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Peptide synthesis

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https://www.readbyqxmd.com/read/28342399/design-synthesis-and-biological-evaluation-of-pegylated-xenopus-glucagon-like-peptide-1-derivatives-as-long-acting-hypoglycemic-agents
#1
Jing Han, Yiyun Wang, Qinghua Meng, Guangchao Li, Fangmin Huang, Su Wu, Yingying Fei, Feng Zhou, Junjie Fu
In order to develop novel long-acting GLP-1 derivatives, a peptide hybrid (1a) from human GLP-1 and Xenopus GLP-1 discovered in our previous research was selected as the lead compound. Exendin-4 inspired modification resulted in peptide 1b with enhanced glucose-lowering activity. Cysteine mutated 1b derivatives with reserved bioactivity were further site-specifically connected with mPEG2000-MAL to provide conjugates 3a-h, among which 3d and 3e were found to have significantly improved hypoglycemic activity and insulinotropic ability than GLP-1...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28338682/simple-peptides-derived-from-the-ribosomal-core-potentiate-rna-polymerase-ribozyme-function
#2
Shunsuke Tagami, James Attwater, Philipp Holliger
The emergence of functional interactions between nucleic acids and polypeptides was a key transition in the origin of life and remains at the heart of all biology. However, how and why simple non-coded peptides could have become critical for RNA function is unclear. Here, we show that putative ancient peptide segments from the cores of both ribosomal subunits enhance RNA polymerase ribozyme (RPR) function, as do derived homopolymeric peptides comprising lysine or the non-proteinogenic lysine analogues ornithine or, to a lesser extent, diaminobutyric acid, irrespective of chirality or chiral purity...
April 2017: Nature Chemistry
https://www.readbyqxmd.com/read/28337175/effects-of-chronic-acth-excess-on-human-adrenal-cortex
#3
REVIEW
Xavier Bertagna
Chronic ACTH excess leads to chronic cortisol excess, without escape phenomenon, resulting in Cushing's syndrome. Excess adrenal androgens also occur: in females, they will overcompensate the gonadotrophic loss, inducing high testosterone; in males, they will not compensate it, inducing low testosterone. Chronic ACTH excess leads to chronic adrenal mineralocorticoid excess and low aldosterone levels: after an acute rise, aldosterone plasma levels resume low values after a few days when ACTH is prolonged. Two other mineralocorticoids in man, cortisol and 11 deoxycorticosterone (DOC), at the zona fasciculata, will not escape the long-term effect of chronic ACTH excess and their secretion rates will remain elevated in parallel...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28336138/preparation-of-an-epitope-imprinted-polymer-with-antibody-like-selectivity-for-beta2-microglobulin-and-application-in-serum-sample-analysis-with-a-facile-method-of-on-line-solid-phase-extraction-coupling-with-high-performance-liquid-chromatography
#4
Fangfang Yang, Dandan Deng, Xiangchao Dong, Shen Lin
Molecularly imprinted polymers (MIPs) for protein recognition have great application potential in the biological analysis. However, preparation of protein imprinted polymer is still facing challenge. Beta2-microglobulin (β2m) is a protein biomarker that can be used in diagnosis of different diseases. In this research, a novel MIP with ability of β2m recognition has been developed by epitope and surface-confined imprinting approaches. A peptide with sequence of MIQRTPKIQ was selected as template. A strategy of combination of hierarchical imprinting and template immobilization was employed in the β2m-MIP synthesis...
March 9, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28334756/measurements-of-translation-initiation-from-all-64-codons-in-e-coli
#5
Ariel Hecht, Jeff Glasgow, Paul R Jaschke, Lukmaan A Bawazer, Matthew S Munson, Jennifer R Cochran, Drew Endy, Marc Salit
Our understanding of translation underpins our capacity to engineer living systems. The canonical start codon (AUG) and a few near-cognates (GUG, UUG) are considered as the 'start codons' for translation initiation in Escherichia coli. Translation is typically not thought to initiate from the 61 remaining codons. Here, we quantified translation initiation of green fluorescent protein and nanoluciferase in E. coli from all 64 triplet codons and across a range of DNA copy number. We detected initiation of protein synthesis above measurement background for 47 codons...
February 21, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28333255/alkaline-protease-contributes-to-pyocyanin-production-in-pseudomonas-aeruginosa
#6
Kazuhiro Iiyama, Eigo Takahashi, Jae Man Lee, Hiroaki Mon, Mai Morishita, Takahiro Kusakabe, Chisa Yasunaga-Aoki
The role of the alkaline protease (AprA) in pyocyanin production in Pseudomonas aeruginosa was investigated. AprA was overproduced when a plasmid carrying the aprA gene was introduced to an aprA-deletion mutant strain, EG03; thus, aprA-complemented EG03 was used as an overproducing strain. The complemented strain produced higher pyocyanin than the mutant strain in all commercially available media evaluated. Particularly, pyocyanin production was higher in the complemented than in the parental strain in brain-heart infusion and tryptic soy broths...
March 15, 2017: FEMS Microbiology Letters
https://www.readbyqxmd.com/read/28333237/new-paenibacillus-strain-produces-a-family-of-linear-and-cyclic-antimicrobial-lipopeptides-cyclization-is-not-essential-for-their-antimicrobial-activity
#7
En Huang, Xu Yang, Liwen Zhang, