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Pharmaceuticals, Volume 12, Issue 2

June 2019 - 54 articles

Cover Story: HIV-1 inhibition by the long-acting antiviral 4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA). The active site of HIV-1 reverse transcriptase (RT) (thumb (green), palm (red), and fingers (blue) subdomain) bound to template (cyan) annealed to EFdA-terminated primer (yellow). The monophosphate form of EFdA (colored atoms: carbons in gray, oxygens in red, nitrogen in blue, fluorine in green, phosphorus in orange) is shown incorporated at the 3'-end of the primer, with the 4'-ethynyl group of EFdA strongly bound at a conserved hydrophobic pocket (in cyan), thus blocking RT translocation and further DNA synthesis. View this paper.
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Articles (54)

  • Review
  • Open Access
33 Citations
10,738 Views
49 Pages

Psychotropic Drugs for the Management of Chronic Pain and Itch

  • Daria A. Belinskaia,
  • Mariia A. Belinskaia,
  • Oleg I. Barygin,
  • Nina P. Vanchakova and
  • Natalia N. Shestakova

Clinical observations have shown that patients with chronic neuropathic pain or itch exhibit symptoms of increased anxiety, depression and cognitive impairment. Such patients need corrective therapy with antidepressants, antipsychotics or anticonvuls...

  • Review
  • Open Access
23 Citations
6,079 Views
14 Pages

Iron is at the forefront of a number of pivotal biological processes due to its ability to readily accept and donate electrons. However, this property may also catalyze the generation of free radicals with ensuing cellular and tissue toxicity. Accord...

  • Review
  • Open Access
43 Citations
7,745 Views
11 Pages

The Zika virus (ZIKV) is a mosquito-borne flavivirus that can lead to birth defects (microcephaly), ocular lesions and neurological disorders (Guillain-Barré syndrome). There is no licensed vaccine or antiviral treatment against ZIKV infection...

  • Article
  • Open Access
13 Citations
5,893 Views
18 Pages

Design and Synthesis of CNS-targeted Flavones and Analogues with Neuroprotective Potential Against H2O2- and Aβ1-42-Induced Toxicity in SH-SY5Y Human Neuroblastoma Cells

  • Ana M. de Matos,
  • Alice Martins,
  • Teresa Man,
  • David Evans,
  • Magnus Walter,
  • Maria Conceição Oliveira,
  • Óscar López,
  • José G. Fernandez-Bolaños,
  • Philipp Dätwyler and
  • Beat Ernst
  • + 4 authors

With the lack of available drugs able to prevent the progression of Alzheimer’s disease (AD), the discovery of new neuroprotective treatments able to rescue neurons from cell injury is presently a matter of extreme importance and urgency. Here,...

  • Review
  • Open Access
59 Citations
11,150 Views
13 Pages

Therapeutic Potential of Kappa Opioid Agonists

  • Tyler C. Beck,
  • Matthew A. Hapstack,
  • Kyle R. Beck and
  • Thomas A. Dix

Many original research articles have been published that describe findings and outline areas for the development of kappa-opioid agonists (KOAs) as novel drugs; however, a single review article that summarizes the broad potential for KOAs in drug dev...

  • Review
  • Open Access
40 Citations
9,265 Views
12 Pages

CDK8-Novel Therapeutic Opportunities

  • Ingeborg Menzl,
  • Agnieszka Witalisz-Siepracka and
  • Veronika Sexl

Improvements in cancer therapy frequently stem from the development of new small-molecule inhibitors, paralleled by the identification of biomarkers that can predict the treatment response. Recent evidence supports the idea that cyclin-dependent kina...

  • Review
  • Open Access
92 Citations
8,499 Views
11 Pages

Cellular Senescence and Iron Dyshomeostasis in Alzheimer’s Disease

  • Shashank Masaldan,
  • Abdel Ali Belaidi,
  • Scott Ayton and
  • Ashley I. Bush

Iron dyshomeostasis is a feature of Alzheimer’s disease (AD). The impact of iron on AD is attributed to its interactions with the central proteins of AD pathology (amyloid precursor protein and tau) and/or through the iron-mediated generation o...

  • Review
  • Open Access
30 Citations
5,618 Views
10 Pages

Ironing out Macrophage Immunometabolism

  • Stefania Recalcati,
  • Elena Gammella and
  • Gaetano Cairo

Over the last decade, increasing evidence has reinforced the key role of metabolic reprogramming in macrophage activation. In addition to supporting the specific immune response of different subsets of macrophages, intracellular metabolic pathways al...

  • Article
  • Open Access
3 Citations
4,588 Views
17 Pages

Synthesis and Study of New Quinolineaminoethanols as Anti-Bacterial Drugs

  • Pierre Laumaillé,
  • Alexandra Dassonville-Klimpt,
  • François Peltier,
  • Catherine Mullié,
  • Claire Andréjak,
  • Sophie Da-Nascimento,
  • Sandrine Castelain and
  • Pascal Sonnet

The lack of antibiotics with a novel mode of action associated with the spread of drug resistant bacteria make the fight against infectious diseases particularly challenging. A quinoline core is found in several anti-infectious drugs, such as mefloqu...

  • Article
  • Open Access
17 Citations
5,394 Views
22 Pages

CK2 Pro-Survival Role in Prostate Cancer Is Mediated via Maintenance and Promotion of Androgen Receptor and NFκB p65 Expression

  • Janeen H. Trembley,
  • Betsy T. Kren,
  • Md. J. Abedin,
  • Daniel P. Shaughnessy,
  • Yingming Li,
  • Scott M. Dehm and
  • Khalil Ahmed

The prosurvival protein kinase CK2, androgen receptor (AR), and nuclear factor kappa B (NFκB) interact in the function of prostate cells, and there is evidence of crosstalk between these signals in the pathobiology of prostate cancer (PCa). As...

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Pharmaceuticals - ISSN 1424-8247