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Pharmaceuticals, Volume 13, Issue 12

December 2020 - 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
23 Citations
4,765 Views
19 Pages

Overexpression of Key Sterol Pathway Enzymes in Two Model Marine Diatoms Alters Sterol Profiles in Phaeodactylum tricornutum

  • Ana Cristina Jaramillo-Madrid,
  • Raffaela Abbriano,
  • Justin Ashworth,
  • Michele Fabris,
  • Mathieu Pernice and
  • Peter J. Ralph

21 December 2020

Sterols are a class of triterpenoid molecules with diverse functional roles in eukaryotic cells, including intracellular signaling and regulation of cell membrane fluidity. Diatoms are a dominant eukaryotic phytoplankton group that produce a wide div...

  • Article
  • Open Access
49 Citations
7,432 Views
17 Pages

Imidazole and Imidazolium Antibacterial Drugs Derived from Amino Acids

  • Adriana Valls,
  • Jose J. Andreu,
  • Eva Falomir,
  • Santiago V. Luis,
  • Elena Atrián-Blasco,
  • Scott G. Mitchell and
  • Belén Altava

21 December 2020

The antibacterial activity of imidazole and imidazolium salts is highly dependent upon their lipophilicity, which can be tuned through the introduction of different hydrophobic substituents on the nitrogen atoms of the imidazole or imidazolium ring o...

  • Review
  • Open Access
6 Citations
3,657 Views
11 Pages

Cell Penetrating Peptides Used in Delivery of Therapeutic Oligonucleotides Targeting Hepatitis B Virus

  • Bénédicte Ndeboko,
  • Serge Thierry Omouessi,
  • Brice Ongali and
  • Augustin Mouinga-Ondémé

21 December 2020

Peptide Nucleic Acid (PNAs) and small noncoding RNAs including small interfering RNAs (siRNAs) represent a new class of oligonucleotides considered as an alternative therapeutic strategy in the chronic hepatitis B treatment. Indeed, chronic hepatitis...

  • Feature Paper
  • Article
  • Open Access
23 Citations
8,898 Views
25 Pages

Apremilast Microemulsion as Topical Therapy for Local Inflammation: Design, Characterization and Efficacy Evaluation

  • Paulo Sarango-Granda,
  • Marcelle Silva-Abreu,
  • Ana Cristina Calpena,
  • Lyda Halbaut,
  • María-José Fábrega,
  • María J. Rodríguez-Lagunas,
  • Natalia Díaz-Garrido,
  • Josefa Badia and
  • Lupe Carolina Espinoza

21 December 2020

Apremilast (APR) is a selective phosphodiesterase 4 inhibitor administered orally in the treatment of moderate-to-severe plaque psoriasis and active psoriatic arthritis. The low solubility and permeability of this drug hinder its dermal administratio...

  • Article
  • Open Access
5 Citations
3,813 Views
24 Pages

Exploring the Anti-Cancer Mechanism of Novel 3,4′-Substituted Diaryl Guanidinium Derivatives

  • Viola Previtali,
  • Helene B. Mihigo,
  • Rebecca Amet,
  • Anthony M. McElligott,
  • Daniela M. Zisterer and
  • Isabel Rozas

21 December 2020

We previously identified a guanidinium-based lead compound that inhibited BRAF through a hypothetic type-III allosteric mechanism. Considering the pharmacophore identified in this lead compound (i.e., “lipophilic group”, “di-substit...

  • Article
  • Open Access
10 Citations
4,720 Views
13 Pages

An Integrated In Silico and In Vivo Approach to Identify Protective Effects of Palonosetron in Cisplatin-Induced Nephrotoxicity

  • Eri Wakai,
  • Yuya Suzumura,
  • Kenji Ikemura,
  • Toshiro Mizuno,
  • Masatoshi Watanabe,
  • Kazuhiko Takeuchi and
  • Yuhei Nishimura

20 December 2020

Cisplatin is widely used to treat various types of cancers, but it is often limited by nephrotoxicity. Here, we employed an integrated in silico and in vivo approach to identify potential treatments for cisplatin-induced nephrotoxicity (CIN). Using p...

  • Article
  • Open Access
12 Citations
5,495 Views
19 Pages

A New Phage Lysin Isolated from the Oral Microbiome Targeting Streptococcus pneumoniae

  • Imme van der Kamp,
  • Lorraine A. Draper,
  • Muireann K. Smith,
  • Colin Buttimer,
  • R. Paul Ross and
  • Colin Hill

19 December 2020

Streptococcus pneumoniae is highly pathogenic and causes several mucosal and invasive infections. Due to the rising number of multidrug-resistant (MDR) strains of S. pneumoniae, new antimicrobials with alternative mechanisms of action are urgently ne...

  • Review
  • Open Access
22 Citations
6,122 Views
26 Pages

Thymus mastichina: Composition and Biological Properties with a Focus on Antimicrobial Activity

  • Márcio Rodrigues,
  • Ana Clara Lopes,
  • Filipa Vaz,
  • Melanie Filipe,
  • Gilberto Alves,
  • Maximiano P. Ribeiro,
  • Paula Coutinho and
  • André R. T. S. Araujo

19 December 2020

Thymus mastichina has the appearance of a semishrub and can be found in jungles and rocky lands of the Iberian Peninsula. This work aimed to review and gather available scientific information on the composition and biological properties of T. mastich...

  • Review
  • Open Access
20 Citations
5,273 Views
18 Pages

Circulating Melanoma-Derived Extracellular Vesicles: Impact on Melanoma Diagnosis, Progression Monitoring, and Treatment Response

  • Stephanie M. Bollard,
  • Cristina Casalou,
  • Chia Yin Goh,
  • Desmond J. Tobin,
  • Pamela Kelly,
  • Amanda McCann and
  • Shirley M. Potter

18 December 2020

Malignant melanoma, one of the most aggressive human malignancies, is responsible for 80% of skin cancer deaths. Whilst early detection of disease progression or metastasis can improve patient survival, this remains a challenge due to the lack of rel...

  • Article
  • Open Access
43 Citations
7,355 Views
17 Pages

18 December 2020

Triple negative breast cancer is one of the most aggressive breast cancer type with abilities of early metastasis and chemoresistance. The tropical plant Citrus hystrix DC. has been reported to promote many biological activities including anticancer....

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Pharmaceuticals - ISSN 1424-8247