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https://www.readbyqxmd.com/read/28238034/35-years-of-marine-natural-product-research-in-sweden-cool-molecules-and-models-from-cold-waters
#1
Lars Bohlin, Paco Cárdenas, Anders Backlund, Ulf Göransson
Currents efforts in marine biodiscovery have essentially focused on temperate to tropical shallow water organisms. With more than 6000 species of marine plants and animals, the Kosterfjord area has the richest marine biodiversity in Swedish waters, but it remains understudied. The overall objective of our marine pharmacognosy research is to explore and reveal the pharmacological potential of organisms from this poorly explored region. More generally, we wish to understand aspects of structure-activity relationships of chemical interactions in cold-water marine environment (shallow and deep)...
2017: Progress in Molecular and Subcellular Biology
https://www.readbyqxmd.com/read/28236243/identifying-loop-mediated-protein-protein-interactions-using-loopfinder
#2
Timothy R Siegert, Michael Bird, Joshua A Kritzer
Peptides are an increasingly useful class of molecules, finding unique applications as chemical probes and potential drugs. They are particularly adept at inhibiting protein-protein interactions, which are often difficult to target using small molecules. The identification and rational design of protein-binding epitopes remains a bottleneck in the development of bioactive peptides. One fruitful strategy has been using structured scaffolds to present essential hot spot residues involved in protein-protein recognition, and this process has been greatly advanced by computational tools that can identify hot spot residues...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28235974/acute-effects-of-glucagon-like-peptide-1-glp-19-36-amide-and-exenatide-on-mesenteric-blood-flow-cardiovascular-parameters-and-biomarkers-in-healthy-volunteers
#3
Lasse Bremholm, Ulrik B Andersen, Mads Hornum, Linda Hilsted, Simon Veedfald, Bolette Hartmann, Jens Juul Holst
Glucagon-like peptide-1 (GLP-1, GLP-17-36amide) and its sister peptide glucagon-like peptide 2 (GLP-2) influence numerous intestinal functions and GLP-2 greatly increases intestinal blood flow. We hypothesized that GLP-1 also stimulates intestinal blood flow and that this would impact on the overall digestive and cardiovascular effects of the hormone. To investigate the influence of GLP-1 receptor agonism on mesenteric and renal blood flow and cardiovascular parameters, we carried out a double-blinded randomized clinical trial...
February 2017: Physiological Reports
https://www.readbyqxmd.com/read/28235800/a-trimeric-structural-fusion-of-an-antagonistic-tumor-necrosis-factor-%C3%AE-mutant-enhances-molecular-stability-and-enables-facile-modification
#4
Masaki Inoue, Daisuke Ando, Haruhiko Kamada, Shintaro Taki, Mayumi Niiyama, Yohei Mukai, Takashi Tadokoro, Katsumi Maenaka, Taisuke Nakayama, Yuji Kado, Tsuyoshi Inoue, Yasuo Tsutsumi, Shin-Ichi Tsunoda
Tumor necrosis factor-α (TNF) exerts its biological effect through two types of receptors, p55 TNF receptor (TNFR1) and p75 TNF receptor (TNFR2). An inflammatory response is known to be induced mainly by TNFR1, whereas an anti-inflammatory reaction is thought to be mediated by TNFR2 in some autoimmune diseases. We have been investigating the use of an antagonistic TNF mutant (R1antTNF) to reveal the pharmacological effect of TNFR1-selective inhibition as a new therapeutic modality. Here, we aimed to further improve and optimize the activity and behavior of this mutant protein both in vitro and in vivo...
February 24, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28230187/silencing-salusin-%C3%AE-attenuates-cardiovascular-remodeling-and-hypertension-in-spontaneously-hypertensive-rats
#5
Xing-Sheng Ren, Li Ling, Bing Zhou, Ying Han, Ye-Bo Zhou, Qi Chen, Yue-Hua Li, Yu-Ming Kang, Guo-Qing Zhu
Salusin-β is a bioactive peptide involved in vascular smooth muscle cell proliferation, vascular fibrosis and hypertension. The present study was designed to determine the effects of silencing salusin-β on hypertension and cardiovascular remodeling in spontaneously hypertensive rats (SHR). Thirteen-week-old male SHR and normotensive Wistar-Kyoto rats (WKY) were subjected to intravenous injection of PBS, adenoviral vectors encoding salusin-β shRNA (Ad-Sal-shRNA) or a scramble shRNA. Salusin-β levels in plasma, myocardium and mesenteric artery were increased in SHR...
