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Pharmaceuticals, Volume 11, Issue 3

2018 September - 29 articles

Cover Story: In the era of precision medicine, precision diagnosis is indispensable in oncology. As aptamers show superior target recognition and quick uptake, cancer-specific aptamers have emerged as remarkable detection probes for targeted imaging. Biosensors engineered with fluorogenic aptamers show innovative intracellular imaging in living cells. Aptamers conjugated with fluorophores or gold nanoparticles successfully characterize cancers in tissue imaging. Cancer-specific aptamers labeled with various imaging dyes show satisfactory cancer-specific detection, resulting in the achievement of high-resolution images with low signal-to-noise ratios in vivo in multiple imaging arrays. These advanced molecular imaging approaches demonstrate the value of aptamers in precision diagnostics. View this paper.
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Articles (29)

  • Review
  • Open Access
35 Citations
9,805 Views
15 Pages

19 September 2018

Friedreich ataxia is a neurodegenerative disease with an autosomal recessive inheritance. In most patients, the disease is caused by the presence of trinucleotide GAA expansions in the first intron of the frataxin gene. These expansions cause the dec...

(This article belongs to the Special Issue Iron as Therapeutic Targets in Human Diseases)
  • Review
  • Open Access
30 Citations
7,004 Views
21 Pages

Mitochondrial Targeting in Neurodegeneration: A Heme Perspective

  • Veronica Fiorito,
  • Deborah Chiabrando and
  • Emanuela Tolosano

18 September 2018

Mitochondrial dysfunction has achieved an increasing interest in the field of neurodegeneration as a pathological hallmark for different disorders. The impact of mitochondria is related to a variety of mechanisms and several of them can co-exist in t...

(This article belongs to the Special Issue Iron as Therapeutic Targets in Human Diseases)
  • Article
  • Open Access
11 Citations
8,005 Views
14 Pages

Creatinine-Based Renal Function Estimates and Dosage of Postoperative Pain Management for Elderly Acute Hip Fracture Patients

  • Morten Baltzer Houlind,
  • Kristian Kjær Petersen,
  • Henrik Palm,
  • Lillian Mørch Jørgensen,
  • Mia Aakjær,
  • Lona Louring Christrup,
  • Janne Petersen,
  • Ove Andersen and
  • Charlotte Treldal

18 September 2018

Many analgesics and their metabolites are renally excreted. The widely used Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI)-estimated glomerular filtration rate (eGFR) equations are not developed for use in the elderly, while the recent B...

(This article belongs to the Special Issue Choices of the Journal)
  • Review
  • Open Access
84 Citations
11,514 Views
23 Pages

Aptamers as Diagnostic Tools in Cancer

  • Dario Ruiz Ciancio,
  • Mauricio R. Vargas,
  • William H. Thiel,
  • Martin A. Bruno,
  • Paloma H. Giangrande and
  • María Belén Mestre

11 September 2018

Cancer is the second leading cause of death worldwide. Researchers have been working hard on investigating not only improved therapeutics but also on early detection methods, both critical to increasing treatment efficacy, and developing methods for...

(This article belongs to the Special Issue Aptamer-Based Diagnostics and Therapeutics)
  • Article
  • Open Access
10 Citations
13,633 Views
14 Pages

10 September 2018

Plasma non-transferrin-bound iron (NTBI) is potentially harmful due to the generation of free radicals that cause tissue damage in vascular and other diseases. Studies in iron-replete and iron-deficient subjects, receiving a single oral test dose of...

(This article belongs to the Special Issue Iron as Therapeutic Targets in Human Diseases)
  • Review
  • Open Access
41 Citations
8,493 Views
17 Pages

Modulation of Iron Metabolism in Response to Infection: Twists for All Tastes

  • Ana Cordeiro Gomes,
  • Ana C. Moreira,
  • Gonçalo Mesquita and
  • Maria Salomé Gomes

1 September 2018

Iron is an essential nutrient for almost all living organisms, but is not easily made available. Hosts and pathogens engage in a fight for the metal during an infection, leading to major alterations in the host’s iron metabolism. Important path...

(This article belongs to the Special Issue Iron as Therapeutic Targets in Human Diseases)
  • Article
  • Open Access
6 Citations
6,864 Views
11 Pages

29 August 2018

Several studies showed that [11C]ABP688 binding is altered following drug-induced perturbation of glutamate levels in brains of humans, non-human primates and rats. We evaluated whether the fluorinated derivative [18F]PSS232 can be used to assess met...

