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Pharmaceuticals

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https://www.readbyqxmd.com/read/28635674/exploring-wound-healing-genomic-machinery-with-a-network-based-approach
#1
Francesca Vitali, Simone Marini, Martina Balli, Hanne Grosemans, Maurilio Sampaolesi, Yves A Lussier, Maria Gabriella Cusella De Angelis, Riccardo Bellazzi
The molecular mechanisms underlying tissue regeneration and wound healing are still poorly understood despite their importance. In this paper we develop a bioinformatics approach, combining biology and network theory to drive experiments for better understanding the genetic underpinnings of wound healing mechanisms and for selecting potential drug targets. We start by selecting literature-relevant genes in murine wound healing, and inferring from them a Protein-Protein Interaction (PPI) network. Then, we analyze the network to rank wound healing-related genes according to their topological properties...
June 21, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28635637/a-short-term-biological-indicator-for-long-term-kidney-damage-after-radionuclide-therapy-in-mice
#2
Giovanni Pellegrini, Klaudia Siwowska, Stephanie Haller, Daniel J Antoine, Roger Schibli, Anja Kipar, Cristina Müller
Folate receptor (FR)-targeted radionuclide therapy using folate radioconjugates is of interest due to the expression of the FR in a variety of tumor types. The high renal accumulation of radiofolates presents, however, a risk of radionephropathy. A potential option to address this challenge would be to use radioprotectants, such as amifostine. Methods for early detection of kidney damage that-in this case-cannot be predicted based on dose estimations, would facilitate the development of novel therapies. The aim of this study was, therefore, to assess potentially changing levels of plasma and urine biomarkers and to determine DNA damage at an early stage after radiofolate application...
June 21, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28632200/the-beginning-and-development-of-the-theranostic-approach-in-nuclear-medicine-as-exemplified-by-the-radionuclide-pair-86-y-and-90-y
#3
Frank Rösch, Hans Herzog, Syed M Qaim
In the context of radiopharmacy and molecular imaging, the concept of theranostics entails a therapy-accompanying diagnosis with the aim of a patient-specific treatment. Using the adequate diagnostic radiopharmaceutical, the disease and the state of the disease are verified for an individual patient. The other way around, it verifies that the radiopharmaceutical in hand represents a target-specific and selective molecule: the "best one" for that individual patient. Transforming diagnostic imaging into quantitative dosimetric information, the optimum radioactivity (expressed in maximum radiation dose to the target tissue and tolerable dose to healthy organs) of the adequate radiotherapeutical is applied to that individual patient...
June 20, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28608822/the-good-the-bad-and-the-ugly-of-glycosaminoglycans-in-tissue-engineering-applications
#4
REVIEW
Bethanie I Ayerst, Catherine L R Merry, Anthony J Day
High sulfation, low cost, and the status of heparin as an already FDA- and EMA- approved product, mean that its inclusion in tissue engineering (TE) strategies is becoming increasingly popular. However, the use of heparin may represent a naïve approach. This is because tissue formation is a highly orchestrated process, involving the temporal expression of numerous growth factors and complex signaling networks. While heparin may enhance the retention and activity of certain growth factors under particular conditions, its binding 'promiscuity' means that it may also inhibit other factors that, for example, play an important role in tissue maintenance and repair...
June 13, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28608799/in-vitro-and-in-vivo-studies-of-alar-nasal-cartilage-using-autologous-micro-grafts-the-use-of-the-rigenera-%C3%A2-protocol-in-the-treatment-of-an-osteochondral-lesion-of-the-nose
#5
Gabriele Ceccarelli, Pietro Gentile, Marco Marcarelli, Martina Balli, Flavio Lorenzo Ronzoni, Laura Benedetti, Maria Gabriella Cusella De Angelis
Cartilage defects represent a serious problem due to the poor regenerative properties of this tissue. Regarding the nose, nasal valve collapse is associated with nasal blockage and persistent airway obstruction associated with a significant drop in the quality of life for patients. In addition to surgical techniques, several cell-based tissue-engineering strategies are studied to improve cartilage support in the nasal wall, that is, to ameliorate wall insufficiency. Nevertheless, there are no congruent data available on the benefit for patients during the follow-up time...
