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Pharmaceuticals, Volume 15, Issue 1

January 2022 - 108 articles

Cover Story: Lipids play a diverse range of physiological roles. In response to stimuli, lipids affect signaling pathways by often acting as chemical messengers that bind and activate G protein-coupled receptors (GPCRs) studded on the cell surface. In the present review, we specifically focus on the signaling activities of lipids from the perspective of their cognate GPCRs, especially those from class A (rhodopsin-like) GPCRs and their binding and interactions with agonists/antagonists (orthosteric and allosteric). We summarize the latest structural, functional, and dynamical insights gleaned from recently elucidated structures and computational studies. We also discuss the implications of these findings for drug discovery and development as well as present new directions and approaches. View this paper
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Articles (108)

  • Review
  • Open Access
46 Citations
10,734 Views
36 Pages

Mini-Tablets: A Valid Strategy to Combine Efficacy and Safety in Pediatrics

  • Guendalina Zuccari,
  • Silvana Alfei,
  • Danilo Marimpietri,
  • Valentina Iurilli,
  • Paola Barabino and
  • Leonardo Marchitto

17 January 2022

In the treatment of pediatric diseases, mass-produced dosage forms are often not suitable for children. Commercially available medicines are commonly manipulated and mixed with food by caregivers at home, or extemporaneous medications are routinely c...

  • Article
  • Open Access
6 Citations
3,633 Views
15 Pages

Synthesis and Anti-Hepatoma Activities of U12 Derivatives Arresting G0/G1 Phase and Inducing Apoptosis by PI3K/AKT/mTOR Pathway

  • Renjing Yang,
  • Chunchun Du,
  • Ting Cao,
  • Guanghui Wang,
  • Xin Jiang,
  • Jun Gao,
  • Ting Lin,
  • Cuiling Sun,
  • Rong Ding and
  • Wenjing Tian
  • + 1 author

17 January 2022

Ursodeoxycholic acid (UDCA) is a first-line clinical drug for the treatment of liver diseases. U12, a derivative of UDCA, showed effective anti-hepatoma activities in previous works. However, the low polarity and large doses limited the druglikeness...

  • Article
  • Open Access
39 Citations
4,682 Views
22 Pages

Identification of Cyclic Sulfonamides with an N-Arylacetamide Group as α-Glucosidase and α-Amylase Inhibitors: Biological Evaluation and Molecular Modeling

  • Furqan Ahmad Saddique,
  • Matloob Ahmad,
  • Usman Ali Ashfaq,
  • Muhammad Muddassar,
  • Sadia Sultan and
  • Magdi E. A. Zaki

17 January 2022

Diabetes mellitus (DM), a complicated metabolic disorder, is due to insensitivity to insulin function or reduction in insulin secretion, which results in postprandial hyperglycemia. α-Glucosidase inhibitors (AGIs) and α-amylase inhibitors...

  • Perspective
  • Open Access
9 Citations
6,507 Views
14 Pages

A 5-Year Study of Lithium and Valproic Acid Drug Monitoring in Patients with Bipolar Disorders in an Italian Clinical Center

  • Marco Carli,
  • Eleonora Risaliti,
  • Mena Francomano,
  • Shivakumar Kolachalam,
  • Biancamaria Longoni,
  • Guido Bocci,
  • Roberto Maggio and
  • Marco Scarselli

17 January 2022

Therapeutic drug monitoring (TDM) is an effective tool used to improve the pharmacological treatment in clinical practice, especially to detect subtherapeutic drug plasma concentration (Cp) in order to consider a change of dosage during treatment and...

  • Article
  • Open Access
20 Citations
3,992 Views
14 Pages

Coumarin Derivatives Exert Anti-Lung Cancer Activity by Inhibition of Epithelial–Mesenchymal Transition and Migration in A549 Cells

  • Rodrigo Santos Aquino de Araújo,
  • Julianderson de Oliveira dos Santos Carmo,
  • Simone Lara de Omena Silva,
  • Camila Radelley Azevedo Costa da Silva,
  • Tayhana Priscila Medeiros Souza,
  • Natália Barbosa de Mélo,
  • Jean-Jacques Bourguignon,
  • Martine Schmitt,
  • Thiago Mendonça de Aquino and
  • Renato Santos Rodarte
  • + 4 authors

17 January 2022

A series of coumarin derivatives and isosteres were synthesized from the reaction of triflic intermediates with phenylboronic acids, terminal alkynes, and organozinc compounds through palladium-catalyzed cross-coupling reactions. The in vitro cytotox...

