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Pharmaceuticals

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https://www.readbyqxmd.com/read/28531154/announcing-the-2017-pharmaceuticals-travel-award-for-young-post-doctoral-researchers
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
https://www.readbyqxmd.com/read/28358322/development-of-trpm8-antagonists-to-treat-chronic-pain-and-migraine
#12
REVIEW
Andy D Weyer, Sonya G Lehto
A review. Development of pharmaceutical antagonists of transient receptor potential melastatin 8 (TRPM8) have been pursued for the treatment of chronic pain and migraine. This review focuses on the current state of this progress.
March 30, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28353658/development-of-a-glycosaminoglycan-derived-selectin-targeting-anti-adhesive-coating-to-treat-endothelial-cell-dysfunction
#13
James R Wodicka, Andrea M Chambers, Gurneet S Sangha, Craig J Goergen, Alyssa Panitch
Endothelial cell (EC) dysfunction is associated with many disease states including deep vein thrombosis (DVT), chronic kidney disease, sepsis and diabetes. Loss of the glycocalyx, a thin glycosaminoglycan (GAG)-rich layer on the EC surface, is a key feature of endothelial dysfunction and increases exposure of EC adhesion molecules such as selectins, which are involved in platelet binding to ECs. Once bound, platelets cause thrombus formation and an increased inflammatory response. We have developed a GAG derived, selectin targeting anti-adhesive coating (termed EC-SEAL) consisting of a dermatan sulfate backbone and multiple selectin-binding peptides designed to bind to inflamed endothelium and prevent platelet binding to create a more quiescent endothelial state...
March 29, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28346371/modulation-of-trp-channel-activity-by-hydroxylation-and-its-therapeutic-potential
#14
REVIEW
Yagnesh Nagarajan, Grigori Y Rychkov, Daniel J Peet
Two transient receptor potential (TRP) channels-TRPA1 and TRPV3-are post-translationally hydroxylated, resulting in oxygen-dependent regulation of channel activity. The enzymes responsible are the HIF prolyl hydroxylases (PHDs) and the asparaginyl hydroxylase factor inhibiting HIF (FIH). The PHDs and FIH are well characterized for their hydroxylation of the hypoxic inducible transcription factors (HIFs), mediating their hypoxic regulation. Consequently, these hydroxylases are currently being targeted therapeutically to modulate HIF activity in anemia, inflammation, and ischemic disease...
March 27, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28346368/pathophysiological-significance-of-dermatan-sulfate-proteoglycans-revealed-by-human-genetic-disorders
#15
REVIEW
Shuji Mizumoto, Tomoki Kosho, Shuhei Yamada, Kazuyuki Sugahara
The indispensable roles of dermatan sulfate-proteoglycans (DS-PGs) have been demonstrated in various biological events including construction of the extracellular matrix and cell signaling through interactions with collagen and transforming growth factor-β, respectively. Defects in the core proteins of DS-PGs such as decorin and biglycan cause congenital stromal dystrophy of the cornea, spondyloepimetaphyseal dysplasia, and Meester-Loeys syndrome. Furthermore, mutations in human genes encoding the glycosyltransferases, epimerases, and sulfotransferases responsible for the biosynthesis of DS chains cause connective tissue disorders including Ehlers-Danlos syndrome and spondyloepimetaphyseal dysplasia with joint laxity characterized by skin hyperextensibility, joint hypermobility, and tissue fragility, and by severe skeletal disorders such as kyphoscoliosis, short trunk, dislocation, and joint laxity...
March 27, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28333082/an-updated-view-on-an-emerging-target-selected-papers-from-the-8th-international-conference-on-protein-kinase-ck2
#16
EDITORIAL
Joachim Jose, Marc Le-Borgne, Lorenzo A Pinna, Mathias Montenarh
n/a.
March 23, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28300791/anacardic-acid-constituents-from-cashew-nut-shell-liquid-nmr-characterization-and-the-effect-of-unsaturation-on-its-biological-activities
#17
Selene M Morais, Katherine A Silva, Halisson Araujo, Icaro G P Vieira, Daniela R Alves, Raquel O S Fontenelle, Artur M S Silva
Anacardic acids are the main constituents of natural cashew nut shell liquid (CNSL), obtained via the extraction of cashew shells with hexane at room temperature. This raw material presents high technological potential due to its various biological properties. The main components of CNSL are the anacardic acids, salicylic acid derivatives presenting a side chain of fifteen carbon atoms with different degrees of unsaturation (monoene-15:1, diene-15:2, and triene-15:3). Each constituent was isolated by column chromatography using silica gel impregnated with silver nitrate...
March 16, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28300769/aptamers-biomedical-interest-and-applications
#18
EDITORIAL
Cristina Romero-López, Alfredo Berzal-Herranz
Aptamers are short DNA or RNA oligonucleotides specialized in the specific and efficient binding to a target molecule. They are obtained by in vitro selection or evolution processes. It was in 1990 that two independent research groups described the bases of a new in vitro technology for the identification of RNA molecules able to specifically bind to a target [1,2]. Tuerk and Gold established the principals of the in vitro selection process that was named SELEX (Systematic Evolution of Ligands by Exponential enrichment), which is based on iterative cycles of binding, partitioning, and amplification of oligonucleotides from a pool of variant sequences [2]...
March 16, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28295000/current-status-of-radiopharmaceuticals-for-the-theranostics-of-neuroendocrine-neoplasms
#19
REVIEW
Melpomeni Fani, Petra Kolenc Peitl, Irina Velikyan
Nuclear medicine plays a pivotal role in the management of patients affected by neuroendocrine neoplasms (NENs). Radiolabeled somatostatin receptor analogs are by far the most advanced radiopharmaceuticals for diagnosis and therapy (radiotheranostics) of NENs. Their clinical success emerged receptor-targeted radiolabeled peptides as an important class of radiopharmaceuticals and it paved the way for the investigation of other radioligand-receptor systems. Besides the somatostatin receptors (sstr), other receptors have also been linked to NENs and quite a number of potential radiolabeled peptides have been derived from them...
March 15, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28287433/theranostic-value-of-multimers-lessons-learned-from-trimerization-of-neurotensin-receptor-ligands-and-other-targeting-vectors
#20
Simone Maschauer, Jürgen Einsiedel, Dominik Reich, Harald Hübner, Peter Gmeiner, Hans-Jürgen Wester, Olaf Prante, Johannes Notni
Neurotensin receptor 1 (NTS1) is overexpressed on a variety of cancer entities; for example, prostate cancer, ductal pancreatic adenocarcinoma, and breast cancer. Therefore, it represents an interesting target for the diagnosis of these cancers types by positron emission tomography (PET) [...].
March 10, 2017: Pharmaceuticals
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