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https://www.readbyqxmd.com/read/28093944/healing-efficacy-of-fracture-targeted-gsk3%C3%AE-inhibitor-loaded-micelles-for-improved-fracture-repair
#1
Stewart A Low, Chris V Galliford, Yava L Jones-Hall, Jyoti Roy, Jiyuan Yang, Philip S Low, Jindřich Kopeček
AIM: To evaluate the fracture healing capabilities of a GSK3β inhibitor, 6-bromoindirubin-3'-oxime, coupled with an aspartic acid octapeptide in a micellar delivery system. MATERIALS & METHODS: The efficacy of the intravenously administered micelles to accelerate healing of femoral fracture in mice was evaluated. Micro-computed tomography analysis was employed to obtain bone density, total volume, relative volume, trabecular thickness and trabecular spacing. RESULTS: Both fracture bone mineral density and volume were significantly higher in the micelle treatment groups when compared with controls...
January 17, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28055219/integrating-molecular-networking-and-biological-assays-to-target-the-isolation-of-a-cytotoxic-cyclic-octapeptide-samoamide-a-from-an-american-samoan-marine-cyanobacterium
#2
C Benjamin Naman, Ramandeep Rattan, Svetlana E Nikoulina, John Lee, Bailey W Miller, Nathan A Moss, Lorene Armstrong, Paul D Boudreau, Hosana M Debonsi, Frederick A Valeriote, Pieter C Dorrestein, William H Gerwick
Integrating LC-MS/MS molecular networking and bioassay-guided fractionation enabled the targeted isolation of a new and bioactive cyclic octapeptide, samoamide A (1), from a sample of cf. Symploca sp. collected in American Samoa. The structure of 1 was established by detailed 1D and 2D NMR experiments, HRESIMS data, and chemical degradation/chromatographic (e.g., Marfey's analysis) studies. Pure compound 1 was shown to have in vitro cytotoxic activity against several human cancer cell lines in both traditional cell culture and zone inhibition bioassays...
January 5, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/27943639/genetic-prion-disease-experience-of-a-rapidly-progressive-dementia-center-in-the-united-states-and-a-review-of-the-literature
#3
REVIEW
Leonel T Takada, Mee-Ohk Kim, Ross W Cleveland, Katherine Wong, Sven A Forner, Ignacio Illán Gala, Jamie C Fong, Michael D Geschwind
Although prion diseases are generally thought to present as rapidly progressive dementias with survival of only a few months, the phenotypic spectrum for genetic prion diseases (gPrDs) is much broader. The majority have a rapid decline with short survival, but many patients with gPrDs present as slowly progressive ataxic or parkinsonian disorders with progression over a few to several years. A few very rare mutations even present as neuropsychiatric disorders, sometimes with systemic symptoms such as gastrointestinal disorders and neuropathy, progressing over years to decades...
January 2017: American Journal of Medical Genetics. Part B, Neuropsychiatric Genetics
https://www.readbyqxmd.com/read/27929804/familial-creutzfeldt-jakob-disease-case-report-and-role-of-genetic-counseling-in-post-mortem-testing
#4
Kristin Clift, Kimberly Guthrie, Eric W Klee, Nicole Boczek, Margot Cousin, Patrick Blackburn, Paldeep Atwal
Here we present a case of an asymptomatic 53-year-old woman who sought genetic testing for Familial Creutzfeldt-Jakob Disease (fCJD) after learning that her mother had fCJD. The patient's mother had a sudden onset of memory problems and rapidly deteriorating mental faculties in her late 70s, which led to difficulties ambulating, progressive non-fluent aphasia, dysphagia and death within ∼1 y of symptom onset. The cause of death was reported as "rapid onset dementia." The patient's family, unhappy with the vague diagnosis, researched prion disorders online and aggressively pursued causation and submitted frozen brain tissue from the mother to the National Prion Disease Surveillance Center, where testing revealed a previously described 5-octapeptide repeat insertion (5-OPRI) in the prion protein gene (PRNP) that is known to cause fCJD...
November 2016: Prion
https://www.readbyqxmd.com/read/27926796/novel-umami-ingredients-umami-peptides-and-their-taste
#5
REVIEW
Yin Zhang, Chandrasekar Venkitasamy, Zhongli Pan, Wenlong Liu, Liming Zhao
Umami substances are very important for food seasoning and healthy eating. In addition to monosodium glutamate and some nucleotides, recent investigations have revealed that several peptides also exhibit umami taste. In recent years, 52 peptides have been reported to show umami taste, including 24 dipeptides, 16 tripeptides, 5 octapeptides, 2 pentapeptides, 2 hexapeptides, 1 tetrapeptide, 1 heptapeptide, and 1 undecapeptide. Twenty of these peptides have been examined for the present of umami taste. In this review, we have listed these umami peptides based on their category, source, taste, and threshold concentration...
