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Pharmaceuticals, Volume 13, Issue 12

2020 December - 68 articles

Cover Story: Zinc and Copper Detection by MRI using Metal-Based Contrast Agents - What We Know Thus Far. Zn2+ and Cu2+ are essential cations involved in numerous biological processes, and variations in their concentrations can cause diseases. Hence, detection and quantification of these cations are of utmost importance for better understanding their role and for early diagnosis. MRI is a powerful imaging technique and responsive contrast agents have been successfully utilized to detect Zn2+ and are now being developed for Cu2+. These systems are reviewed and the challenges encountered going from Zn2+ to Cu2+ detection are discussed (selectivity and responsivity at physiologically relevant concentrations). In vivo applications are only in their infancy and the recent developments are described, along with the associated quantification problems. View this paper
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Articles (68)

  • Article
  • Open Access
7 Citations
4,574 Views
12 Pages

Synthesis, Biological, and Computational Evaluation of Antagonistic, Chiral Hydrobenzoin Esters of Arecaidine Targeting mAChR M1

  • Marius Ozenil,
  • Jonas Aronow,
  • Daniela Piljak,
  • Chrysoula Vraka,
  • Wolfgang Holzer,
  • Helmut Spreitzer,
  • Wolfgang Wadsak,
  • Marcus Hacker and
  • Verena Pichler

30 November 2020

Muscarinic acetylcholine receptors (mAChRs) are a pivotal constituent of the central and peripheral nervous system. Yet, therapeutic and diagnostic applications thereof are hampered by the lack of subtype selective ligands. Within this work, we synth...

(This article belongs to the Special Issue GPCRs: Ligands and beyond 2022)
  • Article
  • Open Access
9 Citations
6,996 Views
25 Pages

Hepatic Tumor Cell Morphology Plasticity under Physical Constraints in 3D Cultures Driven by YAP–mTOR Axis

  • Adam Frtús,
  • Barbora Smolková,
  • Mariia Uzhytchak,
  • Mariia Lunova,
  • Milan Jirsa,
  • Martin Hof,
  • Piotr Jurkiewicz,
  • Vladimir I. Lozinsky,
  • Lucie Wolfová and
  • Oleg Lunov
  • + 3 authors

28 November 2020

Recent studies undoubtedly show that the mammalian target of rapamycin (mTOR) and the Hippo–Yes-associated protein 1 (YAP) pathways are important mediators of mechanical cues. The crosstalk between these pathways as well as de-regulation of the...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
22 Citations
4,372 Views
13 Pages

Tree-Based QSAR Model for Drug Repurposing in the Discovery of New Antibacterial Compounds against Escherichia coli

  • Beatriz Suay-Garcia,
  • Antonio Falcó,
  • J. Ignacio Bueso-Bordils,
  • Gerardo M. Anton-Fos,
  • M. Teresa Pérez-Gracia and
  • Pedro A. Alemán-López

28 November 2020

Drug repurposing appears as an increasing popular tool in the search of new treatment options against bacteria. In this paper, a tree-based classification method using Linear Discriminant Analysis (LDA) and discrete indexes was used to create a QSAR...

(This article belongs to the Collection Old Pharmaceuticals with New Applications)
  • Review
  • Open Access
56 Citations
8,198 Views
27 Pages

28 November 2020

Autophagy is an evolutionarily conserved lysosomal-dependent pathway for degrading cytoplasmic proteins, macromolecules, and organelles. Autophagy-related genes (Atgs) are the core molecular machinery in the control of autophagy, and several major fu...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
10 Citations
4,677 Views
21 Pages

Synthesis of Platinum(II) Complexes with Some 1-Methylnitropyrazoles and In Vitro Research on Their Cytotoxic Activity

  • Henryk Mastalarz,
  • Agnieszka Mastalarz,
  • Joanna Wietrzyk,
  • Magdalena Milczarek,
  • Andrzej Kochel and
  • Andrzej Regiec

28 November 2020

A series of eight novel platinum(II) complexes were synthesized by the reaction of the appropriate 1-methylnitropyrazole derivatives with K2PtCl4 and characterized by elemental analysis, ESI MS spectrometry, 1H NMR, 195Pt NMR, IR and far IR spectrosc...

