purely unintentional. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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23 pages, 2816 KiB  
Review
From Basic Research to Clinical Practice: Considerations for Treatment Drugs for Silicosis
by Rou Li, Huimin Kang and Shi Chen
Int. J. Mol. Sci. 2023, 24(9), 8333; https://doi.org/10.3390/ijms24098333 - 5 May 2023
Cited by 9 | Viewed by 3571
Abstract
Silicosis, characterized by irreversible pulmonary fibrosis, remains a major global public health problem. Nowadays, cumulative studies are focusing on elucidating the pathogenesis of silicosis in order to identify preventive or therapeutic antifibrotic agents. However, the existing research on the mechanism of silica-dust-induced pulmonary [...] Read more.
Silicosis, characterized by irreversible pulmonary fibrosis, remains a major global public health problem. Nowadays, cumulative studies are focusing on elucidating the pathogenesis of silicosis in order to identify preventive or therapeutic antifibrotic agents. However, the existing research on the mechanism of silica-dust-induced pulmonary fibrosis is only the tip of the iceberg and lags far behind clinical needs. Idiopathic pulmonary fibrosis (IPF), as a pulmonary fibrosis disease, also has the same problem. In this study, we examined the relationship between silicosis and IPF from the perspective of their pathogenesis and fibrotic characteristics, further discussing current drug research and limitations of clinical application in silicosis. Overall, this review provided novel insights for clinical treatment of silicosis with the hope of bridging the gap between research and practice in silicosis. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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21 pages, 1045 KiB  
Review
Protein Tyrosine Phosphatase Receptor Zeta 1 as a Potential Target in Cancer Therapy and Diagnosis
by Evangelia Papadimitriou and Vasiliki K. Kanellopoulou
Int. J. Mol. Sci. 2023, 24(9), 8093; https://doi.org/10.3390/ijms24098093 - 30 Apr 2023
Cited by 6 | Viewed by 3065
Abstract
Protein tyrosine phosphatase receptor zeta 1 (PTPRZ1) is a type V transmembrane tyrosine phosphatase that is highly expressed during embryonic development, while its expression during adulthood is limited. PTPRZ1 is highly detected in the central nervous system, affecting oligodendrocytes’ survival and maturation. In [...] Read more.
Protein tyrosine phosphatase receptor zeta 1 (PTPRZ1) is a type V transmembrane tyrosine phosphatase that is highly expressed during embryonic development, while its expression during adulthood is limited. PTPRZ1 is highly detected in the central nervous system, affecting oligodendrocytes’ survival and maturation. In gliomas, PTPRZ1 expression is significantly upregulated and is being studied as a potential cancer driver and as a target for therapy. PTPRZ1 expression is also increased in other cancer types, but there are no data on the potential functional significance of this finding. On the other hand, low PTPRZ1 expression seems to be related to a worse prognosis in some cancer types, suggesting that in some cases, it may act as a tumor-suppressor gene. These discrepancies may be due to our limited understanding of PTPRZ1 signaling and tumor microenvironments. In this review, we present evidence on the role of PTPRZ1 in angiogenesis and cancer and discuss the phenomenal differences among the different types of cancer, depending on the regulation of its tyrosine phosphatase activity or ligand binding. Clarifying the involved signaling pathways will lead to its efficient exploitation as a novel therapeutic target or as a biomarker, and the development of proper therapeutic approaches. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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23 pages, 2113 KiB  
Review
A Systematic Review of Deep Learning Methodologies Used in the Drug Discovery Process with Emphasis on In Vivo Validation
by Nikoletta-Maria Koutroumpa, Konstantinos D. Papavasileiou, Anastasios G. Papadiamantis, Georgia Melagraki and Antreas Afantitis
Int. J. Mol. Sci. 2023, 24(7), 6573; https://doi.org/10.3390/ijms24076573 - 31 Mar 2023
Cited by 11 | Viewed by 5210
Abstract
The discovery and development of new drugs are extremely long and costly processes. Recent progress in artificial intelligence has made a positive impact on the drug development pipeline. Numerous challenges have been addressed with the growing exploitation of drug-related data and the advancement [...] Read more.