June 13, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28598408/anti-mycobacterial-evaluation-of-7-chloro-4-aminoquinolines-and-hologram-quantitative-structure-activity-relationship-hqsar-modeling-of-amino-imino-tautomers
#6
Marcelle L F Bispo, Camilo H S Lima, Laura N F Cardoso, André L P Candéa, Flávio A F M Bezerra, Maria C S Lourenço, Maria G M O Henriques, Ricardo B Alencastro, Carlos R Kaiser, Marcus V N Souza, Magaly G Albuquerque
In an ongoing research program for the development of new anti-tuberculosis drugs, we synthesized three series (A, B, and C) of 7-chloro-4-aminoquinolines, which were evaluated in vitro against Mycobacterium tuberculosis (MTB). Now, we report the anti-MTB and cytotoxicity evaluations of a new series, D (D01-D21). Considering the active compounds of series A (A01-A13), B (B01-B13), C (C01-C07), and D (D01-D09), we compose a data set of 42 compounds and carried out hologram quantitative structure-activity relationship (HQSAR) analysis...
June 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28587160/advances-in-drug-discovery-of-new-antitubercular-multidrug-resistant-compounds
#7
REVIEW
Guilherme Felipe Dos Santos Fernandes, Chung Man Chin, Jean Leandro Dos Santos
Tuberculosis (TB), a disease caused mainly by the Mycobacterium tuberculosis (Mtb), is according to the World Health Organization (WHO) the infectious disease responsible for the highest number of deaths worldwide. The increased number of multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains, and the ineffectiveness of the current treatment against latent tuberculosis are challenges to be overcome in the coming years. The scenario of drug discovery becomes alarming when it is considered that the number of new drugs does not increase proportionally to the emergence of drug resistance...
June 1, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28561772/chiral-derivatives-of-xanthones-investigation-of-the-effect-of-enantioselectivity-on-inhibition-of-cyclooxygenases-cox-1-and-cox-2-and-binding-interaction-with-human-serum-albumin
#8
Carla Fernandes, Andreia Palmeira, Inês I Ramos, Carlos Carneiro, Carlos Afonso, Maria Elizabeth Tiritan, Honorina Cidade, Paula C A G Pinto, M Lúcia M F S Saraiva, Salette Reis, Madalena M M Pinto
Searching of new enantiomerically pure chiral derivatives of xanthones (CDXs) with potential pharmacological properties, particularly those with anti-inflammatory activity, has remained an area of interest of our group. Herein, we describe in silico studies and in vitro inhibitory assays of cyclooxygenases (COX-1 and COX-2) for different enantiomeric pairs of CDXs. The evaluation of the inhibitory activities was performed by using the COX Inhibitor Screening Assay Kit. Docking simulations between the small molecules (CDXs; known ligands and decoys) and the enzyme targets were undertaken with AutoDock Vina embedded in PyRx-Virtual Screening Tool software...
May 31, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28556793/syntheses-of-radioiodinated-pyrimidine-2-4-6-triones-as-potential-agents-for-non-invasive-imaging-of-matrix-metalloproteinases
#9
Hans-Jörg Breyholz, Klaus Kopka, Michael Schäfers, Stefan Wagner
Dysregulated expression or activation of matrix metalloproteinases (MMPs) is observed in many kinds of live-threatening diseases. Therefore, MMP imaging for example with radiolabelled MMP inhibitors (MMPIs) potentially represents a valuable tool for clinical diagnostics using non-invasive single photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging. This work includes the organic chemical syntheses and in vitro evaluation of five iodinated barbiturate based MMPIs and the selection of derivative 9 for radiosyntheses of isotopologues [(123)I]9 potentially useful for MMP SPECT imaging and [(124)I]9 for MMP PET imaging...
