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Pharmaceuticals, Volume 11, Issue 2

2018 June - 30 articles

Cover Story: Over the past few years, drug repositioning has become a relevant strategy for drug discovery, being a time and money saving process. Neurodegenerative diseases are particularly well suited for this approach, as these diseases are age-related and popular treatments of co-morbidities in these kind of pathologies can exhibit beneficial side effects. Our review “Old Drugs as New Treatments for Neurodegenerative Diseases” shows that, in this area of research, the key to the future can be found in the past, and old drugs can become effective new treatments for neurodegenerative diseases. View the paper here.
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Articles (30)

  • Article
  • Open Access
23 Citations
6,418 Views
14 Pages

Parallel Evolution of Host-Attachment Proteins in Phage PP01 Populations Adapting to Escherichia coli O157:H7

  • Chidiebere Akusobi,
  • Benjamin K. Chan,
  • Elizabeth S.C.P. Williams,
  • John E. Wertz and
  • Paul E. Turner

The emergence of antibiotic resistance has sparked interest in phage therapy, which uses virulent phages as antibacterial agents. Bacteriophage PP01 has been studied for potential bio-control of Escherichia coli O157:H7, its natural host, but in the...

  • Article
  • Open Access
10 Citations
5,017 Views
18 Pages

The 3-trifluoroacetyl–substituted 7-acetamido-2-aryl-5-bromoindoles 5ah were prepared and evaluated for potential antigrowth effect in vitro against human lung cancer (A549) and cervical cancer (HeLa) cells and for the potential to inhib...

  • Review
  • Open Access
95 Citations
8,349 Views
14 Pages

TRPM Family Channels in Cancer

  • Aline Hantute-Ghesquier,
  • Aurélien Haustrate,
  • Natalia Prevarskaya and
  • V’yacheslav Lehen’kyi

Members of the TRPM (“Melastatin”) family fall into the subclass of the TRP channels having varying permeability to Ca2+ and Mg2+, with three members of the TRPM family being chanzymes, which contain C-terminal enzyme domains. The role of different T...

  • Review
  • Open Access
144 Citations
14,240 Views
21 Pages

Changing Trends in Computational Drug Repositioning

  • Jaswanth K. Yella,
  • Suryanarayana Yaddanapudi,
  • Yunguan Wang and
  • Anil G. Jegga

Efforts to maximize the indications potential and revenue from drugs that are already marketed are largely motivated by what Sir James Black, a Nobel Prize-winning pharmacologist advocated—“The most fruitful basis for the discovery of a n...

  • Review
  • Open Access
235 Citations
25,411 Views
14 Pages

Inflammation and Neuro-Immune Dysregulations in Autism Spectrum Disorders

  • Dario Siniscalco,
  • Stephen Schultz,
  • Anna Lisa Brigida and
  • Nicola Antonucci

Autism Spectrum Disorder (ASD) is characterized by persistent deficits in social communication and interaction and restricted-repetitive patterns of behavior, interests, or activities. Strong inflammation states are associated with ASD. This inflamma...

  • Review
  • Open Access
43 Citations
11,127 Views
48 Pages

Endocannabinoids in Body Weight Control

  • Henrike Horn,
  • Beatrice Böhme,
  • Laura Dietrich and
  • Marco Koch

Maintenance of body weight is fundamental to maintain one’s health and to promote longevity. Nevertheless, it appears that the global obesity epidemic is still constantly increasing. Endocannabinoids (eCBs) are lipid messengers that are involve...

  • Review
  • Open Access
106 Citations
14,360 Views
29 Pages

The current concept in searching for new bioactive products, including mainly original active substances with potential application in pharmacy and medicine, is based on compounds with a previously determined structure, well-known properties, and bio...

  • Feature Paper
  • Article
  • Open Access
19 Citations
8,412 Views
9 Pages

BACKGROUND: Neuropathic pain can be disabling, and is often difficult to treat. Within a year, over half of all patients stop taking their prescribed neuropathic pain medication, which is most probably due to side effects or disappointing analgesic r...

  • Article
  • Open Access
27 Citations
8,848 Views
13 Pages

There are health concerns associated with increased folic acid intake from fortified food and supplements. Existing analytical methods, however, which can be employed to carry out epidemiological and bioavailability studies for folic acid involve lab...

  • Review
  • Open Access
77 Citations
14,367 Views
19 Pages

The paper addresses the safety of febuxostat and summarizes reports on side effects and interactions of febuxostat published by the cut-off date (last day of literature search) of 20 March 2018. Publications on side effects and the interactions of fe...

  • Article
  • Open Access
9 Citations
6,307 Views
8 Pages

Controlled-Deactivation CB1 Receptor Ligands as a Novel Strategy to Lower Intraocular Pressure

  • Sally Miller,
  • Shashank Kulkarni,
  • Alex Ciesielski,
  • Spyros P. Nikas,
  • Ken Mackie,
  • Alexandros Makriyannis and
  • Alex Straiker

Nearly half a century has passed since the demonstration that cannabis and its chief psychoactive component Δ9-THC lowers intraocular pressure (IOP). Elevated IOP remains the chief hallmark and therapeutic target for glaucoma, a condition that...

