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British Journal of Pharmacology Oct 2023The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format,... (Review)
Review
The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and about 6000 interactions with about 3900 ligands. There is an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes almost 500 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.16176. In addition to this overview, in which are identified 'Other protein targets' which fall outside of the subsequent categorisation, there are six areas of focus: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2023, and supersedes data presented in the 2021/22, 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.
Topics: Humans; Databases, Factual; Databases, Pharmaceutical; Ion Channels; Ligands; Pharmacology; Receptors, Cytoplasmic and Nuclear
PubMed: 38123153
DOI: 10.1111/bph.16176 -
Molecules (Basel, Switzerland) Oct 2023The introduction of computational techniques to pharmaceutical chemistry and molecular biology in the 20th century has changed the way people develop drugs [...].
The introduction of computational techniques to pharmaceutical chemistry and molecular biology in the 20th century has changed the way people develop drugs [...].
Topics: Humans; Computer-Aided Design; Drug Discovery; Drug Design; Chemistry, Pharmaceutical
PubMed: 37894639
DOI: 10.3390/molecules28207160 -
Journal of Medicinal Chemistry Apr 2024Molecules with -oxide functionalities are omnipresent in nature and play an important role in Medicinal Chemistry. They are synthetic or biosynthetic intermediates,... (Review)
Review
Molecules with -oxide functionalities are omnipresent in nature and play an important role in Medicinal Chemistry. They are synthetic or biosynthetic intermediates, prodrugs, drugs, or polymers for applications in drug development and surface engineering. Typically, the -oxide group is critical for biomedical applications of these molecules. It may provide water solubility or decrease membrane permeability or immunogenicity. In other cases, the -oxide has a special redox reactivity which is important for drug targeting and/or cytotoxicity. Many of the underlying mechanisms have only recently been discovered, and the number of applications of -oxides in the healthcare field is rapidly growing. This Perspective article gives a short summary of the properties of -oxides and their synthesis. It also provides a discussion of current applications of -oxides in the biomedical field and explains the basic molecular mechanisms responsible for their biological activity.
Topics: Oxides; Chemistry, Pharmaceutical; Polymers
PubMed: 38549449
DOI: 10.1021/acs.jmedchem.4c00254 -
Pharmaceutical Biology Dec 2023L. (Polygonaceae) (PH) is a traditional Chinese traditional medicine with a pungent flavor and mild drug properties. PH is mainly distributed in the channel tropism in... (Review)
Review
CONTEXT
L. (Polygonaceae) (PH) is a traditional Chinese traditional medicine with a pungent flavor and mild drug properties. PH is mainly distributed in the channel tropism in the stomach and large intestine. PH has multiple uses and can be used to treat a variety of diseases for a long time.
OBJECTIVE
This review summarizes the phytochemical and pharmacological activities, and applications of PH from 1980 to 2022. We also provide suggestions for promoting further research and developing additional applications of PH.
METHODS
The data and information on PH from 1980 to 2022 reviewed in this article were obtained from scientific databases, including Science Direct, PubMed, Science Citation Index, SciFinder Scholar (SciFinder), Springer, American Chemical Society (ACS) Publications, and China National Knowledge Infrastructure (CNKI), etc. Some information was obtained from classic literature on traditional Chinese medicines. The search terms were , phytochemistry compositions of , pharmacological activities of , and applications of .
RESULTS
The comprehensive analysis of the literature resulted in 324 compounds being isolated, identified, and reported from PH. Regarding traditional uses, the majority of phytochemical and pharmacological studies have indicated the diverse bioactivities of PH extracts, flavonoids, and volatile oil elements, including antibacterial, antifungal, insecticidal, antioxidant, and anti-inflammatory.
CONCLUSIONS
PH has a long history of diversified medicinal uses, some of which have been verified in modern pharmacological studies. Further detailed studies are required to establish scientific and reasonable quality evaluation standards and action mechanisms of active constituents from PH.
Topics: Polygonum; Medicine, Chinese Traditional; Plant Extracts; Phytochemicals; Oils, Volatile; Ethnopharmacology
PubMed: 37194713
DOI: 10.1080/13880209.2023.2208639 -
Journal of Medicinal Chemistry Mar 2024Photochemistry has emerged as a transformative force in organic chemistry, significantly expanding the chemical space accessible for medicinal chemistry. Light-induced... (Review)
Review
Photochemistry has emerged as a transformative force in organic chemistry, significantly expanding the chemical space accessible for medicinal chemistry. Light-induced reactions enable the efficient synthesis of intricate organic structures and have found applications throughout the different stages of the drug discovery and development processes. Moreover, photochemical techniques provide innovative solutions in chemical biology, allowing precise spatiotemporal drug activation and targeted delivery. In this Perspective, we highlight the already numerous remarkable applications and the even more promising future of photochemistry in medicinal chemistry and chemical biology.
