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Pharmaceuticals, Volume 9, Issue 3

2016 September - 26 articles

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Articles (26)

  • Review
  • Open Access
394 Citations
26,117 Views
33 Pages

20 September 2016

Antimicrobial peptides (AMPs) have remarkably different structures as well as biological activity profiles, whereupon most of these peptides are supposed to kill bacteria via membrane damage. In order to understand their molecular mechanism and targe...

(This article belongs to the Special Issue Antimicrobial Peptides: Expanded Activity Spectrum and Applications)
  • Review
  • Open Access
61 Citations
13,105 Views
17 Pages

TRPV3 in Drug Development

  • Lisa M. Broad,
  • Adrian J. Mogg,
  • Elizabeth Eberle,
  • Marcia Tolley and ,
  • Dominic L. Li and
  • Kelly L. Knopp
  • + 1 author+ 0 author

9 September 2016

Transient receptor potential vanilloid 3 (TRPV3) is a member of the TRP (Transient Receptor Potential) super-family. It is a relatively underexplored member of the thermo-TRP sub-family (Figure 1), however, genetic mutations and use of gene knock-out...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Article
  • Open Access
36 Citations
9,362 Views
11 Pages

8 September 2016

Temozolomide (TMZ) is one of the most effective chemotherapeutic agents for glioblastoma multiforme, but the required high administration dose is accompanied by side effects. To overcome this problem and to further improve TMZ’s efficacy, targeted de...

  • Article
  • Open Access
40 Citations
8,418 Views
14 Pages

Therapeutic Potential of Gramicidin S in the Treatment of Root Canal Infections

  • Marina Berditsch,
  • Hannah Lux,
  • Oleg Babii,
  • Sergii Afonin and
  • Anne S. Ulrich

7 September 2016

An intrinsic clindamycin-resistant Enterococcus faecalis, the most common single species present in teeth after failed root canal therapy, often possesses acquired tetracycline resistance. In these cases, root canal infections are commonly treated wi...

(This article belongs to the Special Issue Antimicrobial Peptides: Expanded Activity Spectrum and Applications)
  • Article
  • Open Access
14 Citations
8,416 Views
11 Pages

7 September 2016

Heparin and heparan sulfate are structurally related glycosaminoglycans (GAGs). Both GAGs present, although in different concentrations, N-sulfo-glucosamine (GlcNS) as one of their various composing units. The conditional fast exchange property of th...

  • Review
  • Open Access
47 Citations
10,553 Views
17 Pages

Targeting TRPM2 in ROS-Coupled Diseases

  • Shinichiro Yamamoto and
  • Shunichi Shimizu

7 September 2016

Under pathological conditions such as inflammation and ischemia-reperfusion injury large amounts of reactive oxygen species (ROS) are generated which, in return, contribute to the development and exacerbation of disease. The second member of the tran...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Review
  • Open Access
78 Citations
10,181 Views
15 Pages

6 September 2016

Influenza A virus (IAV) remains a major threat that can cause severe morbidity and mortality due to rapid genomic variation. Resistance of IAVs to current anti-IAV drugs has been emerging, and antimicrobial peptides (AMPs) have been considered to be...

(This article belongs to the Special Issue Antimicrobial Peptides: Expanded Activity Spectrum and Applications)
  • Review
  • Open Access
96 Citations
18,249 Views
20 Pages

TRPV1: A Target for Rational Drug Design

  • Vincenzo Carnevale and
  • Tibor Rohacs

23 August 2016

Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca2+ permeable cation channel activated by noxious heat, and chemical ligands, such as capsaicin and resiniferatoxin (RTX). Many compounds have been developed that either activate o...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Article
  • Open Access
54 Citations
41,504 Views
23 Pages

Acceptability, Safety, and Efficacy of Oral Administration of Extracts of Black or Red Maca (Lepidium meyenii) in Adult Human Subjects: A Randomized, Double-Blind, Placebo-Controlled Study

  • Carla Gonzales-Arimborgo,
  • Irma Yupanqui,
  • Elsa Montero,
  • Dulce E. Alarcón-Yaquetto and ,
  • Alisson Zevallos-Concha,
  • Lidia Caballero,
  • Manuel Gasco,
  • Jianping Zhao,
  • Ikhlas A. Khan and
  • Gustavo F. Gonzales
  • + 5 authors+ 0 author

18 August 2016

The plant maca, grown at 4000 m altitude in the Peruvian Central Andes, contains hypocotyls that have been used as food and in traditional medicine for centuries. The aim of this research was to provide results on some health effects of oral administ...