The discovery and development of new drugs are extremely long and costly processes. Recent progress in artificial intelligence has made a positive impact on the drug development pipeline. Numerous challenges have been addressed with the growing exploitation of drug-related data and the advancement of deep learning technology. Several model frameworks have been proposed to enhance the performance of deep learning algorithms in molecular design. However, only a few have had an immediate impact on drug development since computational results may not be confirmed experimentally. This systematic review aims to summarize the different deep learning architectures used in the drug discovery process and are validated with further in vivo experiments. For each presented study, the proposed molecule or peptide that has been generated or identified by the deep learning model has been biologically evaluated in animal models. These state-of-the-art studies highlight that even if artificial intelligence in drug discovery is still in its infancy, it has great potential to accelerate the drug discovery cycle, reduce the required costs, and contribute to the integration of the 3R (Replacement, Reduction, Refinement) principles. Out of all the reviewed scientific articles, seven algorithms were identified: recurrent neural networks, specifically, long short-term memory (LSTM-RNNs), Autoencoders (AEs) and their Wasserstein Autoencoders (WAEs) and Variational Autoencoders (VAEs) variants; Convolutional Neural Networks (CNNs); Direct Message Passing Neural Networks (D-MPNNs); and Multitask Deep Neural Networks (MTDNNs). LSTM-RNNs were the most used architectures with molecules or peptide sequences as inputs. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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16 pages, 1061 KiB  
Review
Cardiac RGS Proteins in Human Heart Failure and Atrial Fibrillation: Focus on RGS4
by Jordana I. Borges, Malka S. Suster and Anastasios Lymperopoulos
Int. J. Mol. Sci. 2023, 24(7), 6136; https://doi.org/10.3390/ijms24076136 - 24 Mar 2023
Cited by 6 | Viewed by 2662
Abstract
The regulator of G protein signaling (RGS) proteins are crucial for the termination of G protein signals elicited by G protein-coupled receptors (GPCRs). This superfamily of cell membrane receptors, by far the largest and most versatile in mammals, including humans, play pivotal roles [...] Read more.
The regulator of G protein signaling (RGS) proteins are crucial for the termination of G protein signals elicited by G protein-coupled receptors (GPCRs). This superfamily of cell membrane receptors, by far the largest and most versatile in mammals, including humans, play pivotal roles in the regulation of cardiac function and homeostasis. Perturbations in both the activation and termination of their G protein-mediated signaling underlie numerous heart pathologies, including heart failure (HF) and atrial fibrillation (AFib). Therefore, RGS proteins play important roles in the pathophysiology of these two devasting cardiac diseases, and several of them could be targeted therapeutically. Although close to 40 human RGS proteins have been identified, each RGS protein seems to interact only with a specific set of G protein subunits and GPCR types/subtypes in any given tissue or cell type. Numerous in vitro and in vivo studies in animal models, and also in diseased human heart tissue obtained from transplantations or tissue banks, have provided substantial evidence of the roles various cardiomyocyte RGS proteins play in cardiac normal homeostasis as well as pathophysiology. One RGS protein in particular, RGS4, has been reported in what are now decades-old studies to be selectively upregulated in human HF. It has also been implicated in protection against AFib via knockout mice studies. This review summarizes the current understanding of the functional roles of cardiac RGS proteins and their implications for the treatment of HF and AFib, with a specific focus on RGS4 for the aforementioned reasons but also because it can be targeted successfully with small organic molecule inhibitors. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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15 pages, 1866 KiB  
Review
Claudin-4: A New Molecular Target for Epithelial Cancer Therapy
by Rina Fujiwara-Tani, Shiori Mori, Ruiko Ogata, Rika Sasaki, Ayaka Ikemoto, Shingo Kishi, Masuo Kondoh and Hiroki Kuniyasu
Int. J. Mol. Sci. 2023, 24(6), 5494; https://doi.org/10.3390/ijms24065494 - 13 Mar 2023
Cited by 19 | Viewed by 4737
Abstract
Claudin-4 (CLDN4) is a key component of tight junctions (TJs) in epithelial cells. CLDN4 is overexpressed in many epithelial malignancies and correlates with cancer progression. Changes in CLDN4 expression have been associated with epigenetic factors (such as hypomethylation of promoter DNA), inflammation associated [...] Read more.