May 30, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28531154/announcing-the-2017-pharmaceuticals-travel-award-for-young-post-doctoral-researchers
#10
EDITORIAL
Jean Jacques Vanden Eynde
Last year, for the first time in its history, our Journal was able to offer a travel grant of 800 CHF to a young researcher in the field of medicinal chemistry.
May 22, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28524118/novel-radiolabeled-bisphosphonates-for-pet-diagnosis-and-endoradiotherapy-of-bone-metastases
#11
REVIEW
Nina Pfannkuchen, Marian Meckel, Ralf Bergmann, Michael Bachmann, Chandrasekhar Bal, Mike Sathekge, Wolfgang Mohnike, Richard P Baum, Frank Rösch
Bone metastases, often a consequence of breast, prostate, and lung carcinomas, are characterized by an increased bone turnover, which can be visualized by positron emission tomography (PET), as well as single-photon emission computed tomography (SPECT). Bisphosphonate complexes of (99m)Tc are predominantly used as SPECT tracers. In contrast to SPECT, PET offers a higher spatial resolution and, owing to the (68)Ge/(68)Ga generator, an analog to the established (99m)Tc generator exists. Complexation of Ga(III) requires the use of chelators...
May 18, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28524111/synthesis-and-pharmacological-properties-of-novel-esters-based-on-monoterpenoids-and-glycine
#12
Mariia Nesterkina, Iryna Kravchenko
Esters based on mono- and bicyclic terpenoids with glycine have been synthesized via Steglich esterification and characterized by ¹H-NMR, IR, and mass spectral studies. Their analgesic and anti-inflammatory activities were investigated after transdermal delivery on models of formalin, capsaicin, and AITC-induced pain, respectively. Glycine esters of menthol and borneol exhibited higher antinociceptive action, whereas eugenol derivative significantly suppressed the development of the inflammatory process. The mechanism of competitive binding between terpenoid esters and TRPA1/TRPV1 agonists was proposed explaining significant analgesic effect of synthesized derivatives...
May 18, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28524095/pkc-in-regenerative-therapy-new-insights-for-old-targets
#13
REVIEW
Marta Rui, Rita Nasti, Emanuele Bignardi, Serena Della Volpe, Giacomo Rossino, Daniela Rossi, Simona Collina
Effective therapies for chronic or non-healing wounds are still lacking. These tissue insults often result in severe clinical complications (i.e., infections and/or amputation) and sometimes lead to patient death. Accordingly, several research groups have focused their efforts in finding innovative and powerful therapeutic strategies to overcome these issues. On the basis of these considerations, the comprehension of the molecular cascades behind these pathological conditions could allow the identification of molecules against chronic wounds...
May 18, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28471403/pathogenesis-and-inhibition-of-flaviviruses-from-a-carbohydrate-perspective
#14
REVIEW
So Young Kim, Bing Li, Robert J Linhardt
Flaviviruses are enveloped, positive single stranded ribonucleic acid (RNA) viruses with various routes of transmission. While the type and severity of symptoms caused by pathogenic flaviviruses vary from hemorrhagic fever to fetal abnormalities, their general mechanism of host cell entry is similar. All pathogenic flaviviruses, such as dengue virus, yellow fever virus, West Nile virus, Japanese encephalitis virus, and Zika virus, bind to glycosaminglycans (GAGs) through the putative GAG binding sites within their envelope proteins to gain access to the surface of host cells...
May 4, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28468287/information-phage-therapy-research-should-report
#15
Stephen T Abedon
Bacteriophages, or phages, are viruses which infect bacteria. A large subset of phages infect bactericidally and, consequently, for nearly one hundred years have been employed as antibacterial agents both within and outside of medicine. Clinically these applications are described as phage or bacteriophage therapy. Alternatively, and especially in the treatment of environments, this practice instead may be described as a phage-mediated biocontrol of bacteria. Though the history of phage therapy has involved substantial clinical experimentation, current standards along with drug regulations have placed a premium on preclinical approaches, i...