  • Article
  • Open Access
44 Citations
10,789 Views
19 Pages

CD44-Targeted Carriers: The Role of Molecular Weight of Hyaluronic Acid in the Uptake of Hyaluronic Acid-Based Nanoparticles

  • Enrica Chiesa,
  • Antonietta Greco,
  • Federica Riva,
  • Rossella Dorati,
  • Bice Conti,
  • Tiziana Modena and
  • Ida Genta

17 January 2022

Nanotechnology offers advanced biomedical tools for diagnosis and drug delivery, stressing the value of investigating the mechanisms by which nanocarriers interact with the biological environment. Herein, the cellular response to CD44-targeted nanopa...

  • Article
  • Open Access
7 Citations
5,739 Views
15 Pages

Synthesis, In Vitro, In Vivo and In Silico Antidiabetic Bioassays of 4-Nitro(thio)phenoxyisobutyric Acids Acting as Unexpected PPARγ Modulators: An In Combo Study

  • Blanca Colin-Lozano,
  • Héctor Torres-Gomez,
  • Sergio Hidalgo-Figueroa,
  • Fabiola Chávez-Silva,
  • Samuel Estrada-Soto,
  • Julio Cesar Almanza-Pérez and
  • Gabriel Navarrete-Vazquez

15 January 2022

Four isobutyric acids (two nitro and two acetamido derivatives) were prepared in two steps and characterized using spectral analysis. The mRNA concentrations of PPARγ and GLUT-4 (two proteins documented as key diabetes targets) were increased b...

  • Article
  • Open Access
8 Citations
4,045 Views
28 Pages

Antimicrobial Activity and Degradation Ability Study on Nanoparticle-Enriched Formulations Specially Designed for the Neutralization of Real and Simulated Biological and Chemical Warfare Agents

  • Raluca-Elena Ginghina,
  • Gabriela Toader,
  • Munizer Purica,
  • Adriana-Elena Bratu,
  • Claudiu Lazaroaie,
  • Tudor-Viorel Tiganescu,
  • Ramona-Elena Oncioiu,
  • George-Ovidiu Iorga,
  • Florina-Lucica Zorila and
  • Mihai Constantin
  • + 3 authors

14 January 2022

The present work reveals a comprehensive decontamination study on real and simulated biological and chemical warfare agents (BCWA). The emphasis was on evaluating the antimicrobial activity against real biological warfare agents, such as Bacillus ant...

  • Review
  • Open Access
26 Citations
8,986 Views
50 Pages

Discovering the Potential of Natural Antioxidants in Age-Related Macular Degeneration: A Review

  • Kah-Hui Wong,
  • Hui-Yin Nam,
  • Sze-Yuen Lew,
  • Murali Naidu,
  • Pamela David,
  • Tengku Ain Kamalden,
  • Siti Nurma Hanim Hadie and
  • Lee-Wei Lim

14 January 2022

Age-related macular degeneration (AMD) is a multifactorial disease associated with anatomical changes in the inner retina. Despite tremendous advances in clinical care, there is currently no cure for AMD. This review aims to evaluate the published li...

  • Article
  • Open Access
20 Citations
5,397 Views
15 Pages

Optimization of Solvent-Free Microwave-Assisted Hydrodiffusion and Gravity Extraction of Morus nigra L. Fruits Maximizing Polyphenols, Sugar Content, and Biological Activities Using Central Composite Design

  • Ahmed M. Mustafa,
  • Eugenia Mazzara,
  • Doaa Abouelenein,
  • Simone Angeloni,
  • Sonia Nunez,
  • Gianni Sagratini,
  • Víctor López,
  • Marco Cespi,
  • Sauro Vittori and
  • Giovanni Caprioli
  • + 1 author

14 January 2022

Black mulberry, Morus nigra L. (family: Moraceae), is a healthy food and medicinal plant. Microwave hydrodiffusion and gravity (MHG) is one of the most innovative applications of solvent-free microwave extraction. The aim of this study was to optimiz...

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Pharmaceuticals - ISSN 1424-8247