Claudin-4 (CLDN4) is a key component of tight junctions (TJs) in epithelial cells. CLDN4 is overexpressed in many epithelial malignancies and correlates with cancer progression. Changes in CLDN4 expression have been associated with epigenetic factors (such as hypomethylation of promoter DNA), inflammation associated with infection and cytokines, and growth factor signaling. CLDN4 helps to maintain the tumor microenvironment by forming TJs and acts as a barrier to the entry of anticancer drugs into tumors. Decreased expression of CLDN4 is a potential marker of epithelial-mesenchymal transition (EMT), and decreased epithelial differentiation due to reduced CLDN4 activity is involved in EMT induction. Non-TJ CLDN4 also activates integrin beta 1 and YAP to promote proliferation, EMT, and stemness. These roles in cancer have led to investigations of molecular therapies targeting CLDN4 using anti-CLDN4 extracellular domain antibodies, gene knockdown, clostridium perfringens enterotoxin (CPE), and C-terminus domain of CPE (C-CPE), which have demonstrated the experimental efficacy of this approach. CLDN4 is strongly involved in promoting malignant phenotypes in many epithelial cancers and is regarded as a promising molecular therapeutic target. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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17 pages, 4468 KiB  
Review
Structural Biology Inspired Development of a Series of Human Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Ligands: From Agonist to Antagonist
by Hiroyuki Miyachi
Int. J. Mol. Sci. 2023, 24(4), 3940; https://doi.org/10.3390/ijms24043940 - 15 Feb 2023
Cited by 7 | Viewed by 2333
Abstract
Recent progress in the structural and molecular pharmacological understanding of the nuclear receptor, peroxisome proliferator-activated receptor gamma (hPPARγ)—a transcription factor with pleiotropic effects on biological responses—has enabled the investigation of various graded hPPARγ ligands (full agonist, partial agonist, and antagonist). Such ligands are [...] Read more.
Recent progress in the structural and molecular pharmacological understanding of the nuclear receptor, peroxisome proliferator-activated receptor gamma (hPPARγ)—a transcription factor with pleiotropic effects on biological responses—has enabled the investigation of various graded hPPARγ ligands (full agonist, partial agonist, and antagonist). Such ligands are useful tools to investigate the functions of hPPARγ in detail and are also candidate drugs for the treatment of hPPARγ-mediated diseases, such as metabolic syndrome and cancer. This review summarizes our medicinal chemistry research on the design, synthesis, and pharmacological evaluation of a covalent-binding and non-covalent-binding hPPARγ antagonist, both of which have been created based on our working hypothesis of the helix 12 (H12) holding induction/inhibition concept. X-ray crystallographic analyses of our representative antagonists complexed with an hPPARγ ligand binding domain (LBD) indicated the unique binding modes of hPPARγ LBD, which are quite different from the binding modes observed for hPPARγ agonists and partial agonists. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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17 pages, 618 KiB  
Review
Kidney Drug Transporters in Pharmacotherapy
by Joanna Łapczuk-Romańska, Maria Droździk, Stefan Oswald and Marek Droździk
Int. J. Mol. Sci. 2023, 24(3), 2856; https://doi.org/10.3390/ijms24032856 - 2 Feb 2023
Cited by 7 | Viewed by 3755
Abstract
The kidney functions not only as a metabolite elimination organ but also plays an important role in pharmacotherapy. The kidney tubule epithelia cells express membrane carriers and transporters, which play an important role in drug elimination, and can determine drug nephrotoxicity and drug–drug [...] Read more.
The kidney functions not only as a metabolite elimination organ but also plays an important role in pharmacotherapy. The kidney tubule epithelia cells express membrane carriers and transporters, which play an important role in drug elimination, and can determine drug nephrotoxicity and drug–drug interactions, as well as constituting direct drug targets. The above aspects of kidney transport proteins are discussed in the review. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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19 pages, 2052 KiB  
Review
Small Molecule EGFR Inhibitors as Anti-Cancer Agents: Discovery, Mechanisms of Action, and Opportunities
by Tanzida Zubair and Debasish Bandyopadhyay
Int. J. Mol. Sci. 2023, 24(3), 2651; https://doi.org/10.3390/ijms24032651 - 31 Jan 2023
Cited by 77 | Viewed by 8504
Abstract
Epidermal growth factor receptors (EGFRs) are a class of receptor tyrosine kinase that are also called ErbB1 and HER1. EGFR tyrosine kinase activity inhibition is considered a promising therapeutic strategy for the treatment of cancer. Many small-molecule inhibitors of EGFR tyrosine kinase (EGFR-TK), [...] Read more.