April 30, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28420143/biotinylated-chlorin-and-its-zinc-and-indium-complexes-synthesis-and-in-vitro-biological-evaluation-for-photodynamic-therapy
#16
Meden F Isaac-Lam, Dewana M Hammonds
The synthesis and characterization of biotinylated chlorin photosensitizer and the corresponding zinc and indium complexes are described for potential applications in photodynamic therapy (PDT) for cancer. Phototoxicity of the biotin-chlorin conjugate and the metallated complexes was determined in colon carcinoma CT26 cell lines known to overexpress biotin (Vit B₇) receptors. Cell survival assay indicated that the biotinylated chlorin and indium complex showed increased cell growth inhibition than the zinc complex and the starting chlorin (methyl pheophorbide)...
April 15, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28420127/glycosaminoglycan-binding-and-non-endocytic-membrane-translocation-of-cell-permeable-octaarginine-monitored-by-real-time-in-cell-nmr-spectroscopy
#17
Yuki Takechi-Haraya, Kenzo Aki, Yumi Tohyama, Yuichi Harano, Toru Kawakami, Hiroyuki Saito, Emiko Okamura
Glycosaminoglycans (GAGs), which are covalently-linked membrane proteins at the cell surface have recently been suggested to involve in not only endocytic cellular uptake but also non-endocytic direct cell membrane translocation of arginine-rich cell-penetrating peptides (CPPs). However, in-situ comprehensive observation and the quantitative analysis of the direct membrane translocation processes are challenging, and the mechanism therefore remains still unresolved. In this work, real-time in-cell NMR spectroscopy was applied to investigate the direct membrane translocation of octaarginine (R8) into living cells...
April 15, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28398261/novel-proteasome-inhibitors-and-histone-deacetylase-inhibitors-progress-in-myeloma-therapeutics
#18
REVIEW
Saurabh Chhabra
The unfolded protein response is responsible for the detection of misfolded proteins and the coordination of their disposal and is necessary to maintain the cellular homoeostasis. Multiple myeloma cells secrete large amounts of immunoglobulins, proteins that need to be correctly folded by the chaperone system. If this process fails, the misfolded proteins have to be eliminated by the two main garbage-disposal systems of the cell: proteasome and aggresome. The blockade of either of these systems will result in accumulation of immunoglobulins and other toxic proteins in the cytoplasm and cell death...
April 11, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28379203/role-of-trpm7-in-cancer-potential-as-molecular-biomarker-and-therapeutic-target
#19
REVIEW
Nelson S Yee
The transient receptor potential melastatin-subfamily member 7 (TRPM7) is a ubiquitously expressed ion channel with intrinsic kinase activity. Molecular and electrophysiological analyses of the structure and activity of TRPM7 have revealed functional coupling of its channel and kinase activity. Studies have indicated the important roles of TRPM7 channel-kinase in fundamental cellular processes, physiological responses, and embryonic development. Accumulating evidence has shown that TRPM7 is aberrantly expressed and/or activated in human diseases including cancer...
April 5, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28368296/systematic-analysis-of-pharmaceutical-preparations-of-chondroitin-sulfate-combined-with-glucosamine
#20
Gustavo R C Santos, Adriana A Piquet, Bianca F Glauser, Ana M F Tovar, Mariana S Pereira, Eduardo Vilanova, Paulo A S Mourão
Glycosaminoglycans are carbohydrate-based compounds widely employed as nutraceuticals or prescribed drugs. Oral formulations of chondroitin sulfate combined with glucosamine sulfate have been increasingly used to treat the symptoms of osteoarthritis and osteoarthrosis. The chondroitin sulfate of these combinations can be obtained from shark or bovine cartilages and hence presents differences regarding the proportions of 4- and 6-sulfated N-acetyl β-d-galactosamine units. Herein, we proposed a systematic protocol to assess pharmaceutical batches of this combination drug...
April 1, 2017: Pharmaceuticals
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