February 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28228748/chromogranin-a-regulation-of-obesity-and-peripheral-insulin-sensitivity
#6
REVIEW
Gautam K Bandyopadhyay, Sushil K Mahata
Chromogranin A (CgA) is a prohormone and granulogenic factor in endocrine and neuroendocrine tissues, as well as in neurons, and has a regulated secretory pathway. The intracellular functions of CgA include the initiation and regulation of dense-core granule biogenesis and sequestration of hormones in neuroendocrine cells. This protein is co-stored and co-released with secreted hormones. The extracellular functions of CgA include the generation of bioactive peptides, such as pancreastatin (PST), vasostatin, WE14, catestatin (CST), and serpinin...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28228069/recent-advances-in-the-gastric-mucosal-protection-against-stress-induced-gastric-lesions-importance-of-renin-angiotensin-vasoactive-metabolites-gaseous-mediators-and-appetite-peptides
#7
Tomasz Brzozowski, Katarzyna Magierowska, Marcin Magierowski, Agata Ptak-Belowska, Robert Pajdo, Slawomir Kwiecien, Rafal Olszanecki, Ryszard Korbut
Stress is known to cause severe adverse effects in the human gastrointestinal tract including mucosal microbleedings and erosions or even gastric ulceration but the mechanism of these complications has not been fully elucidated. The pathogenesis of stress-induced gastric damage involves the fall in gastric blood flow (GBF), an increase in gastric acid secretion and gastric motility, enhanced adrenergic and cholinergic nerve activity and the rise in gastric mucosal generation of reactive oxygen species. The gastric mucosal defense mechanisms against the deleterious effect of stress include the activation of the hypothalamic-pituitary-adrenal axis which has been linked with glucocorticoids release capable of counteracting of stress-induced gastric lesions...
February 20, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28223047/diversity-in-sequences-post-translational-modifications-and-expected-pharmacological-activities-of-toxins-from-four-conus-species-revealed-by-the-combination-of-cutting-edge-proteomics-transcriptomics-and-bioinformatics
#8
Michel Degueldre, Marion Verdenaud, Garikoitz Legarda, Rebeca Minambres, Sheila Zuniga, Mathieu Leblanc, Nicolas Gilles, Frederic Ducancel, Edwin De Pauw, Loic Quinton
Venomous animals have developed a huge arsenal of reticulated peptides for defense and predation. Based on various scaffolds, they represent a colossal pharmacological diversity, making them top candidates for the development of innovative drugs. Instead of relying on the classical, low-throughput bioassay-guided approach to identify innovative bioactive peptides, this work exploits a recent paradigm to access to venom diversity. This strategy bypasses the classical approach by combining high-throughput transcriptomics, proteomics and bioinformatics cutting-edge technologies to generate reliable peptide sequences...
February 18, 2017: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/28221753/structure-activity-relationships-of-the-competence-stimulating-peptides-csps-in-streptococcus-pneumoniae-reveal-motifs-critical-for-intra-group-and-cross-group-comd-receptor-activation
#9
Yifang Yang, Bimal Koirala, Lucia A Sanchez, Naiya R Phillips, Sally R Hamry, Yftah Tal-Gan
Streptococcus pneumoniae is a highly recombinogenic human pathogen that utilizes the competence stimulating peptide (CSP)-based quorum sensing (QS) circuitry to acquire antibiotic resistance genes from the environment and initiate its attack on the human host. Modulation of QS in this bacterium, either inhibition or activation, can therefore be used to attenuate S. pneumoniae infectivity and slow down pneumococcal resistance development. In this study we set to determine the molecular mechanism that drives CSP:receptor binding and identify CSP-based QS modulators with distinct activity profiles...
February 21, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28220178/a-photo-degradable-supramolecular-hydrogel-for-selective-delivery-of-microrna-into-3d-cultured-cells
#10
Zhengquan Zhou, Qikun Yi, Tingting Xia, Wencui Yin, Adnan A Kadi, Jinbo Li, Yan Zhang
Multi-functional supramolecular hydrogels have emerged as smart biomaterials for diverse biomedical applications. Here we report a multi-functional supramolecular hydrogel formed by the conjugate of the bioactive GRGDS peptide with biaryltetrazole that is the substrate of photo-click reaction. The hydrogel was used as a biocompatible matrix to encapsulate live cells for 3D culture. The presence of the RGD epitope in the hydrogelator enhanced the interaction of the nanofiber with integrin over-expressing cells, which resulted in the selective enhancement in the miRNA delivery into the encapsulated U87 cells...