(This article belongs to the Special Issue Targets, Tracers and Translation – Novel Radiopharmaceuticals Boost Nuclear Medicine)
  • Article
  • Open Access
3 Citations
6,865 Views
23 Pages

27 August 2018

This work describes a novel screening strategy that implements small-scale spray-drying in early development of binary amorphous solid dispersions (ASDs). The proposed methodology consists of a three-stage decision protocol in which small batches (20...

(This article belongs to the Special Issue Choices of the Journal)
  • Review
  • Open Access
76 Citations
19,048 Views
20 Pages

Intravenous Irons: From Basic Science to Clinical Practice

  • Sunil Bhandari,
  • Dora I. A. Pereira,
  • Helen F. Chappell and
  • Hal Drakesmith

27 August 2018

Iron is an essential trace mineral necessary for life, and iron deficiency anaemia (IDA) is one of the most common haematological problems worldwide, affecting a sixth of the global population. Principally linked to poverty, malnutrition and infectio...

(This article belongs to the Special Issue Iron as Therapeutic Targets in Human Diseases)
  • Review
  • Open Access
52 Citations
6,946 Views
13 Pages

26 August 2018

Aptamer binding has been used effectively for diagnostics, in-vivo targeting of therapeutics, and the construction and control of nanomachines. Nanostructures that respond to pH by releasing or changing affinity to a target have also been used for in...

(This article belongs to the Special Issue Aptamer-Based Diagnostics and Therapeutics)
  • Review
  • Open Access
11 Citations
5,724 Views
14 Pages

Nucleic Acid Aptamers Targeting Epigenetic Regulators: An Innovative Therapeutic Option

  • Silvia Catuogno,
  • Carla Lucia Esposito,
  • Paola Ungaro and
  • Vittorio De Franciscis

24 August 2018

Epigenetic mechanisms include DNA methylation, posttranslational modifications of histones, chromatin remodeling factors, and post transcriptional gene regulation by noncoding RNAs. All together, these processes regulate gene expression by changing c...

(This article belongs to the Special Issue Aptamer-Based Diagnostics and Therapeutics)
  • Article
  • Open Access
24 Citations
7,280 Views
16 Pages

Isolation and Structural Characterization of Bioactive Molecules on Prostate Cancer from Mayan Traditional Medicinal Plants

  • Rafael Sebastián Fort,
  • Juan M. Trinidad Barnech,
  • Juliette Dourron,
  • Marcos Colazzo,
  • Francisco J. Aguirre-Crespo,
  • María Ana Duhagon and
  • Guzmán Álvarez

14 August 2018

Prostate cancer is the most common cancer in men around the world. It is a complex and heterogeneous disease in which androgens and their receptors play a crucial role in the progression and development. The current treatment for prostate cancer is a...

(This article belongs to the Special Issue Selected Papers from the 3rd International Electronic Conference on Medicinal Chemistry)
  • Article
  • Open Access
10 Citations
5,105 Views
14 Pages

This study investigated the potential hepatoprotective effect of oligoribonucleotides-d-mannitol complexes (ORNs-d-M) against thioacetamide (TAA)-induced hepatotoxicity in mice. The hepatoprotective activity of ORNs-d-M was evaluated in thioacetamide...

(This article belongs to the Special Issue Selected Papers from the 3rd International Electronic Conference on Medicinal Chemistry)
  • Article
  • Open Access
23 Citations
7,393 Views
10 Pages

Antiproliferative Activity of Neem Leaf Extracts Obtained by a Sequential Pressurized Liquid Extraction

  • Klebson S. Santos,
  • Andriele M. Barbosa,
  • Victor Freitas,
  • Ana Veruska C. S. Muniz,
  • Marcelo C. Mendonça,
  • Ricardo C. Calhelha,
  • Isabel C. F. R. Ferreira,
  • Elton Franceschi,
  • Francine F. Padilha and
  • Cláudio Dariva
  • + 1 author

Azadirachta indica A. Juss (neem) extracts have been used in pharmaceutical applications as antitumor agents, due to their terpenes and phenolic compounds. To obtain extracts from neem leaves with potential antiproliferative effect, a sequential proc...

