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Pharmaceuticals, Volume 11, Issue 1

March 2018 - 30 articles

Cover Story: Briefly, amyloid β 1–42 (Aβ) binds to the brain insulin receptor (IR) and dysregulates its signalling cascade in the hippocampus and other brain areas, contributing to the development of insulin resistance. In addition, Aβ indirectly modulates IR activation through the phosphorylation of IR substrates 1 (IRS-1) at its inactivation sites. This response would be the consequence of the increase in reactive glia induced by Aβ and the subsequent release of molecules like tumour necrosis factor alpha (TNFα). Decreased IR signalling leads to reduced activation of protein kinase B (PKB/AKT) which influences other pathways like those controlled by glycogen synthase kinase 3β (GSK3β) and the trafficking of the insulin-sensitive glucose transporter type 4 (GLUT4) to the plasma membrane. In conclusion, all these interrelated mechanisms eventually lead to the well-known memory impairment characteristic of Alzheimer’s disease. View this paper
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Articles (30)

  • Article
  • Open Access
9 Citations
5,165 Views
11 Pages
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Self-Assembled Supramolecular Nanoparticles Improve the Cytotoxic Efficacy of CK2 Inhibitor THN7

  • Abdelhamid Nacereddine,
  • Andre Bollacke,
  • Eszter Róka,
  • Christelle Marminon,
  • Zouhair Bouaziz,
  • Ferenc Fenyvesi,
  • Ildikó Katalin Bácskay,
  • Joachim Jose,
  • Florent Perret and
  • Marc Le Borgne
Pharmaceuticals2018, 11(1), 10;https://doi.org/10.3390/ph11010010

26 January 2018

Since the approval of imatinib in 2001, kinase inhibitors have revolutionized cancer therapies. Inside this family of phosphotransferases, casein kinase 2 (CK2) is of great interest and numerous scaffolds have been investigated to design CK2 inhibito...

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  • Article
  • Open Access
12 Citations
4,926 Views
16 Pages
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Improved Intranasal Retentivity and Transnasal Absorption Enhancement by PEGylated Poly-l-ornithine

  • Yusuke Kamiya,
  • Tsutomu Yamaki,
  • Shigehiro Omori,
  • Masaki Uchida,
  • Kazuo Ohtake,
  • Mitsutoshi Kimura,
  • Hiroshi Yamazaki and
  • Hideshi Natsume
Pharmaceuticals2018, 11(1), 9;https://doi.org/10.3390/ph11010009

25 January 2018

We reported that the introduction of polyethylene glycol (PEG) to poly-l-ornithine (PLO), which is an homopolymeric basic amino acid having absorption-enhancement ability, prolonged retention time in an in vitro inclined plate test, probably due to a...

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  • Article
  • Open Access
24 Citations
5,010 Views
9 Pages
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Gastroprotective Effects of Sulphated Polysaccharides from the Alga Caulerpa mexicana Reducing Ethanol-Induced Gastric Damage

  • José Gerardo Carneiro,
  • Ticiana De Brito Lima Holanda,
  • Ana Luíza Gomes Quinderé,
  • Annyta Fernandes Frota,
  • Vitória Virgínia Magalhães Soares,
  • Rayane Siqueira de Sousa,
  • Manuela Araújo Carneiro,
  • Dainesy Santos Martins,
  • Antoniella Souza Gomes Duarte and
  • Norma Maria Barros Benevides
Pharmaceuticals2018, 11(1), 6;https://doi.org/10.3390/ph11010006

20 January 2018

The development of the gastric lesion is complex and the result of the imbalance between aggressive and protective factors, involving the generation of free radicals and disturbance in nitric oxide (NO) production. Sulphated polysaccharides (SP), fro...