February 21, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28218804/detection-of-lunasin-in-quinoa-chenopodium-quinoa-willd-and-the-in-vitro-evaluation-of-its-antioxidant-and-anti-inflammatory-activities
#11
Guixing Ren, Yingying Zhu, Zhenxing Shi
BACKGROUND: Lunasin is a novel cancer preventive peptide that has been detected in various plants. However, the presence and bioactivity of lunasin in quinoa has not been demonstrated. RESULTS: Lunasin was detected in quinoa using UPLC-ESI-MS. The content in fifteen quinoa samples ranged from 1.01 × 10(-3) g kg(-1) dry seed to 4.89 × 10(-3) g kg(-1) dry seed. Significant differences (p<0.05) in lunasin content among different cultivars (yy22, xsg86, xsg59, yy30 and yy19) from the same area and the same cultivar from different areas (Hainan, Hebei and Shanxi provinces) were observed...
February 20, 2017: Journal of the Science of Food and Agriculture
https://www.readbyqxmd.com/read/28218671/human-scfvs-that-counteract-bioactivities-of-staphylococcus-aureus-tsst-1
#12
Thunchanok Rukkawattanakul, Nitat Sookrung, Watee Seesuay, Nattawat Onlamoon, Pornphan Diraphat, Wanpen Chaicumpa, Nitaya Indrawattana
Some Staphylococcus aureus isolates produced toxic shock syndrome toxin-1 (TSST-1) which is a pyrogenic toxin superantigen (PTSAg). The toxin activates a large fraction of peripheral blood T lymphocytes causing the cells to proliferate and release massive amounts of pro-inflammatory cytokines leading to a life-threatening multisystem disorder: toxic shock syndrome (TSS). PTSAg-mediated-T cell stimulation circumvents the conventional antigenic peptide presentation to T cell receptor (TCR) by the antigen-presenting cell (APC)...
February 17, 2017: Toxins
https://www.readbyqxmd.com/read/28218527/bioactive-peptides-isolated-from-casein-phosphopeptides-enhance-calcium-and-magnesium-uptake-in-caco-2-cell-monolayers
#13
Yong Cao, Jian-Yin Miao, Guo Liu, Zhen Luo, Zumeng Xia, Fei Liu, Mingfei Yao, Xiaoqiong Cao, Shengwei Sun, Yanyin Lin, Yaqi Lan, Hang Xiao
The ability of casein phosphopeptides (CPPs) to bind and transport minerals has been previously studied. However, the single bioactive peptides responsible for the effects of CPPs have not been identified. This study was to purify calcium-binding peptides from CPPs and to determine their effects on calcium and magnesium uptake by Caco-2 cell monolayers. Five monomer peptides designated P1 to P5 were isolated and the amino acid sequences were determined using LC-MS/MS. Compared with the CPP-free control, all five monomeric peptides exhibited significant enhancing effects on the uptake of calcium and magnesium (P < 0...
February 20, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28217810/-effects-of-intrathecal-administration-of-am22-52-on-mechanical-allodynia-and-ccl2-expression-in-drg-in-bone-cancer-rats
#14
Ya-Juan Chen, Yuan-Hui Huo, Yanguo Hong
The pain peptide adrenomedullin (AM) plays a pivotal role in pathological pain. The present study was designed to investigate the effect of blockade of AM receptor on bone cancer pain (BCP) and its mechanism. BCP was developed by inoculation of Walker 256 mammary gland carcinoma cells in the tibia medullary cavity of Sprague Dawley rats. The selective AM receptor antagonist AM22-52 was administered intrathecally on 15 d after the inoculation. Quantitative real-time PCR was used to detect mRNA level of CC chemokine ligand 2 (CCL2) in dorsal root ganglion (DRG)...
February 25, 2017: Sheng Li Xue Bao: [Acta Physiologica Sinica]
https://www.readbyqxmd.com/read/28216409/structure-and-activity-of-contryphan-vc2-importance-of-the-d-amino-acid-residue
#15
Stephen B Drane, Samuel D Robinson, Christopher A MacRaild, Sandeep Chhabra, Balasubramanyam Chittoor, Rodrigo A V Morales, Eleanor W W Leung, Alessia Belgi, Samuel S Espino, Baldomero M Olivera, Andrea J Robinson, David K Chalmers, Raymond S Norton
In natural proteins and peptides, amino acids exist almost invariably as L-isomers. There are, however, several examples of naturally-occurring peptides containing D-amino acids. In this study we investigated the role of a naturally-occurring D-amino acid in a small peptide identified in the transcriptome of a marine cone snail. This peptide belongs to a family of peptides known as contryphans, all of which contain a single D-amino acid residue. The solution structure of this peptide was solved by NMR, but further investigations with molecular dynamics simulations suggest that its solution behaviour may be more dynamic than suggested by the NMR ensemble...