Topics: Photochemistry; Chemistry, Pharmaceutical; Drug Discovery; Biology
PubMed: 38457829
DOI: 10.1021/acs.jmedchem.3c02109 -
Molecular Pharmaceutics Sep 2023Drug delivery systems (DDSs) play an important role in delivering active pharmaceutical ingredients (APIs) to targeted sites with a predesigned release pattern. The... (Review)
Review
Drug delivery systems (DDSs) play an important role in delivering active pharmaceutical ingredients (APIs) to targeted sites with a predesigned release pattern. The chemical and biological properties of APIs and excipients have been extensively studied for their contribution to DDS quality and effectiveness; however, the structural characteristics of DDSs have not been adequately explored. Structure pharmaceutics involves the study of the structure of DDSs, especially the three-dimensional (3D) structures, and its interaction with the physiological and pathological structure of organisms, possibly influencing their release kinetics and targeting abilities. A systematic overview of the structures of a variety of dosage forms, such as tablets, granules, pellets, microspheres, powders, and nanoparticles, is presented. Moreover, the influence of structures on the release and targeting capability of DDSs has also been discussed, especially the and release correlation and the structure-based organ- and tumor-targeting capabilities of particles with different structures. Additionally, an in-depth discussion is provided regarding the application of structural strategies in the DDSs design and evaluation. Furthermore, some of the most frequently used characterization techniques in structure pharmaceutics are briefly described along with their potential future applications.
Topics: Humans; Biopharmaceutics; Drug Delivery Systems; Pharmaceutical Preparations; Excipients; Neoplasms
PubMed: 37552597
DOI: 10.1021/acs.molpharmaceut.3c00514 -
Therapie 2023Although it can be difficult to define who should be considered an elderly person, the population aged 65 and over is experiencing the fastest demographic expansion and...
Although it can be difficult to define who should be considered an elderly person, the population aged 65 and over is experiencing the fastest demographic expansion and will represent almost one billion inhabitants of the 2030 World. Drug use increases dramatically with age and the elderly population is, by far, the highest consumer of medicines, up to 10 times more than younger adults. This consumption is in many aspects inappropriate, unjustified or sub-optimal and associated with a huge number of adverse reactions, admissions in emergency units and attributable deaths. A good part of which could be prevented if basic rules of good prescription and ad-hoc guidelines were systematically used. Even if older adults are more likely to present an adverse drug reaction, available data tend to support that the main risk factor of iatrogenesis in the elderly is the number of drugs used. Moreover, it is often irrelevant to transpose to this population the conclusions concerning the benefit-risk balance of drugs assessed in younger adults; similarly, approaches and programs classically used in pharmacovigilance and pharmacoepidemiology should be tailored to this specific population.
Topics: Humans; Aged; Drug-Related Side Effects and Adverse Reactions; Hospitalization; Risk Factors; Pharmacoepidemiology; Prescriptions
PubMed: 36841650
DOI: 10.1016/j.therap.2023.01.003 -
Congenital Anomalies Jan 2024
Topics: Pregnancy; Female; Humans; Pharmacoepidemiology; Japan; Research
PubMed: 38163674
DOI: 10.1111/cga.12549 -
Molecules (Basel, Switzerland) Nov 2023Pyrazine is a six-membered heterocyclic ring containing nitrogen, and many of its derivatives are biologically active compounds. References have been downloaded through... (Review)
Review
Pyrazine is a six-membered heterocyclic ring containing nitrogen, and many of its derivatives are biologically active compounds. References have been downloaded through Web of Science, PubMed, Science Direct, and SciFinder Scholar. The structure, biological activity, and mechanism of natural product derivatives containing pyrazine fragments reported from 2000 to September 2023 were reviewed. Publications reporting only the chemistry of pyrazine derivatives are beyond the scope of this review and have not been included. The results of research work show that pyrazine-modified natural product derivatives have a wide range of biological activities, including anti-inflammatory, anticancer, antibacterial, antiparasitic, and antioxidant activities. Many of these derivatives exhibit stronger pharmacodynamic activity and less toxicity than their parent compounds. This review has a certain reference value for the development of heterocyclic compounds, especially pyrazine natural product derivatives.
Topics: Pyrazines; Chemistry, Pharmaceutical; Anti-Inflammatory Agents; Anti-Bacterial Agents; Biological Products
PubMed: 37959859
DOI: 10.3390/molecules28217440 -
Journal of Controlled Release :... Sep 2023Classic methods for evaluating the disintegration and dissolution kinetics of solid dosage forms are no longer sufficient to meet the growing demands in the... (Review)
Review
Classic methods for evaluating the disintegration and dissolution kinetics of solid dosage forms are no longer sufficient to meet the growing demands in the pharmaceutical field. Hence, scientists have turned to imaging techniques and computer technology to develop innovative visualization methods. These methods allow for a visual understanding of the disintegration or dissolution process and offer valuable insights into the drug release kinetics. This article aims to provide an overview of the commonly used imaging techniques and their applications in studying the disintegration or dissolution of solid dosage forms. Therefore, imaging presents a novel and alternative approach to understanding the mechanisms of disintegration and dissolution in the formulation study of solid dosages.
Topics: Chemistry, Pharmaceutical; Tablets; Solubility; Drug Liberation; Kinetics; Dosage Forms
PubMed: 37567508
DOI: 10.1016/j.jconrel.2023.08.013