Epidermal growth factor receptors (EGFRs) are a class of receptor tyrosine kinase that are also called ErbB1 and HER1. EGFR tyrosine kinase activity inhibition is considered a promising therapeutic strategy for the treatment of cancer. Many small-molecule inhibitors of EGFR tyrosine kinase (EGFR-TK), from medicinally privileged molecules to commercial drugs, have been overviewed. Particular attention has been paid to the structure of the molecule and its mechanism of action if reported. Subsequent classification of the molecules under discussion has been carried out. Both natural and synthetic and reversible and irreversible EGFR-tyrosine kinase inhibitors have been discussed. Various types of cancers that are caused by overexpression of the EGFR gene, their possible molecular origins, and their natures have also been counted in this article. Because the EGFR signaling pathway controls the proliferation, growth, survival, and differentiation of cells, and the mutated EGFR gene overproduces EGFR protein, which ultimately causes several types of cancer, proper understanding of the molecular dynamics between the protein structure and its inhibitors will lead to more effective and selective EGFR-TKIs, which in turn will be able to save more lives in the battle against cancer. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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29 pages, 2699 KiB  
Review
Recent Advances in the Applications of Small Molecules in the Treatment of Multiple Myeloma
by Hanley N. Abramson
Int. J. Mol. Sci. 2023, 24(3), 2645; https://doi.org/10.3390/ijms24032645 - 31 Jan 2023
Cited by 6 | Viewed by 3946
Abstract
Therapy for multiple myeloma (MM), a hematologic neoplasm of plasma cells, has undergone remarkable changes over the past 25 years. Small molecules (molecular weight of less than one kDa), together with newer immunotherapies that include monoclonal antibodies, antibody-drug conjugates, and most recently, chimeric [...] Read more.
Therapy for multiple myeloma (MM), a hematologic neoplasm of plasma cells, has undergone remarkable changes over the past 25 years. Small molecules (molecular weight of less than one kDa), together with newer immunotherapies that include monoclonal antibodies, antibody-drug conjugates, and most recently, chimeric antigen receptor (CAR) T-cells, have combined to double the disease’s five-year survival rate to over 50% during the past few decades. Despite these advances, the disease is still considered incurable, and its treatment continues to pose substantial challenges, since therapeutic refractoriness and patient relapse are exceedingly common. This review focuses on the current pipeline, along with the contemporary roles and future prospects for small molecules in MM therapy. While small molecules offer prospective benefits in terms of oral bioavailability, cellular penetration, simplicity of preparation, and improved cost–benefit considerations, they also pose problems of toxicity due to off-target effects. Highlighted in the discussion are recent developments in the applications of alkylating agents, immunomodulators, proteasome inhibitors, apoptosis inducers, kinesin spindle protein inhibitors, blockers of nuclear transport, and drugs that affect various kinases involved in intracellular signaling pathways. Molecular and cellular targets are described for each class of agents in relation to their roles as drivers of MM. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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20 pages, 1246 KiB  
Review
Lysosomes as a Target of Anticancer Therapy
by Wojciech Trybus, Ewa Trybus and Teodora Król
Int. J. Mol. Sci. 2023, 24(3), 2176; https://doi.org/10.3390/ijms24032176 - 22 Jan 2023
Cited by 12 | Viewed by 4160
Abstract
Lysosomes are organelles containing acidic hydrolases that are responsible for lysosomal degradation and the maintenance of cellular homeostasis. They play an important role in autophagy, as well as in various cell death pathways, such as lysosomal and apoptotic death. Various agents, including drugs, [...] Read more.
Lysosomes are organelles containing acidic hydrolases that are responsible for lysosomal degradation and the maintenance of cellular homeostasis. They play an important role in autophagy, as well as in various cell death pathways, such as lysosomal and apoptotic death. Various agents, including drugs, can induce lysosomal membrane permeability, resulting in the translocation of acidic hydrolases into the cytoplasm, which promotes lysosomal-mediated death. This type of death may be of great importance in anti-cancer therapy, as both cancer cells with disturbed pathways leading to apoptosis and drug-resistant cells can undergo it. Important compounds that damage the lysosomal membrane include lysosomotropic compounds, antihistamines, immunosuppressants, DNA-damaging drugs, chemotherapeutics, photosensitizers and various plant compounds. An interesting approach in the treatment of cancer and the search for ways to overcome the chemoresistance of cancer cells may also be combining lysosomotropic compounds with targeted modulators of autophagy to induce cell death. These compounds may be an alternative in oncological treatment, and lysosomes may become a promising therapeutic target for many diseases, including cancer. Understanding the functional relationships between autophagy and apoptosis and the possibilities of their regulation, both in relation to normal and cancer cells, can be used to develop new and more effective anticancer therapies. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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39 pages, 13640 KiB  
Review
The Bright Side of Psychedelics: Latest Advances and Challenges in Neuropharmacology
by Andrea Mastinu, Margrate Anyanwu, Marinella Carone, Giulia Abate, Sara Anna Bonini, Gregorio Peron, Emanuela Tirelli, Mariachiara Pucci, Giovanni Ribaudo, Erika Oselladore, Marika Premoli, Alessandra Gianoncelli, Daniela Letizia Uberti and Maurizio Memo
Int. J. Mol. Sci. 2023, 24(2), 1329; https://doi.org/10.3390/ijms24021329 - 10 Jan 2023
Cited by 13 | Viewed by 13506
Abstract
The need to identify effective therapies for the treatment of psychiatric disorders is a particularly important issue in modern societies. In addition, difficulties in finding new drugs have led pharmacologists to review and re-evaluate some past molecules, including psychedelics. For several years there [...] Read more.