(This article belongs to the Special Issue Nutraceuticals and Botanicals: Bioactive Molecules and Therapeutic Properties for Human Health)
  • Review
  • Open Access
47 Citations
8,971 Views
16 Pages

17 August 2016

During the last three to four decades the prevalence of obesity and diabetes mellitus has greatly increased worldwide, including in the United States. Both the short- and long-term forecasts predict serious consequences for the near future, and encou...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Communication
  • Open Access
7 Citations
8,711 Views
6 Pages

17 August 2016

Column-switching high performance liquid chromatography (HPLC) is extensively used for the critical analysis of radiolabeled ligands and their metabolites in plasma. However, the lack of streamlined apparatus and consequently varying protocols remain...

  • Article
  • Open Access
29 Citations
11,021 Views
18 Pages

Nutraceutical Improvement Increases the Protective Activity of Broccoli Sprout Juice in a Human Intestinal Cell Model of Gut Inflammation

  • Simonetta Ferruzza,
  • Fausta Natella,
  • Giulia Ranaldi,
  • Chiara Murgia and ,
  • Carlotta Rossi,
  • Kajetan Trošt,
  • Fulvio Mattivi,
  • Mirella Nardini,
  • Mariateresa Maldini and
  • Simona Baima
  • + 10 authors+ 5 authors

12 August 2016

Benefits to health from a high consumption of fruits and vegetables are well established and have been attributed to bioactive secondary metabolites present in edible plants. However, the effects of specific health-related phytochemicals within a com...

(This article belongs to the Special Issue Nutraceuticals and Botanicals: Bioactive Molecules and Therapeutic Properties for Human Health)
  • Review
  • Open Access
88 Citations
11,836 Views
11 Pages

11 August 2016

Control of chronic pain is frequently inadequate or can be associated with debilitating side effects. Ablation of certain nociceptive neurons, while retaining all other sensory modalities and motor function, represents a new therapeutic approach to c...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Review
  • Open Access
30 Citations
12,291 Views
10 Pages

Chronic cough is common in the population, and among some there is no evident medical explanation for the symptoms. Such a refractory or idiopathic cough is now often regarded as a neuropathic disease due to dysfunctional airway ion channels, though...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Review
  • Open Access
21 Citations
7,127 Views
18 Pages

Activation of TRPV1, TRPA1 or TRPM8 channel expressed in the central terminal of dorsal root ganglion (DRG) neuron increases the spontaneous release of l-glutamate onto spinal dorsal horn lamina II (substantia gelatinosa; SG) neurons which play a piv...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Review
  • Open Access
38 Citations
7,867 Views
8 Pages

TRPM8 Puts the Chill on Prostate Cancer

  • Guillaume P. Grolez and
  • Dimitra Gkika

Prostate cancer (PCa) is one of the most frequently diagnosed cancers in developed countries. Several studies suggest that variations in calcium homeostasis are involved in carcinogenesis. Interestingly, (Transient Receptor Potential Melastatin membe...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Communication
  • Open Access
15 Citations
9,917 Views
11 Pages

Convergent Synthesis of Two Fluorescent Ebselen-Coumarin Heterodimers

  • Jim Küppers,
  • Anna Christina Schulz-Fincke,
  • Jerzy Palus,
  • Mirosław Giurg and ,
  • Jacek Skarżewski and
  • Michael Gütschow
  • + 1 author+ 0 author

The organo-seleniumdrug ebselen exhibits a wide range of pharmacological effects that are predominantly due to its interference with redox systems catalyzed by seleno enzymes, e.g., glutathione peroxidase and thioredoxin reductase. Moreover, ebselen...