January 2017: Journal of Food Science
https://www.readbyqxmd.com/read/27909427/biocombinatorial-synthesis-of-novel-lipopeptides-by-com-domain-mediated-reprogramming-of-the-plipastatin-nrps-complex
#6
Hongxia Liu, Ling Gao, Jinzhi Han, Zhi Ma, Zhaoxin Lu, Chen Dai, Chong Zhang, Xiaomei Bie
Both donors and acceptors of communication-mediating (COM) domains are essential for coordinating intermolecular communication within nonribosomal peptides synthetases (NRPSs) complexes. Different sets of COM domains provide selectivity, allowing NRPSs to utilize different natural biosynthetic templates. In this study, novel lipopeptides were synthesized by reprogramming the plipastatin biosynthetic machinery. A Thr-to-Asp point mutation was sufficient to shift the selectivity of the donor COM domain of ppsB toward that of ppsD...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/27882474/effects-of-cck-8-and-cystathionine-%C3%AE-lyase-hydrogen-sulfide-system-on-acute-lung-injury-in-rats
#7
Fengjun Tian, Yiling Ling, Yuqin Chen, Zhiyong Wang
Acute lung injury (ALI) is mainly characterized by diffusive injuries to lung epithelium and increased permeability of alveolar-capillary membranes caused by various factors, which leads to pulmonary edema and pulmonary closure. Lipopolysaccharide (LPS), which is the main component of the cell wall of gram-negative bacteria, is one of the most important factors causing pulmonary infection and ALI. More and more reports have indicated that hydrogen sulfide (H2S) is closely correlated with ALI and has anti-inflammation function, while the specific mechanism needs further investigation...
November 24, 2016: Inflammation
https://www.readbyqxmd.com/read/27875906/the-therapeutic-effects-of-cholecystokinin-octapeptide-on-rat-liver-and-kidney-microcirculation-disorder-in-endotoxic-shock
#8
Dong Zhang, Hui Li, Jing Geng, Yingmin Li, Shujin Li, Chunling Ma, Bin Cong, Xiaojing Zhang
OBJECTIVES: Our previous studies demonstrated that pretreatment with cholecystokinin octapeptide (CCK-8) could alleviate endothelial cell injury and reverse abnormal vascular reactivity as well as reduce LPS-induced inflammation cascades, which suggested that CCK-8 plays a potential role in anti-endotoxic shock. The present study aimed to determine the therapeutic effects of CCK-8 on rat liver and kidney microcirculatory perfusion disorder under endotoxic shock (ES) conditions. MATERIALS AND METHODS: Sprague-Dawley rats were induced to lethal endotoxic shock by an injection of LPS...
November 22, 2016: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/27865351/quercetin-relaxes-guinea-pig-gallbladder-strips
#9
Loren Kline, Edward Karpinski
Quercetin, a phytoestrogen and flavonoid, relaxes intestinal and vascular smooth muscle. The purpose of this study was to determine if quercetin had an effect on gallbladder smooth muscle. An in vitro technique was used to determine the effects of quercetin on gallbladder strips and which system(s) mediated the relaxation. Paired t tests were used; differences between means of P < .05 were considered significant. Adding quercetin before cholecystokinin or KCl produced a significant (P < .001) decrease in the amount of tension (0...
October 2016: Nutrition Research
https://www.readbyqxmd.com/read/27855337/osteotropic-peptide-mediated-bone-targeting-for-photothermal-treatment-of-bone-tumors
#10
Yitong Wang, Jian Yang, Hongmei Liu, Xinyu Wang, Zhengjie Zhou, Quan Huang, Dianwen Song, Xiaopan Cai, Lin Li, Kaili Lin, Jianru Xiao, Peifeng Liu, Qiang Zhang, Yiyun Cheng
The treatment of bone tumors is a challenging problem due to the inefficient delivery of therapeutics to bone and the bone microenvironment-associated tumor resistance to chemo- and radiotherapy. Here, we developed a bone-targeted nanoparticle, aspartate octapeptide-modified dendritic platinum-copper alloy nanoparticle (Asp-DPCN), for photothermal therapy (PTT) of bone tumors. Asp-DPCN showed much higher affinity toward hydroxyapatite and bone fragments than the non-targeted DPCN in vitro. Furthermore, Asp-DPCN accumulated more efficiently around bone tumors in vivo, and resulted in a higher temperature in bone tumors during PTT...