The need to identify effective therapies for the treatment of psychiatric disorders is a particularly important issue in modern societies. In addition, difficulties in finding new drugs have led pharmacologists to review and re-evaluate some past molecules, including psychedelics. For several years there has been growing interest among psychotherapists in psilocybin or lysergic acid diethylamide for the treatment of obsessive-compulsive disorder, of depression, or of post-traumatic stress disorder, although results are not always clear and definitive. In fact, the mechanisms of action of psychedelics are not yet fully understood and some molecular aspects have yet to be well defined. Thus, this review aims to summarize the ethnobotanical uses of the best-known psychedelic plants and the pharmacological mechanisms of the main active ingredients they contain. Furthermore, an up-to-date overview of structural and computational studies performed to evaluate the affinity and binding modes to biologically relevant receptors of ibogaine, mescaline, N,N-dimethyltryptamine, psilocin, and lysergic acid diethylamide is presented. Finally, the most recent clinical studies evaluating the efficacy of psychedelic molecules in some psychiatric disorders are discussed and compared with drugs already used in therapy. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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15 pages, 923 KiB  
Review
Clinical Pharmacokinetics of Approved RNA Therapeutics
by Seong Jun Jo, Soon Uk Chae, Chae Bin Lee and Soo Kyung Bae
Int. J. Mol. Sci. 2023, 24(1), 746; https://doi.org/10.3390/ijms24010746 - 1 Jan 2023
Cited by 10 | Viewed by 7571
Abstract
RNA-mediated drugs are a rapidly growing class of therapeutics. Over the last five years, the list of FDA-approved RNA therapeutics has expanded owing to their unique targets and prolonged pharmacological effects. Their absorption, distribution, metabolism, and excretion (ADME) have important clinical im-plications, but [...] Read more.
RNA-mediated drugs are a rapidly growing class of therapeutics. Over the last five years, the list of FDA-approved RNA therapeutics has expanded owing to their unique targets and prolonged pharmacological effects. Their absorption, distribution, metabolism, and excretion (ADME) have important clinical im-plications, but their pharmacokinetic properties have not been fully understood. Most RNA therapeutics have structural modifications to prevent rapid elimination from the plasma and are administered intravenously or subcutaneously, with some exceptions, for effective distribution to target organs. Distribution of drugs into tissues depends on the addition of a moiety that can be transported to the target and RNA therapeutics show a low volume of distribution because of their molecular size and negatively-charged backbone. Nucleases metabolize RNA therapeutics to a shortened chain, but their metabolic ratio is relatively low. Therefore, most RNA therapeutics are excreted in their intact form. This review covers not only ADME features but also clinical pharmacology data of the RNA therapeutics such as drug–drug interaction or population pharmacokinetic analyses. As the market of RNA therapeutics is expected to rapidly expand, comprehensive knowledge will contribute to interpreting and evaluating the pharmacological properties. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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18 pages, 1415 KiB  
Review
Niclosamide as a Promising Therapeutic Player in Human Cancer and Other Diseases
by Zhan Wang, Junyi Ren, Jinxiu Du, Huan Wang, Jia Liu and Guiling Wang
Int. J. Mol. Sci. 2022, 23(24), 16116; https://doi.org/10.3390/ijms232416116 - 17 Dec 2022
Cited by 18 | Viewed by 5925
Abstract
Niclosamide is an FDA-approved anthelmintic drug for the treatment of parasitic infections. However, over the past few years, increasing evidence has shown that niclosamide could treat diseases beyond parasitic diseases, which include metabolic diseases, immune system diseases, bacterial and viral infections, asthma, arterial [...] Read more.
Niclosamide is an FDA-approved anthelmintic drug for the treatment of parasitic infections. However, over the past few years, increasing evidence has shown that niclosamide could treat diseases beyond parasitic diseases, which include metabolic diseases, immune system diseases, bacterial and viral infections, asthma, arterial constriction, myopia, and cancer. Therefore, we systematically reviewed the pharmacological activities and therapeutic prospects of niclosamide in human disease and cancer and summarized the related molecular mechanisms and signaling pathways, indicating that niclosamide is a promising therapeutic player in various human diseases, including cancer. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Pharmacology 2023)
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