  • Article
  • Open Access
10 Citations
7,561 Views
26 Pages

Malaysia is a multi-ethnic society whereby the impact of pharmacogenetic differences between ethnic groups may contribute significantly to variability in clinical therapy. One of the leading causes of mortality in Malaysia is cardiovascular disease (...

  • Article
  • Open Access
23 Citations
11,613 Views
16 Pages

Polyethylene glycol (PEG) is an inert, water soluble polymer, used for decades in pharmaceuticals. Although PEG is considered safe, concerns persist about the potential adverse effects of long-term exposure to PEG-containing therapies, specifically i...

  • Article
  • Open Access
8 Citations
5,837 Views
16 Pages

Rapid replication of the influenza A virus and lung tissue damage caused by exaggerated pro-inflammatory host immune responses lead to numerous deaths. Therefore, novel therapeutic agents that have anti-influenza activities and attenuate excessive pr...

(This article belongs to the Special Issue Selected Papers from the 3rd International Electronic Conference on Medicinal Chemistry)
  • Article
  • Open Access
52 Citations
7,697 Views
20 Pages

An Antioxidant Potential, Quantum-Chemical and Molecular Docking Study of the Major Chemical Constituents Present in the Leaves of Curatella americana Linn

  • Mayara Amoras Teles Fujishima,
  • Nayara Dos Santos Raulino da Silva,
  • Ryan Da Silva Ramos,
  • Elenilze Figueiredo Batista Ferreira,
  • Kelton Luís Belém dos Santos,
  • Carlos Henrique Tomich de Paula da Silva,
  • Jocivania Oliveira da Silva,
  • Joaquín Maria Campos Rosa and
  • Cleydson Breno Rodrigues dos Santos

Reactive oxygen species (ROS) are continuously generated in the normal biological systems, primarily by enzymes as xanthine oxidase (XO). The inappropriate scavenging or inhibition of ROS has been considered to be linked with aging, inflammatory diso...

(This article belongs to the Special Issue Chemoinformatics and Drug Design)
  • Review
  • Open Access
37 Citations
7,307 Views
16 Pages

Imaging is not only seeing, but also believing. For targeted imaging modalities, nucleic acid aptamers have features such as superior recognition of structural epitopes and quick uptake in target cells. This explains the emergence of an evolved new c...

(This article belongs to the Special Issue Aptamer-Based Diagnostics and Therapeutics)
  • Article
  • Open Access
7 Citations
5,800 Views
15 Pages

Design and Synthesis of 99mTcN-Labeled Dextran-Mannose Derivatives for Sentinel Lymph Node Detection

  • Alessandra Boschi,
  • Micòl Pasquali,
  • Claudio Trapella,
  • Alessandro Massi,
  • Petra Martini,
  • Adriano Duatti,
  • Remo Guerrini,
  • Vinicio Zanirato,
  • Anna Fantinati and
  • Licia Uccelli
  • + 2 authors

Background: New approaches based on the receptor-targeted molecular interaction have been recently developed with the aim to investigate specific probes for sentinel lymph nodes. In particular, the mannose receptors expressed by lymph node macrophage...

(This article belongs to the Special Issue Targets, Tracers and Translation – Novel Radiopharmaceuticals Boost Nuclear Medicine)
  • Article
  • Open Access
14 Citations
5,501 Views
14 Pages

In Silico SAR Studies of HIV-1 Inhibitors

  • Ismail Hdoufane,
  • Imane Bjij,
  • Mahmoud Soliman,
  • Alia Tadjer,
  • Didier Villemin,
  • Jane Bogdanov and
  • Driss Cherqaoui

Quantitative Structure Activity Relationships (QSAR or SAR) have helped scientists to establish mathematical relationships between molecular structures and their biological activities. In the present article, SAR studies have been carried out on 89 t...

(This article belongs to the Special Issue Selected Papers from the 3rd International Electronic Conference on Medicinal Chemistry)
  • Article
  • Open Access
8 Citations
5,817 Views
14 Pages

Looking for Novel Capsid Protein Multimerization Inhibitors of Feline Immunodeficiency Virus

  • Natalia Sierra,
  • Christelle Folio,
  • Xavier Robert,
  • Mathieu Long,
  • Christophe Guillon and
  • Guzmán Álvarez

Feline immunodeficiency virus (FIV) is a member of the retroviridae family of viruses. It causes acquired immunodeficiency syndrome (AIDS) in worldwide domestic and non-domestic cats and is a cause of an important veterinary issue. The genome organiz...