  • Article
  • Open Access
7 Citations
4,784 Views
10 Pages

A Short Peptide Inhibitor as an Activity-Based Probe for Matriptase-2

  • Martin Mangold,
  • Michael Gütschow and
  • Marit Stirnberg

Matriptase-2 is a type II transmembrane serine protease and a key regulator of systemic iron homeostasis. Since the activation mechanism and several features of the physiological role of matriptase-2 are not fully understood, there is strong need for...

  • Article
  • Open Access
14 Citations
6,926 Views
13 Pages

High Concentrations of Sodium Chloride Improve Microbicidal Activity of Ibuprofen against Common Cystic Fibrosis Pathogens

  • Adrián J. Muñoz,
  • Roxana V. Alasino,
  • Ariel G. Garro,
  • Valeria Heredia,
  • Néstor H. García,
  • David C. Cremonezzi and
  • Dante M. Beltramo

Ibuprofen (IBU-H), a widely used anti-inflammatory, also shows a marked antimicrobial effect against several bacterial species, including those involved in cystic fibrosis such as Pseudomona aeruginosa, methicillin resistant Staphylococcus aureus and...

  • Review
  • Open Access
68 Citations
8,497 Views
25 Pages

The Role of TRP Channels in the Metastatic Cascade

  • Benedikt Fels,
  • Etmar Bulk,
  • Zoltán Pethő and
  • Albrecht Schwab

A dysregulated cellular Ca2+ homeostasis is involved in multiple pathologies including cancer. Changes in Ca2+ signaling caused by altered fluxes through ion channels and transporters (the transportome) are involved in all steps of the metastatic cas...

  • Feature Paper
  • Article
  • Open Access
43 Citations
8,409 Views
22 Pages

Novel N4-Like Bacteriophages of Pectobacterium atrosepticum

  • Colin Buttimer,
  • Hanne Hendrix,
  • Alan Lucid,
  • Horst Neve,
  • Jean-Paul Noben,
  • Charles Franz,
  • Jim O’Mahony,
  • Rob Lavigne and
  • Aidan Coffey

Pectobacterium atrosepticum is an economically important phytopathogen that is responsible for potato blackleg and soft rot, and for which current control strategies are limited. In this study, stem samples of potato crops exhibiting blackleg were ta...

  • Article
  • Open Access
6 Citations
4,284 Views
10 Pages

The Effects of Dabigatran and Rivaroxaban on Markers of Polymorphonuclear Leukocyte Activation

  • Guy A. Richards,
  • Annette Theron,
  • Gregory Tintinger and
  • Ronald Anderson

Dabigatran is an oral direct thrombin inhibitor, and rivaroxaban, a factor Xa inhibitor. Dabigatran has been implicated in the etiology of acute coronary syndromes and as these occur following inflammatory changes in the endothelium, we investigated...

  • Review
  • Open Access
290 Citations
27,966 Views
21 Pages

Old Drugs as New Treatments for Neurodegenerative Diseases

  • Fernando Durães,
  • Madalena Pinto and
  • Emília Sousa

Neurodegenerative diseases are increasing in number, given that the general global population is becoming older. They manifest themselves through mechanisms that are not fully understood, in many cases, and impair memory, cognition and movement. Curr...

  • Article
  • Open Access
18 Citations
5,617 Views
11 Pages

This study was carried out to evaluate the anti-parasitic effect of ursolic acid against Toxoplasma gondii (T. gondii) that induces toxoplasmosis, particularly in humans. The anti-parasitic effects of ursolic acid against T. gondii-infected cells and...

  • Feature Paper
  • Review
  • Open Access
52 Citations
10,765 Views
10 Pages

2017 FDA Peptide Harvest

  • Othman Al Musaimi,
  • Danah Al Shaer,
  • Beatriz G. De la Torre and
  • Fernando Albericio

2017 was an excellent year in terms of new drugs (chemical entities and biologics) approved by the FDA, with a total of 46. In turn, one of the highlights was the number of peptides (six) included in this list. Here, the six peptides are analyzed in...

  • Article
  • Open Access
8 Citations
4,710 Views
13 Pages

Synthesis and Structure-Activity Relationships of (−)-cis-N-Normetazocine-Based LP1 Derivatives

  • Lorella Pasquinucci,
  • Carmela Parenti,
  • Emanuele Amata,
  • Zafiroula Georgoussi,
  • Paschalina Pallaki,
  • Valeria Camarda,
  • Girolamo Calò,
  • Emanuela Arena,
  • Lucia Montenegro and
  • Rita Turnaturi

(−)-cis-N-Normetazocine represents a rigid scaffold able to mimic the tyramine moiety of endogenous opioid peptides, and the introduction of different N-substituents influences affinity and efficacy of respective ligands at MOR (mu opioid recep...

