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Alessandra Boschi, Micòl Pasquali, Claudio Trapella, Alessandro Massi, Petra Martini, Adriano Duatti, Remo Guerrini, Vinicio Zanirato, Anna Fantinati, Erika Marzola, Melchiore Giganti, Licia Uccelli
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 macrophages became an attractive target and different multifunctional mannose derivate ligands for the labeling with 99m Tc have been developed. In this study, we report the synthesis of a specific class of dextran-based, macromolecular, multifunctional ligands specially designed for labeling with the highly stable [99m Tc≡N]2+ core...
July 16, 2018: Pharmaceuticals
Ismail Hdoufane, Imane Bjij, Mahmoud Soliman, Alia Tadjer, Didier Villemin, Jane Bogdanov, 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 tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepine (TIBO) derivatives using different classifiers, such as support vector machines, artificial neural networks, random forests, and decision trees. The goal is to propose classification models that will be able to classify TIBO compounds into two groups: high and low inhibitors of HIV-1 reverse transcriptase...
July 13, 2018: Pharmaceuticals
Elvis Legala Ongey, Stephan Pflugmacher, Peter Neubauer
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 natural AMPs as templates for rational design of peptidomimetics are also discussed and some strategies are put forward to curtail cytotoxic effects against eukaryotic cells. Considering the heat-resistant nature, chemical and proteolytic stability of AMPs, we attempt to summarize their molecular targets, examine how these macromolecules may contribute to potential environmental risks vis-à-vis the activities of the peptides...
July 10, 2018: Pharmaceuticals
Natalia Sierra, Christelle Folio, Xavier Robert, Mathieu Long, Christophe Guillon, 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 organization of FIV and the clinical characteristics of the disease caused by FIV are similar to human immunodeficiency virus (HIV). Both viruses infect T lymphocytes, monocytes, and macrophages, with a similar replication cycle in infected cells. Thus, the infection of cats with FIV is also a useful tool for the study and development of novel drugs and vaccines against HIV...
July 10, 2018: Pharmaceuticals
Gerdien A H Korte-Bouws, Floor van Heesch, Koen G C Westphal, Lisa M J Ankersmit, Edwin M van Oosten, Onur Güntürkün, 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 intraperitoneally (i.p.) administered LPS increased extracellular monoamine metabolite levels in the nucleus accumbens (NAc) and medial prefrontal cortex (mPFC), which was completely, or at least partly, prevented by pretreatment with a triple reuptake inhibitor that also blocks the serotonin (5-HT) transporter (SERT)...
July 5, 2018: Pharmaceuticals
Alicia Vall-Sagarra, Shanna Litau, Clemens Decristoforo, Björn Wängler, Ralf Schirrmacher, Gert Fricker, 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 Y receptor subtype 1 (NPY(Y₁)R) as well as the gastrin-releasing peptide receptor (GRPR). Thus, radiolabeled HBPLs being able to bind these two receptors should exhibit an improved tumor targeting efficiency compared to monospecific ligands. We developed here such bispecific HBPLs and radiolabeled them with 68 Ga, achieving high radiochemical yields, purities, and molar activities...
July 4, 2018: Pharmaceuticals
Adwitia Dey, Pamela A Hankey Giblin
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 major depressive disorder does not encompass a systematic characterization of the neurobiological processes that drive the behavioral physiology in patients diagnosed with major depressive disorder. Psychiatric illness is a complex intersection between genetics, physiology, immunology and environmental stress...
June 25, 2018: Pharmaceuticals
Barbora Waclawiková, Sahar El Aidy
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 the past years. A balanced microbial community is a key regulator of the immune response, and metabolism of dietary components, which in turn, modulates several brain processes impacting mood and behavior. Consequently, it is likely that disruptions within the composition of the microbiota would remotely affect the mental state of the host...
June 25, 2018: Pharmaceuticals
John G Bruno
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 leading to deleterious cytokine production via Toll-like receptors (TLRs). Clearly, such CpG or CpG-containing sequences in aptamers intended for therapy could present very damaging side effects to patients. Previous antisense oligonucleotide developers were faced with the same basic CpG dilemma and devised not only avoidance, but other effective strategies from which current aptamer developers can learn to ameliorate or eliminate damaging CpG effects...
June 23, 2018: Pharmaceuticals
Joaquim Aguirre-Plans, Janet Piñero, Jörg Menche, Ferran Sanz, Laura I Furlong, Harald H H W Schmidt, Baldo Oliva, 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 disease (endo)phenotypes and genetic heterogeneity across patients, a natural extension to the current polypharmacology paradigm is to target common biological pathways involved in diseases via endopharmacology (multiple targets, multiple diseases). In this study, we present proximal pathway enrichment analysis (PxEA) for pinpointing drugs that target common disease pathways towards network endopharmacology...