February 16, 2017: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/28212329/enzyme-assisted-discovery-of-antioxidant-peptides-from-edible-marine-invertebrates-a-review
#16
REVIEW
Tsun-Thai Chai, Yew-Chye Law, Fai-Chu Wong, Se-Kwon Kim
Marine invertebrates, such as oysters, mussels, clams, scallop, jellyfishes, squids, prawns, sea cucumbers and sea squirts, are consumed as foods. These edible marine invertebrates are sources of potent bioactive peptides. The last two decades have seen a surge of interest in the discovery of antioxidant peptides from edible marine invertebrates. Enzymatic hydrolysis is an efficient strategy commonly used for releasing antioxidant peptides from food proteins. A growing number of antioxidant peptide sequences have been identified from the enzymatic hydrolysates of edible marine invertebrates...
February 16, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28197324/-125-i-f56-peptide-as-radioanalysis-agent-targeting-vegfr1-in-mice-xenografted-with-human-gastric-tumor
#17
Hua Zhu, Chuanke Zhao, Fei Liu, Lixin Wang, Junnan Feng, Chengchao Shou, Zhi Yang
(125)I-Radiolabeled F56 peptide was designed as a radioactive analogue of F56 (peptide WHSDMEWWYLLG) to bind with VEGFR1 receptor. It was synthesized in high radiochemical yield and specific activity. The in vitro stability of (125)I-F56 was tested, and the bioactivity of (125)I-F56 was confirmed by both cell uptake and binding affinity measurement in VEGFR1 positive BGC-823 cells. The time-radioactivity relationship and biodistribution of (125)I-F56 tracer were conducted using nude mice bearing human gastric carcinoma BGC-823, by noninvasive micro-SPECT/CT imaging...
February 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28195491/prodrug-like-pegylated-protein-toxin-trichosanthin-for-reversal-of-chemoresistance
#18
Yingzhi Chen, Meng Zhang, Hongyue Jin, Yisi Tang, Aihua Wu, Qin Xu, Yongzhuo Huang
Multidrug resistance (MDR) is a main obstacle in cancer chemotherapy. The MDR mechanisms involve P-glycoprotein (P-gp) overexpression, abnormality of apoptosis-related protein, and altered expression of drug-targeting proteins. Therapeutic proteins are emerging as candidates for overcoming cancer MDR because of not only their large molecular size that potentially circumvents the P-gp-mediated drug efflux but also their distinctive bioactivity distinguished from small-molecular drugs. Herein we report trichosanthin, a plant protein toxin, possesses synergistic effect with paclitaxel (PTX) in the PTX-resistance A549/T nonsmall cell lung cancer (NSCLC) cells, by reversing PTX-caused caspase 9 phosphorylation and inducing caspase 3-dependent apoptosis...
February 14, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28195465/identification-and-relative-quantification-of-bioactive-peptides-sequentially-released-during-simulated-gastrointestinal-digestion-of-commercial-kefir
#19
Yufang Liu, Monika Pischetsrieder
Health-promoting effects of kefir may be partially caused by bioactive peptides. To evaluate their formation or degradation during gastrointestinal digestion, we monitored changes of the peptide profile in a model of (1) oral, (2) gastric, and (3) small intestinal digestion of kefir. Matrix-assisted laser desorption/ionization time-of-flight mass spectroscopy analyses revealed clearly different profiles between digests 2/3 and kefir/digest 1. Subsequent ultraperformance liquid chromatography-electrospray ionization-tandem mass spectrometry identified 92 peptides in total (25, 25, 43, and 30, partly overlapping in kefir and digests 1, 2, and 3, respectively), including 16 peptides with ascribed bioactivity...
February 23, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28192654/self-assembly-of-recombinant-silk-as-a-strategy-for-chemical-free-formation-of-bioactive-coatings-a-real-time-study
#20
Linnea Nilebäck, Jesper Hedin, Mona Widhe, Lotta S Floderus, Annika Krona, Helena Bysell, My Hedhammar
Functionalization of biomaterials with biologically active peptides can improve their performance after implantation. By genetic fusion to self-assembling proteins, the functional peptides can easily be presented on different physical formats. Herein, a chemical-free coating method based on self-assembly of the recombinant spider silk protein 4RepCT is described and used to prepare functional coatings on various biomaterial surfaces. The silk assembly was studied in real-time, revealing the occurrence of continuous assembly of silk proteins onto surfaces and the formation of nanofibrillar structures...
February 21, 2017: Biomacromolecules
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