November 9, 2016: Biomaterials
https://www.readbyqxmd.com/read/27832662/effects-of-exogenous-interleukin-9-on-the-growth-proliferation-and-activity-of-interstitial-cells-of-cajal-cultured-in-vitro
#11
Lei Huang, Baofeng Du, Yaoyao Gong, Hairong Xu, Jia Lu, Xinmin Si
OBJECTIVES: To evaluate the role of exogenous interleukin-9 (IL-9) in the growth, proliferation and activity of interstitial cells of Cajal (ICCs) cultured in vitro, and to assess its role in maintaining the functions of ICCs. METHODS: ICCs of murine gastric antrum were isolated and cultured in vitro. ICCs were identified with c-Kit and ANO1 immunofluorescent antibodies. Both fluorescence microscope and confocal microscopy were used to observe the effects of IL-9 on the growth, proliferation and activity of ICCs in cultured in vitro...
2016: Digestion
https://www.readbyqxmd.com/read/27715017/radiosynthesis-and-preclinical-evaluation-of-18-f-fluoroglycosylated-octreotate-for-somatostatin-receptor-imaging
#12
Simone Maschauer, Marcus Heilmann, Carmen Wängler, Ralf Schirrmacher, Olaf Prante
Short synthetic octapeptide analogs derived from the native somatostatin peptides SST-14 and SST-28, namely, octreotate (TATE) or octreotide (TOC), bind with high affinity to somatostatin receptors (sstr), mainly to subtypes 2 and 5, which are expressed in high density on neuroendocrine tumors (NET). Therefore, radiolabeled TATE or TOC derivatives represent highly valuable imaging probes for NET diagnosis by positron emission tomography (PET). The aim of our study was the development of an (18)F-labeled octreotate analog as an alternative radiotracer for the clinically established (68)Ga-DOTATOC and (68)Ga-DOTATATE...
November 16, 2016: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/27713939/novel-tubulin-targeted-cell-penetrating-antimitotic-octapeptide
#13
Debmalya Bhunia, Saswat Mohapatra, Prashant Kurkute, Subhajit Ghosh, Batakrishna Jana, Prasenjit Mondal, Abhijit Saha, Gaurav Das, Surajit Ghosh
An antimitotic cell penetrating octapeptide containing single Arg amino acid is discovered, which strongly binds with the exchangeable GTP/GDP binding site of tubulin, inhibits tubulin polymerization, reduces kinesin driven microtubule motility, activates apoptotic and mitotic check point proteins, induces apoptotic death and significantly inhibits the multicellular tumor spheroid growth of HeLa cells.
October 18, 2016: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/27634327/use-of-an-octapeptide-guanidiniocarbonylpyrrole-conjugate-for-the-formation-of-a-supramolecular-%C3%AE-helix-that-self-assembles-into-ph-responsive-fibers
#14
Mao Li, Marijana Radić Stojković, Martin Ehlers, Elio Zellermann, Ivo Piantanida, Carsten Schmuck
Peptides that adopt β-helix structures are predominantly found in transmembrane protein domains or in the lipid bilayer of vesicles. Constructing a β-helix structure in pure water has been considered difficult without the addition of membrane mimics. Herein, we report such an example; peptide 1 self-assembles into a supramolecular β-helix in pure water based on charge interactions between the individual peptides. Peptide 1 further showed intriguing transitions from small particles to helical fibers in a time-dependent process...
October 10, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27633684/peptide-therapeutics-and-the-pharmaceutical-industry-barriers-encountered-translating-from-the-laboratory-to-patients
#15
John Rafferty, Hema Nagaraj, Alice P McCloskey, Rawan Huwaitat, Simon Porter, Alyaa Albadr, Garry Laverty
Peptides are receiving increasing interest as clinical therapeutics. These highly tunable molecules can be tailored to achieve desirable biocompatibility and biodegradability with simultaneously selective and potent therapeutic effects. Despite challenges regarding up-scaling and licensing of peptide products, their vast clinical potential is reflected in the 60 plus peptide-based therapeutics already on the market, and the further 500 derivatives currently in developmental stages. Peptides are proving effective for a multitude of disease states including: type 2 diabetes (controlled using the licensed glucagon-like peptide-1 receptor liraglutide); irritable bowel syndrome managed with linaclotide (currently at approval stages); acromegaly (treated with octapeptide somostatin analogues lanreotide and octreotide); selective or broad spectrum microbicidal agents such as the Gram-positive selective PTP-7 and antifungal heliomicin; anticancer agents including goserelin used as either adjuvant or monotherapy for prostate and breast cancer, and the first marketed peptide derived vaccine against prostate cancer, sipuleucel-T...
