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https://www.readbyqxmd.com/read/28915041/preorganized-cyclic-%C3%AE-%C3%AE-disubstituted-%C3%AE-amino-acids-bearing-functionalized-side-chains-that-act-as-peptide-helix-inducers
#1
Hiroyuki Kobayashi, Takashi Misawa, Kenji Matsuno, Yosuke Demizu
Preorganized cyclic α,α-disubstituted α-amino acids (dAA) bearing functionalized side chains that acted as peptide-helix inducers, which could be used for solid-phase peptide synthesis, were designed and synthesized. Furthermore, a helical octapeptide with the following amino acid sequence was prepared, and its preferred conformation was analyzed based on its CD spectra: Ac-X(1)EYSAX(2)KA-NH2 (11: X(1) = Api(C4N3), X(2) = Ac6c). The side-chain azido functional group of peptide 11 was efficiently converted to various 1,2,3-triazole groups via Huisgen 1,3-dipolar cycloaddition reactions involving different types of alkynes...
September 15, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28889973/origin-of-the-reflectin-gene-and-hierarchical-assembly-of-its-protein
#2
Zhe Guan, Tiantian Cai, Zhongmin Liu, Yunfeng Dou, Xuesong Hu, Peng Zhang, Xin Sun, Hongwei Li, Yao Kuang, Qiran Zhai, Hao Ruan, Xuanxuan Li, Zeyang Li, Qihui Zhu, Jingeng Mai, Qining Wang, Luhua Lai, Jianguo Ji, Haiguang Liu, Bin Xia, Taijiao Jiang, Shu-Jin Luo, Hong-Wei Wang, Can Xie
Cephalopods, the group of animals including octopus, squid, and cuttlefish, have remarkable ability to instantly modulate body coloration and patterns so as to blend into surrounding environments [1, 2] or send warning signals to other animals [3]. Reflectin is expressed exclusively in cephalopods, filling the lamellae of intracellular Bragg reflectors that exhibit dynamic iridescence and structural color change [4]. Here, we trace the possible origin of the reflectin gene back to a transposon from the symbiotic bioluminescent bacterium Vibrio fischeri and report the hierarchical structural architecture of reflectin protein...
August 31, 2017: Current Biology: CB
https://www.readbyqxmd.com/read/28866879/versatility-of-prolyl-oligopeptidase-b-in-peptide-macrocyclization
#3
Robert Michael Sgambelluri, Miranda O Smith, Jonathan D Walton
Cyclic peptides are promising compounds for new chemical biological tools and therapeutics due to their structural diversity, resistance to proteases, and membrane permeability. Amatoxins, the toxic principles of poisonous mushrooms, are biosynthesized on ribosomes as 35-mer precursor peptides which are ultimately converted to hydroxylated bicyclic octapeptides. The initial cyclization steps, catalyzed by a dedicated prolyl oligopeptidase (POPB), involves removal of the 10-amino acid leader sequence from the precursor peptide and transpeptidation to produce a monocyclic octapeptide intermediate...
September 2, 2017: ACS Synthetic Biology
https://www.readbyqxmd.com/read/28820061/renin-angiotensin-system-and-cytokines-in-chronic-kidney-disease-clinical-and-experimental-evidence
#4
Ariadna Andrade Saldanha Silva, Beranardo Bahia Finotti, Amanda Oliveira Lauar, Thiago Ruiz Rodrigues Prestes, Ana Cristina Simões E Silva
Chronic kidney disease (CKD) has become a major public health problem in Brazil and worldwide. There are many causes of CKD, being the congenital anomalies of the kidney and urinary tract and the glomerular diseases very common in pediatric patients, while diabetic nephropathy, CKD due to chronic arterial hypertension and glomerular diseases are predominant in adult patients. Many endogenous mediators have been related to the pathophysiology of CKD, being relevant the effects of the renin-angiotensin system (RAS) and the immune-inflammatory mediators including cytokines...