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  • Article
  • Open Access
21 Citations
6,278 Views
11 Pages
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Effects of Polymethoxyflavonoids on Bone Loss Induced by Estrogen Deficiency and by LPS-Dependent Inflammation in Mice

  • Shigeru Matsumoto,
  • Tsukasa Tominari,
  • Chiho Matsumoto,
  • Shosei Yoshinouchi,
  • Ryota Ichimaru,
  • Kenta Watanabe,
  • Michiko Hirata,
  • Florian M. W. Grundler,
  • Chisato Miyaura and
  • Masaki Inada
Pharmaceuticals2018, 11(1), 7;https://doi.org/10.3390/ph11010007

20 January 2018

Polymethoxyflavonoids (PMFs) are a family of the natural compounds that mainly compise nobiletin, tangeretin, heptamethoxyflavone (HMF), and tetramethoxyflavone (TMF) in citrus fruits. PMFs have shown various biological functions, including anti-oxid...

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  • Article
  • Open Access
16 Citations
9,379 Views
18 Pages
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In Silico Study, Synthesis, and Cytotoxic Activities of Porphyrin Derivatives

  • Fransiska Kurniawan,
  • Youhei Miura,
  • Rahmana Emran Kartasasmita,
  • Naoki Yoshioka,
  • Abdul Mutalib and
  • Daryono Hadi Tjahjono
Pharmaceuticals2018, 11(1), 8;https://doi.org/10.3390/ph11010008

20 January 2018

Five known porphyrins, 5,10,15,20-tetrakis(p-tolyl)porphyrin (TTP), 5,10,15,20-tetrakis(p-bromophenyl)porphyrin (TBrPP), 5,10,15,20-tetrakis(p-aminophenyl)porphyrin (TAPP), 5,10,15-tris(tolyl)-20-mono(p-nitrophenyl)porphyrin (TrTMNP), 5,10,15-tris(to...

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  • Feature Paper
  • Review
  • Open Access
54 Citations
8,311 Views
8 Pages
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Endolysosomal Cation Channels and Cancer—A Link with Great Potential

  • Christian Grimm,
  • Karin Bartel,
  • Angelika M. Vollmar and
  • Martin Biel
Pharmaceuticals2018, 11(1), 4;https://doi.org/10.3390/ph11010004

5 January 2018

The endolysosomal system (ES) consists of lysosomes; early, late, and recycling endosomes; and autophagosomes. It is a key regulator not only of macromolecule degradation and recycling, plasma membrane repair, homeostasis, and lipid storage, but also...

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  • Article
  • Open Access
46 Citations
7,341 Views
18 Pages
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Antimicrobial and Antibiofilm Activity of UP-5, an Ultrashort Antimicrobial Peptide Designed Using Only Arginine and Biphenylalanine

  • Ammar Almaaytah,
  • Mohammed T. Qaoud,
  • Gubran Khalil Mohammed,
  • Ahmad Abualhaijaa,
  • Daniel Knappe,
  • Ralf Hoffmann and
  • Qosay Al-Balas
Pharmaceuticals2018, 11(1), 3;https://doi.org/10.3390/ph11010003

2 January 2018

The recent upsurge of multidrug resistant bacteria (MDRB) among global communities has become one of the most serious challenges facing health professionals and the human population worldwide. Cationic ultrashort antimicrobial peptides (USAMPs) are a...

Full Article
  • Review
  • Open Access
254 Citations
19,162 Views
18 Pages
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Roles of Heat Shock Proteins in Apoptosis, Oxidative Stress, Human Inflammatory Diseases, and Cancer

  • Paul Chukwudi Ikwegbue,
  • Priscilla Masamba,
  • Babatunji Emmanuel Oyinloye and
  • Abidemi Paul Kappo
Pharmaceuticals2018, 11(1), 2;https://doi.org/10.3390/ph11010002

23 December 2017

Heat shock proteins (HSPs) play cytoprotective activities under pathological conditions through the initiation of protein folding, repair, refolding of misfolded peptides, and possible degradation of irreparable proteins. Excessive apoptosis, resulti...

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