June 22, 2018: Pharmaceuticals
Chidiebere Akusobi, Benjamin K Chan, Elizabeth S C P Williams, John E Wertz, 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 laboratory, PP01 can be inefficient at killing this bacterium. Thus, the goal of this study was to improve the therapeutic potential of PP01 through short-term experimental evolution. Four replicate populations of PP01 were serially passaged 21 times on non-evolving E...
June 20, 2018: Pharmaceuticals
Malose J Mphahlele, Nishal Parbhoo
The 3-trifluoroacetyl⁻substituted 7-acetamido-2-aryl-5-bromoindoles 5a ⁻ h 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 inhibit tubulin polymerization. The corresponding intermediates, namely, the 3-unsubstituted 7-acetyl-2-aryl-5-bromoindole 2a ⁻ d and 7-acetamido-2-aryl-5-bromoindole 4a ⁻ d were included in the assays in order to correlate both structural variations and cytotoxicity. No cytotoxicity was observed for compounds 2a ⁻ d and their 3-trifluoroacetyl⁻substituted derivatives 5a ⁻ d against both cell lines...
June 11, 2018: Pharmaceuticals
Aline Hantute-Ghesquier, Aurélien Haustrate, Natalia Prevarskaya, 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 TRPM members has been shown in various cancers such as prostate cancer for mostly TRPM8 and TRPM2, breast cancer for mostly TRPM2 and TRPM7, and pancreatic cancer for TRPM2/7/8 channels. The role of TRPM5 channels has been shown in lung cancer, TRPM1 in melanoma, and TRPM4 channel in prostate cancer as well...
June 7, 2018: Pharmaceuticals
Jaswanth K Yella, Suryanarayana Yaddanapudi, Yunguan Wang, 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 new drug is to start with an old drug". However, rational design of drug mixtures poses formidable challenges because of the lack of or limited information about in vivo cell regulation, mechanisms of genetic pathway activation, and in vivo pathway interactions. Hence, most of the successfully repositioned drugs are the result of "serendipity", discovered during late phase clinical studies of unexpected but beneficial findings...
June 5, 2018: Pharmaceuticals
Dario Siniscalco, Stephen Schultz, Anna Lisa Brigida, 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 inflammatory condition is often linked to immune system dysfunction. Several cell types are enrolled to trigger and sustain these processes. Neuro-inflammation and neuro-immune abnormalities have now been established in ASD as key factors in its development and maintenance...
June 4, 2018: Pharmaceuticals
Henrike Horn, Beatrice Böhme, Laura Dietrich, 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 involved in overall body weight control by interfering with manifold central and peripheral regulatory circuits that orchestrate energy homeostasis. Initially, blocking of eCB signaling by first generation cannabinoid type 1 receptor (CB1) inverse agonists such as rimonabant revealed body weight-reducing effects in laboratory animals and men...
May 30, 2018: Pharmaceuticals
Dorota Olender, Justyna Żwawiak, Lucjusz Zaprutko
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 biological activity profile. Nowadays, many commonly used drugs originated from natural sources. Moreover, some natural materials have become the source of leading structures for processing further chemical modifications. Many organic compounds with great therapeutic significance have the nitro group in their structure...
May 29, 2018: Pharmaceuticals
David J Kopsky, Jan M Keppel Hesselink
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 results. Therefore, new therapies are needed to alleviate neuropathic pain. As such, topical analgesics could be a new inroad in the treatment of neuropathic pain. In 2014, we developed a new topical formulation containing either phenytoin or sodium phenytoin...
May 28, 2018: Pharmaceuticals
Aref Zayed, Rana Bustami, Wafaa Alabsi, Tamam El-Elimat
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 laborious sample preparation and/or lengthy chromatographic analysis. In this paper we describe a simple, rapid, and sensitive high-performance liquid chromatography⁻electrospray ionisation-tandem mass spectrometry (HPLC⁻ESI-MS/MS) method for determination of unmetabolised folic acid in human plasma using folic acid-d4 as an internal standard...
May 27, 2018: Pharmaceuticals
Andreas Jordan, Ursula Gresser
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 febuxostat were considered. Information concerning the occurrence of side effects and interactions in association with the treatment with febuxostat was collected and summarized in the review. The incidence of severe side effects was much less frequent than mild side effects (1...
May 25, 2018: Pharmaceuticals
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