August 18, 2017: Protein and Peptide Letters
https://www.readbyqxmd.com/read/28819428/development-of-a-new-analog-of-sgk1-inhibitor-and-its-evaluation-as-a-therapeutic-molecule-of-colorectal-cancer
#5
Xuchun Liang, Chunling Lan, Jinzhe Zhou, Wencheng Fu, Xuesha Long, Yu An, Guanming Jiao, Kejin Wang, Yongqin Li, Jiahong Xu, Qi Huang, Bin Xu, Junjie Xiao
Colorectal cancer (CRC) is one of the most leading causes of cancer-related death worldwide. The serum and glucocorticoid inducible kinase SGK1 is highly expressed and involved in several tumors. GSK650394, a SGK1 inhibitor, has been proved to be effective in impeding tumor growth in vitro. In this study, we developed a novel analog of GSK650394, and evaluated its effects on CRC cells and tumor growth both in vitro and in vivo. HCT116 cells were treated with a concentration gradient of new developed compounds and cholecystokinin octapeptide (CCK-8) assay was used to calculate the IC50 value of every analog...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/28790989/a-proposal-for-a-structural-model-of-the-feline-calicivirus-protease-bound-to-the-substrate-peptide-under-physiological-conditions
#6
Masaru Yokoyama, Tomoichiro Oka, Hirotaka Takagi, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Yukinobu Tohya, Hironori Sato
Feline calicivirus (FCV) protease functions to cleave viral precursor proteins during productive infection. Previous studies have mapped a protease-coding region and six cleavage sites in viral precursor proteins. However, how the FCV protease interacts with its substrates remains unknown. To gain insights into the interactions, we constructed a molecular model of the FCV protease bound with the octapeptide containing a cleavage site of the capsid precursor protein by homology modeling and docking simulation...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28757640/effects-of-peripheral-administration-of-a-neuromedin-u-receptor-2-selective-agonist-on-food-intake-and-body-weight-in-obese-mice
#7
T Kaisho, H Nagai, T Asakawa, N Suzuki, H Fujita, K Matsumiya, N Nishizawa, Y Kanematsu-Yamaki, K Dote, J-I Sakamoto, T Asami, S Takekawa
BACKGROUND: Neuromedin U (NMU) is a neuropeptide with various physiological functions including regulation of smooth-muscle contraction, blood pressure, stress responses, and feeding behaviors. NMU activates two distinct receptors, NMUR1 and NMUR2, which are predominantly expressed in peripheral tissues and the central nervous system, respectively. It is reported that the NMU signaling system regulates food intake and body weight via NMUR2, suggesting that an NMUR2 agonist exhibiting anorectic effects would be a potential therapy for obesity...
July 31, 2017: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/28753966/identification-of-a-novel-vasodilatory-octapeptide-from-the-skin-secretion-of-the-african-hyperoliid-frog-kassina-senegalensis
#8
Qiang Du, Hui Wang, Chengbang Ma, Yue Wu, Xinping Xi, Mei Zhou, Tianbao Chen, Chris Shaw, Lei Wang
The defensive skin secretions of amphibians continue to be an excellent source of novel biologically-active peptides. Here we report the identification and pharmacological activity of a novel C-terminally amided myotropic octapeptide from the skin secretion of the African hyperoliid frog, Kassina senegalensis. The 8-amino acid peptide has the following primary structure: WMSLGWSL-amide and has a molecular mass of 978 Da. The primary structure and organisation of the biosynthetic precursor of WL-8 amide was successfully deduced from cloned skin secretion-derived cDNA...
July 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28710552/the-african-froghopper-ptyelus-flavescens-suborder-cicadomorpha-contains-two-novel-and-one-known-peptides-of-the-adipokinetic-hormone%C3%A2-akh-family-structure-function-and-comparison-with-aphid-akh-suborder-sternorrhyncha
#9
Gerd Gäde, Petr Šimek, Heather G Marco
The rationale of "green pesticides" in food security is to use information about endogenous hormones of pest insects to make peptide mimetics that will act against the pest insects to alter their behaviour or physiology, while taking care not to harm beneficial insects or other organisms in the food chain. Such "green" insecticides are designed thus, on the basis of neuropeptide ligand-receptor interaction and it is of paramount interest to have finally a mimetic at hand that is harmful only to pest insects...
July 14, 2017: Amino Acids
https://www.readbyqxmd.com/read/28704418/the-coll%C3%AE-gen-iii-fibril-has-a-flexi-rod-structure-of-flexible-sequences-interspersed-with-rigid-bioactive-domains-including-two-with-hemostatic-roles
#10
J Des Parkin, James D San Antonio, Anton V Persikov, Hayat Dagher, Raymond Dalgleish, Shane T Jensen, Xavier Jeunemaitre, Judy Savige
Collagen III is critical to the integrity of blood vessels and distensible organs, and in hemostasis. Examination of the human collagen III interactome reveals a nearly identical structural arrangement and charge distribution pattern as for collagen I, with cell interaction domains, fibrillogenesis and enzyme cleavage domains, several major ligand-binding regions, and intermolecular crosslink sites at the same sites. These similarities allow heterotypic fibril formation with, and substitution by, collagen I in embryonic development and wound healing...