(This article belongs to the Special Issue Metal-Based Drugs: Updates and Perspectives)
  • Article
  • Open Access
5 Citations
3,874 Views
11 Pages

Pre-Clinical Investigation of Liquid Paclitaxel for Local Drug Delivery: A Pilot Study

  • Claire V. Cawthon,
  • Kathryn Cooper,
  • Clifton Huett,
  • Alyssa Lloret,
  • Estefanny Villar-Matamoros,
  • Lauren Stokes,
  • Uwe Christians,
  • Michele Schuler and
  • Saami K. Yazdani

28 November 2020

The purpose of this pilot study was to investigate the feasibility of a perfusion catheter to deliver liquid paclitaxel into arterial segments. A clinically relevant rabbit ilio-femoral injury model was utilized to determine the impact of liquid pacl...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
5 Citations
4,202 Views
13 Pages

Repurposing of Plasminogen: An Orphan Medicinal Product Suitable for SARS-CoV-2 Inhalable Therapeutics

  • Anna Maria Piras,
  • Ylenia Zambito,
  • Maurizio Lugli,
  • Baldassare Ferro,
  • Paolo Roncucci,
  • Filippo Mori,
  • Alfonso Salvatore,
  • Ester Ascione,
  • Marta Bellini and
  • Roberto Crea

27 November 2020

The SARS-CoV-2 infection is associated with pulmonary coagulopathy, which determines the deposition of fibrin in the air spaces and lung parenchyma. The resulting lung lesions compromise patient pulmonary function and increase mortality, or end in pe...

(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)
  • Feature Paper
  • Review
  • Open Access
9 Citations
4,455 Views
20 Pages

Monoclonal Antibodies: Leading Actors in the Relapsed/Refractory Multiple Myeloma Treatment

  • Sonia Morè,
  • Maria Teresa Petrucci,
  • Laura Corvatta,
  • Francesca Fazio,
  • Massimo Offidani and
  • Attilio Olivieri

27 November 2020

Multiple myeloma is a complex hematologic malignancy, and despite a survival improvement related to the growing number of available therapeutic options since 2000s, it remains an incurable disease with most patients experiencing relapse. However, the...

(This article belongs to the Special Issue Multidrug Therapies Containing Monoclonal Antibodies for Multiple Myeloma)
  • Review
  • Open Access
43 Citations
11,413 Views
25 Pages

Where Does Metformin Stand in Modern Day Management of Type 2 Diabetes?

  • Ehtasham Ahmad,
  • Jack A. Sargeant,
  • Francesco Zaccardi,
  • Kamlesh Khunti,
  • David R. Webb and
  • Melanie J. Davies

27 November 2020

Metformin is the most commonly used glucose-lowering therapy (GLT) worldwide and remains the first-line therapy for newly diagnosed individuals with type 2 diabetes (T2D) in management algorithms and guidelines after the UK Prospective Diabetes Study...

(This article belongs to the Special Issue Metformin: Mechanism and Application 2022)
  • Commentary
  • Open Access
20 Citations
8,533 Views
17 Pages

27 November 2020

Emetine is a potent antiviral that acts on many viruses in the low-nM range, with several studies in animals and humans demonstrating antiviral activity. Historically, emetine was used to treat patients with Spanish influenza, in the last stages of t...

(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)
  • Article
  • Open Access
8 Citations
3,905 Views
12 Pages

GSK5182, 4-Hydroxytamoxifen Analog, a New Potential Therapeutic Drug for Osteoarthritis

  • Yunhui Min,
  • Dahye Kim,
  • Godagama Gamaarachchige Dinesh Suminda,
  • Xiangyu Zhao,
  • Mangeun Kim,
  • Yaping Zhao and
  • Young-Ok Son

27 November 2020

Estrogen-related receptors (ERRs) are the first identified orphan nuclear receptors. The ERR family consists of ERRα, ERRβ, and ERRγ, regulating diverse isoform-specific functions. We have reported the importance of ERRγ in ost...