(This article belongs to the Special Issue Selected Papers from the 1st International Electronic Conference on Medicinal Chemistry)
  • Article
  • Open Access
59 Citations
13,789 Views
13 Pages

Polylactic Acid—Lemongrass Essential Oil Nanocapsules with Antimicrobial Properties

  • Ioannis L. Liakos,
  • Alexandru Mihai Grumezescu,
  • Alina Maria Holban,
  • Iordache Florin and ,
  • Francesca D’Autilia,
  • Riccardo Carzino,
  • Paolo Bianchini and
  • Athanassia Athanassiou
  • + 3 authors+ 0 author

Polylactic acid was combined with lemongrass essential oil (EO) to produce functional nanocapsules (NCs). The obtained polylactic acid nanoparticles showed antimicrobial activity both with and without the presence of lemongrass oil; however, the pres...

  • Review
  • Open Access
36 Citations
11,372 Views
13 Pages

Thymic stromal lymphopoietin (TSLP) is a pleiotropic cytokine, hitherto mostly known to be involved in inflammatory responses and immunoregulation. The human tslp gene gives rise to two transcription and translation variants: a long form (lfTSLP) tha...

(This article belongs to the Special Issue Antimicrobial Peptides: Expanded Activity Spectrum and Applications)
  • Communication
  • Open Access
5 Citations
9,142 Views
8 Pages

Odanacatib, a Cathepsin K Cysteine Protease Inhibitor, Kills Hookworm In Vivo

  • Jon J. Vermeire,
  • Brian M. Suzuki and
  • Conor R. Caffrey

Hookworm infection is chief among soil-transmitted helminthiases (STHs) for the chronic morbidly inflicted. Deworming via mass drug administration (MDA) programs most often employs single doses of benzimidazole drugs to which resistance is a constant...

  • Review
  • Open Access
261 Citations
29,390 Views
12 Pages

Heparin: Past, Present, and Future

  • Eziafa I. Oduah,
  • Robert J. Linhardt and
  • Susan T. Sharfstein

Heparin, the most widely used anticoagulant drug in the world today, remains an animal-derived product with the attendant risks of adulteration and contamination. A contamination crisis in 2007–2008 increased the impetus to provide non-animal-derived...

  • Review
  • Open Access
90 Citations
8,160 Views
10 Pages

Functions of Cationic Host Defense Peptides in Immunity

  • Mahadevappa Hemshekhar,
  • Vidyanand Anaparti and
  • Neeloffer Mookherjee

Cationic host defense peptides are a widely distributed family of immunomodulatory molecules with antimicrobial properties. The biological functions of these peptides include the ability to influence innate and adaptive immunity for efficient resolut...

(This article belongs to the Special Issue Antimicrobial Peptides: Expanded Activity Spectrum and Applications)
  • Feature Paper
  • Review
  • Open Access
29 Citations
11,521 Views
16 Pages

Strategies to Overcome Heparins’ Low Oral Bioavailability

  • Ana Rita Neves,
  • Marta Correia-da-Silva,
  • Emília Sousa and
  • Madalena Pinto

Even after a century, heparin is still the most effective anticoagulant available with few side effects. The poor oral absorption of heparins triggered the search for strategies to achieve oral bioavailability since this route has evident advantages...

  • Feature Paper
  • Article
  • Open Access
14 Citations
10,691 Views
15 Pages

Site-Specific Labeling of Protein Kinase CK2: Combining Surface Display and Click Chemistry for Drug Discovery Applications

  • Christian Nienberg,
  • Anika Retterath,
  • Kira-Sophie Becher,
  • Thorsten Saenger and ,
  • Henning D. Mootz and
  • Joachim Jose
  • + 1 author+ 0 author

Human CK2 is a heterotetrameric constitutively active serine/threonine protein kinase and is an emerging target in current anti-cancer drug discovery. The kinase is composed of two catalytic CK2α subunits and two regulatory CK2β subunits. In order to...

(This article belongs to the Special Issue Selected Papers from the 1st International Electronic Conference on Medicinal Chemistry)
  • Article
  • Open Access
46 Citations
7,175 Views
20 Pages

The performance of compressed tablet drug delivery systems made using polymeric materials depend on multiple factors, such as surface properties like contact angle, surface free energy and water absorption rate, besides the release mechanisms driven...

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Pharmaceuticals - ISSN 1424-8247