2017: PloS One
https://www.readbyqxmd.com/read/28659922/a-poly-lactic-co-glycolic-acid-nanovaccine-based-on-chimeric-peptides-from-different-leishmania-infantum-proteins-induces-dendritic-cells-maturation-and-promotes-peptide-specific-ifn%C3%AE-producing-cd8-t-cells-essential-for-the-protection-against-experimental-visceral
#11
Evita Athanasiou, Maria Agallou, Spyros Tastsoglou, Olga Kammona, Artemis Hatzigeorgiou, Costas Kiparissides, Evdokia Karagouni
Visceral leishmaniasis, caused by Leishmania (L.) donovani and L. infantum protozoan parasites, can provoke overwhelming and protracted epidemics, with high case-fatality rates. An effective vaccine against the disease must rely on the generation of a strong and long-lasting T cell immunity, mediated by CD4(+) TH1 and CD8(+) T cells. Multi-epitope peptide-based vaccine development is manifesting as the new era of vaccination strategies against Leishmania infection. In this study, we designed chimeric peptides containing HLA-restricted epitopes from three immunogenic L...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28648738/current-topics-in-angiotensin-ii-type-1-receptor-research-focus-on-inverse-agonism-receptor-dimerization-and-biased-agonism
#12
REVIEW
Takanobu Takezako, Hamiyet Unal, Sadashiva S Karnik, Koichi Node
Although the octapeptide hormone angiotensin II (Ang II) regulates cardiovascular and renal homeostasis through the Ang II type 1 receptor (AT1R), overstimulation of AT1R causes various human diseases, such as hypertension and cardiac hypertrophy. Therefore, AT1R blockers (ARBs) have been widely used as therapeutic drugs for these diseases. Recent basic research and clinical studies have resulted in the discovery of interesting phenomena associated with AT1R function. For example, ligand-independent activation of AT1R by mechanical stress and agonistic autoantibodies, as well as via receptor mutations, has been shown to decrease the inverse agonistic efficacy of ARBs, though the molecular mechanisms of such phenomena had remained elusive until recently...
September 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28620971/the-adipokinetic-hormone-of-the-coleopteran-suborder-adephaga-structure-function-and-comparison-of-distribution-in-other-insects
#13
Gerd Gäde, Heather G Marco
The aim of the current study is to identify the adipokinetic hormone(s) (AKHs) of a basal suborder of the species-rich Coleoptera, the Adephaga, and possibly learn more about the ancestral AKH of beetles. Moreover, we wanted to compare the ancestral AKH with AKHs of more advanced beetles, of which a number are pest insects. This would allow us to assess whether AKH mimetics would be suitable as insecticides, that is, be harmful to the pest species but not to the beneficial species. Nine species of the Adephaga were investigated and all synthesize only one octapeptide in the corpus cardiacum, as revealed by Edman degradation sequencing techniques or by mass spectrometry...
June 16, 2017: Archives of Insect Biochemistry and Physiology
https://www.readbyqxmd.com/read/28617610/total-synthesis-of-the-cyclic-dodecapeptides-wewakazole-and-wewakazole-b
#14
Martyn Inman, Hannah L Dexter, Christopher J Moody
The cyclic dodecapeptides wewakazole and wewakazole B have been synthesized by a divergent strategy via a common tris-proline containing oxazole octapeptide and two separate bis-oxazole containing tetrapeptide units, followed by peptide coupling and macrocyclization. The three oxazole amino acid fragments are readily accessible by rhodium(II)-catalyzed amide N-H insertion of diazocarbonyl compounds, or by the cycloaddition of rhodium carbenoids with nitriles.