  • Article
  • Open Access
21 Citations
7,343 Views
20 Pages

Mitoxantrone is More Toxic than Doxorubicin in SH-SY5Y Human Cells: A ‘Chemobrain’ In Vitro Study

  • Daniela Almeida,
  • Rita Pinho,
  • Verónica Correia,
  • Jorge Soares,
  • Maria De Lourdes Bastos,
  • Félix Carvalho,
  • João Paulo Capela and
  • Vera Marisa Costa

The potential neurotoxic effects of anticancer drugs, like doxorubicin (DOX) and mitoxantrone (MTX; also used in multiple sclerosis), are presently important reasons for concern, following epidemiological data indicating that cancer survivors submitt...

  • Article
  • Open Access
11 Citations
6,289 Views
10 Pages

Iron Release from Soybean Seed Ferritin Induced by Cinnamic Acid Derivatives

  • Xuejiao Sha,
  • Hai Chen,
  • Jingsheng Zhang and
  • Guanghua Zhao

Plant ferritin represents a novel class of iron supplement, which widely co-exists with phenolic acids in a plant diet. However, there are few reports on the effect of these phenolic acids on function of ferritin. In this study, we demonstrated that...

  • Article
  • Open Access
14 Citations
5,934 Views
13 Pages

Current screening tests for type 2 diabetes mellitus (T2DM) identify less than 50% of undiagnosed T2DM patients and provide no information about how the disease will develop in prediabetic patients. Here, twenty-nine protein glycation sites were quan...

  • Article
  • Open Access
35 Citations
17,539 Views
24 Pages

Mechanism of the Dual Activities of Human CYP17A1 and Binding to Anti-Prostate Cancer Drug Abiraterone Revealed by a Novel V366M Mutation Causing 17,20 Lyase Deficiency

  • Mónica Fernández-Cancio,
  • Núria Camats,
  • Christa E. Flück,
  • Adam Zalewski,
  • Bernhard Dick,
  • Brigitte M. Frey,
  • Raquel Monné,
  • Núria Torán,
  • Laura Audí and
  • Amit V. Pandey

The CYP17A1 gene regulates sex steroid biosynthesis in humans through 17α-hydroxylase/17,20 lyase activities and is a target of anti-prostate cancer drug abiraterone. In a 46, XY patient with female external genitalia, together with a loss of f...

  • Article
  • Open Access
3 Citations
5,395 Views
15 Pages

5-aza-2′,2′-difluorodeoxycytidine (NUC013) has been shown to be significantly safer and more effective than decitabine in xenograft models of human leukemia and colon cancer. However, it suffers from a similar short half-life as other DNA...

  • Review
  • Open Access
93 Citations
18,727 Views
19 Pages

Research Progress on Rolling Circle Amplification (RCA)-Based Biomedical Sensing

  • Lide Gu,
  • Wanli Yan,
  • Le Liu,
  • Shujun Wang,
  • Xu Zhang and
  • Mingsheng Lyu

Enhancing the limit of detection (LOD) is significant for crucial diseases. Cancer development could take more than 10 years, from one mutant cell to a visible tumor. Early diagnosis facilitates more effective treatment and leads to higher survival r...

  • Article
  • Open Access
35 Citations
6,694 Views
14 Pages

Phytochemical Study of the Ecuadorian Species Lepechinia mutica (Benth.) Epling and High Antifungal Activity of Carnosol against Pyricularia oryzae

  • Jorge Ramírez,
  • Gianluca Gilardoni,
  • Erika Ramón,
  • Solveig Tosi,
  • Anna Maria Picco,
  • Carlo Bicchi and
  • Giovanni Vidari

The plant Lepechinia mutica (Benth.) Epling (family Lamiaceae) is endemic to Ecuador. In the present study, we report some major non-volatile secondary metabolites from the leaves and the chemistry of the essential oil distilled from the flowers. The...

  • Review
  • Open Access
32 Citations
7,605 Views
25 Pages

The resurgence of research into phage biology and therapy is, in part, due to the increasing need for novel agents to treat multidrug-resistant infections. Despite a long clinical history in Eastern Europe and initial success within the food industry...

  • Review
  • Open Access
208 Citations
21,900 Views
22 Pages

Antibody-Drug Conjugates for Cancer Therapy: Chemistry to Clinical Implications

  • Nirnoy Dan,
  • Saini Setua,
  • Vivek K. Kashyap,
  • Sheema Khan,
  • Meena Jaggi,
  • Murali M. Yallapu and
  • Subhash C. Chauhan

Chemotherapy is one of the major therapeutic options for cancer treatment. Chemotherapy is often associated with a low therapeutic window due to its poor specificity towards tumor cells/tissues. Antibody-drug conjugate (ADC) technology may provide a...

  • Communication
  • Open Access
31 Citations
7,647 Views
14 Pages

Computational Modelling of Large Scale Phage Production Using a Two-Stage Batch Process

  • Konrad Krysiak-Baltyn,
  • Gregory J. O. Martin and
  • Sally L. Gras

Cost effective and scalable methods for phage production are required to meet an increasing demand for phage, as an alternative to antibiotics. Computational models can assist the optimization of such production processes. A model is developed here t...

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Pharmaceuticals - ISSN 1424-8247