(This article belongs to the Special Issue Selected Papers from the 3rd International Electronic Conference on Medicinal Chemistry)
  • Review
  • Open Access
30 Citations
9,270 Views
28 Pages

This review article provides an overview of recent developments in antimicrobial peptides (AMPs), summarizing structural diversity, potential new applications, activity targets and microbial killing responses in general. The use of artificial and nat...

(This article belongs to the Special Issue Choices of the Journal)
  • Article
  • Open Access
24 Citations
7,431 Views
12 Pages

Bacterial Lipopolysaccharide Increases Serotonin Metabolism in Both Medial Prefrontal Cortex and Nucleus Accumbens in Male Wild Type Rats, but Not in Serotonin Transporter Knockout Rats

  • Gerdien A. H. Korte-Bouws,
  • Floor Van Heesch,
  • Koen G. C. Westphal,
  • Lisa M. J. Ankersmit,
  • Edwin M. Van Oosten,
  • Onur Güntürkün and
  • S. Mechiel Korte

It is well known that bacterial lipopolysaccharides (LPS) both increases proinflammatory cytokines and produces sickness behavior, including fatigue and anhedonia (i.e., the inability to experience pleasure). Previously, we have shown that intraperit...

(This article belongs to the Special Issue Understanding Inflammation-induced Mental Diseases: New Opportunities for Treatment)
  • Article
  • Open Access
17 Citations
6,295 Views
20 Pages

Design, Synthesis, In Vitro, and Initial In Vivo Evaluation of Heterobivalent Peptidic Ligands Targeting Both NPY(Y1)- and GRP-Receptors—An Improvement for Breast Cancer Imaging?

  • Alicia Vall-Sagarra,
  • Shanna Litau,
  • Clemens Decristoforo,
  • Björn Wängler,
  • Ralf Schirrmacher,
  • Gert Fricker and
  • Carmen Wängler

Heterobivalent peptidic ligands (HBPLs), designed to address two different receptors independently, are highly promising tumor imaging agents. For example, breast cancer has been shown to concomitantly and complementarily overexpress the neuropeptide...

(This article belongs to the Special Issue Targets, Tracers and Translation – Novel Radiopharmaceuticals Boost Nuclear Medicine)
  • Review
  • Open Access
162 Citations
22,593 Views
17 Pages

The human gastrointestinal tract is inhabited by trillions of commensal bacteria collectively known as the gut microbiota. Our recognition of the significance of the complex interaction between the microbiota, and its host has grown dramatically over...

(This article belongs to the Special Issue Understanding Inflammation-induced Mental Diseases: New Opportunities for Treatment)
  • Review
  • Open Access
71 Citations
10,899 Views
17 Pages

Over 350 million individuals suffer from depression, a psychiatric illness classified as major depressive disorder (MDD) with symptoms that include a loss of interest or pleasure in life accompanied by depressed mood. The present understanding of maj...

(This article belongs to the Special Issue Understanding Inflammation-induced Mental Diseases: New Opportunities for Treatment)
  • Review
  • Open Access
33 Citations
7,318 Views
7 Pages

It is well known that unmethylated 2′-deoxycytidine-phosphate-2′-guanine (CpG) sequences alone or in longer DNA and RNA oligonucleotides can act like pathogen-associated molecular patterns (PAMPs) and trigger the innate immune response le...

(This article belongs to the Special Issue Aptamer-Based Diagnostics and Therapeutics)
  • Article
  • Open Access
39 Citations
11,956 Views
18 Pages

Proximal Pathway Enrichment Analysis for Targeting Comorbid Diseases via Network Endopharmacology

  • Joaquim Aguirre-Plans,
  • Janet Piñero,
  • Jörg Menche,
  • Ferran Sanz,
  • Laura I. Furlong,
  • Harald H. H. W. Schmidt,
  • Baldo Oliva and
  • Emre Guney

The past decades have witnessed a paradigm shift from the traditional drug discovery shaped around the idea of “one target, one disease” to polypharmacology (multiple targets, one disease). Given the lack of clear-cut boundaries across di...

(This article belongs to the Collection Old Pharmaceuticals with New Applications)
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Pharmaceuticals - ISSN 1424-8247