September 9, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27629560/prnp-prion-protein-regulates-the-secretion-of-exosomes-modulating-cav1-caveolin-1-suppressed-autophagy
#16
Marcos V S Dias, Bianca L Teixeira, Bruna R Rodrigues, Rita Sinigaglia-Coimbra, Isabel Porto-Carreiro, Martín Roffé, Glaucia N M Hajj, Vilma R Martins
Prion protein modulates many cellular functions including the secretion of trophic factors by astrocytes. Some of these factors are found in exosomes, which are formed within multivesicular bodies (MVBs) and secreted into the extracellular space to modulate cell-cell communication. The mechanisms underlying exosome biogenesis were not completely deciphered. Here, we demonstrate that primary cultures of astrocytes and fibroblasts from prnp-null mice secreted lower levels of exosomes than wild-type cells. Furthermore, prnp-null astrocytes exhibited reduced MVB formation and increased autophagosome formation...
November 2016: Autophagy
https://www.readbyqxmd.com/read/27539647/novel-members-of-the-adipokinetic-hormone-family-in-beetles-of-the-superfamily-scarabaeoidea
#17
Gerd Gäde, Petr Šimek, Heather G Marco
Eight beetle species of the superfamily Scarabaeoidea were investigated with respect to peptides belonging to the adipokinetic hormone (AKH) family in their neurohemal organs, the corpora cardiaca (CC). The following beetle families are represented: Scarabaeidae, Lucanidae, and Geotrupidae. AKH peptides were identified through a heterospecific trehalose-mobilizing bioassay and by sequence analyses, using liquid chromatography coupled to positive electrospray mass spectrometry (LC-ESI-MS) and analysis of the tandem MS(2) spectra obtained by collision-induced dissociation...
August 18, 2016: Amino Acids
https://www.readbyqxmd.com/read/27539268/homooligomeric-%C3%AE-3-r-valine-peptides-transformation-between-c14-and-c12-helical-structures-induced-by-a-guest-aib-residue
#18
Basavalingappa Vasantha, Gijo George, Srinivasarao Raghothama, Padmanabhan Balaram
Novel helical, structures unprecedented in the chemistry of α-polypeptides, may be found in polypeptides containing β and γ amino acids. The structural characterization of C12 and C14 -helices in oligo β-peptides was originally achieved using conformationally constrained cyclic β-residues. This study explores the conformational characteristics of proteinogenic β(3) residues in homooligomeric sequences and addresses the issue of inducing a transition between C14 and C12 helices by the introduction of a guest α-residue...
August 19, 2016: Biopolymers
https://www.readbyqxmd.com/read/27537101/from-bulk-to-plasmonic-nanoparticle-surfaces-the-behavior-of-two-potent-therapeutic-peptides-octreotide-and-pasireotide
#19
Belén Hernández, Eduardo López-Tobar, Santiago Sanchez-Cortes, Yves-Marie Coïc, Bruno Baron, Alexandre Chenal, Sergei G Kruglik, Fernando Pflüger, Régis Cohen, Mahmoud Ghomi
Octreotide and pasireotide are two cyclic somatostatin analogues with an important clinical use in the treatment and diagnosis of neuroendocrine tumors. Herein, by the combined use of several techniques (UV-visible absorption, fluorescence, circular dichroism, ζ-potential, transmission electron microscopy, Raman scattering, surface-enhanced Raman scattering, and quantum mechanical calculations) we have followed the structural dynamics of these analogues in the bulk, as well as their binding sites on plasmonic (gold and silver) colloids...
September 21, 2016: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/27518404/exploration-of-the-bf2-15-major-histocompatibility-complex-class-i-binding-motif-and-identification-of-cytotoxic-t-lymphocyte-epitopes-from-the-h5n1-influenza-virus-nucleoprotein-in-chickens
#20
Weijun Zhang, Qinghua Huang, Mei Lu, Fengzhu Zhu, Yan-Yan Huang, Shao-Hua Yang, Zhengjie Kong, Xiu-Mei Zhang, Chuan-Tian Xu
The binding motif of BF2*15 major histocompatibility complex (MHC) class I was explored by analyzing the interaction between an infectious bronchitis virus octapeptide and BF2*15, and the cytotoxic T lymphocyte (CTL) epitope from the nucleoprotein (NP) of H5N1 virus was identified using experimental methods. Computational methods, including homology modeling, molecular dynamics simulation, and molecular docking analysis, were used. The recombinant plasmid pCAGGS-NP was constructed, and NP expression was confirmed by indirect immunofluorescence and Western blot in transfected 293T cells...
November 2016: Archives of Virology
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