June 15, 2017: Organic Letters
https://www.readbyqxmd.com/read/28611581/glial-endozepines-inhibit-feeding-related-autonomic-functions-by-acting-at-the-brainstem-level
#15
Florent Guillebaud, Clémence Girardet, Anne Abysique, Stéphanie Gaigé, Rym Barbouche, Jérémy Verneuil, André Jean, Jérôme Leprince, Marie-Christine Tonon, Michel Dallaporta, Bruno Lebrun, Jean-Denis Troadec
Endozepines are endogenous ligands for the benzodiazepine receptors and also target a still unidentified GPCR. The endozepine octadecaneuropeptide (ODN), an endoproteolytic processing product of the diazepam-binding inhibitor (DBI) was recently shown to be involved in food intake control as an anorexigenic factor through ODN-GPCR signaling and mobilization of the melanocortinergic signaling pathway. Within the hypothalamus, the DBI gene is mainly expressed by non-neuronal cells such as ependymocytes, tanycytes, and protoplasmic astrocytes, at levels depending on the nutritional status...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28548677/destabilization-of-human-insulin-fibrils-by-peptides-of-fruit-bromelain-derived-from-ananas-comosus-pineapple
#16
Sromona Das, Debasish Bhattacharyya
Deposition of insulin aggregates in human body leads to dysfunctioning of several organs. Effectiveness of fruit bromelain from pineapple in prevention of insulin aggregate was investigated. Proteolyses of bromelain was done as par human digestive system and the pool of small peptides was separated from larger peptides and proteins. Under conditions of growth of insulin aggregates from its monomers, this pool of peptides restricted the reaction upto formation of oligomers of limited size. These peptides also destabilized preformed insulin aggregates to oligomers...
May 26, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28490115/mechanistic-insights-into-tyrosinase-mediated-crosslinking-of-soy-glycinin-derived-peptides
#17
Sivan Isaschar-Ovdat, Ayelet Fishman
Tyrosinase from Bacillus megaterium (TyrBm) was previously used to modulate soy glycinin-based emulsions and gels. To study the crosslinking mechanism, TyrBm oxidation of three tyrosine-containing octapeptides derived from glycinin was analyzed by oxygen consumption measurements, absorbance and mass spectrometry. A significant lag period and lower activity were measured when tyrosine was located in the middle of the peptide chain. Mass spectrometry analysis showed that these peptides are crosslinked via the oxidative quinone ring of the tyrosine residue by aryl-alkylamine addition or aryloxy radical coupling to form di-DOPA (3,4-dihydroxyphenylalanine)...
October 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28470351/cck1-receptor-is-involved-in-the-regulation-of-protein-lysine-acetylation-in-gbc-sd-cells-and-gallbladder-carcinoma
#18
W Wu, B Ouyang, Z Lu, H Liu, Y Tan, P Cui
BACKGROUND: CCK1 (cholecystokinin receptor 1) and protein lysine acetylation were associated with several cancers, respectively. However, whether they are involved in the alternation of gallbladder carcinoma is unknown. AIMS: This study investigated the characteristics of CCK1 and protein lysine acetylation in GBC-SD cells and carcinoma of gallbladder. METHODS: The expression and localization of CCK1 were detected by western blot analysis and indirect immunofluorescence...
May 3, 2017: Irish Journal of Medical Science
https://www.readbyqxmd.com/read/28400225/pegylated-neuromedin-u-8-shows-long-lasting-anorectic-activity-and-anti-obesity-effect-in-mice-by-peripheral-administration
#19
Yasushi Masuda, Satoshi Kumano, Jiro Noguchi, Kotaro Sakamoto, Hiroshi Inooka, Tetsuya Ohtaki
Neuromedin U (NMU) is a neuropeptide found in the brain and gastrointestinal tract. The NMU system has been shown to regulate energy homeostasis by both a central and a peripheral mechanism. Peripheral administration of human NMU-25 was recently shown to inhibit food intake in mice. We examined the possibility that other NMU-related peptides exert an anorectic activity by intraperitoneal (i.p.) administration. We found that rat NMU-23 and its structurally-related peptide rat neuromedin S (NMS) significantly reduced food intake in lean mice, whereas NMU-8, an active fragment of the octapeptide sequence conserved in porcine, human and mouse NMU, had no effect...
April 8, 2017: Peptides
https://www.readbyqxmd.com/read/28378780/a-fluorometric-method-of-measuring-carboxypeptidase-activities-for-angiotensin-ii-and-apelin-13
#20
Pan Liu, Jan Wysocki, Peter Serfozo, Minghao Ye, Tomokazu Souma, Daniel Batlle, Jing Jin
Degradation of the biologically potent octapeptide angiotensin Ang II-(1-8) is mediated by the activities of several peptidases. The conversion of Ang II to the septapeptide Ang-(1-7) is of particular interest as the latter also confers organ protection. The conversion is catalyzed by angiotensin-converting enzyme 2 and other enzymes that selectively cleave the peptide bond between the proline and the phenylalanine at the carboxyl terminus of Ang II. The contribution of various enzyme activities that collectively lead to the formation of Ang-(1-7) from Ang II, in both normal conditions and in disease states, remains only partially understood...
April 5, 2017: Scientific Reports
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