(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
  • Review
  • Open Access
29 Citations
5,278 Views
22 Pages

Current Evidence on the Protective Effects of Recombinant Human Erythropoietin and Its Molecular Variants against Pathological Hallmarks of Alzheimer’s Disease

  • José J. Jarero-Basulto,
  • Martha C. Rivera-Cervantes,
  • Deisy Gasca-Martínez,
  • Francisco García-Sierra,
  • Yadira Gasca-Martínez and
  • Carlos Beas-Zárate

26 November 2020

Substantial evidence in the literature demonstrates the pleiotropic effects of the administration of recombinant human erythropoietin (rhEPO) and its molecular variants in different tissues and organs, including the brain. Some of these reports sugge...

(This article belongs to the Special Issue Treatment of Alzheimer Disease)
  • Review
  • Open Access
93 Citations
9,704 Views
40 Pages

25 November 2020

Bowman-Birk inhibitors (BBIs) are found primarily in seeds of legumes and in cereal grains. These canonical inhibitors share a highly conserved nine-amino acids binding loop motif CTP1SXPPXC (where P1 is the inhibitory active site, while X stands for...

(This article belongs to the Special Issue Design of Enzyme Inhibitors as Potential Drugs 2020)
  • Review
  • Open Access
42 Citations
8,330 Views
13 Pages

Statins: HMG-CoA Reductase Inhibitors as Potential Anticancer Agents against Malignant Neoplasms in Women

  • Anna Markowska,
  • Michał Antoszczak,
  • Janina Markowska and
  • Adam Huczyński

25 November 2020

Statins, also known as HMG-CoA inhibitors, are a class of bioactive small molecules that efficiently reduce the levels of cholesterol, and therefore are commonly used to manage and prevent various cardiovascular diseases. With respect to their origin...

(This article belongs to the Special Issue Statins Use and Cancer)
  • Review
  • Open Access
29 Citations
6,222 Views
24 Pages

25 November 2020

Bisphosphonates-related osteonecrosis of the jaw (BRONJ) was firstly reported by Marx in 2003. Since 2014, the term medication-related osteonecrosis of the jaw (MRONJ) is recommended by the American Association of Oral and Maxillofacial Surgeons (AAO...

(This article belongs to the Special Issue Exosomes as a Tool for Disease Progression Monitoring in Humans and Animals)
  • Review
  • Open Access
39 Citations
9,337 Views
26 Pages

CDK4/6 and MAPK—Crosstalk as Opportunity for Cancer Treatment

  • Lisa Scheiblecker,
  • Karoline Kollmann and
  • Veronika Sexl

24 November 2020

Despite the development of targeted therapies and novel inhibitors, cancer remains an undefeated disease. Resistance mechanisms arise quickly and alternative treatment options are urgently required, which may be partially met by drug combinations. Pr...

(This article belongs to the Special Issue Protein Kinases and Cancer)
  • Article
  • Open Access
12 Citations
4,534 Views
18 Pages

Novel mTORC1 Inhibitors Kill Glioblastoma Stem Cells

  • Jose A. Sandoval,
  • Alexey Tomilov,
  • Sandipan Datta,
  • Sonia Allen,
  • Robert O’Donnell,
  • Thomas Sears,
  • Kevin Woolard,
  • Dmytro Kovalskyy,
  • James M. Angelastro and
  • Gino Cortopassi

24 November 2020

Glioblastoma (GBM) is an aggressive tumor of the brain, with an average post-diagnosis survival of 15 months. GBM stem cells (GBMSC) resist the standard-of-care therapy, temozolomide, and are considered a major contributor to tumor resistance. Mammal...

(This article belongs to the Special Issue Novel Therapeutic Targets in Cancer)
  • Article
  • Open Access
23 Citations
4,477 Views
15 Pages

24 November 2020

This study probed the differential utilization of P2Y1 and P2Y12 receptors in mobilizing CD62P (P-selectin) from intracellular granules following activation of human platelets with adenosine 5′-diphosphate (ADP, 100 µmol·L−1)...

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Pharmaceuticals - ISSN 1424-8247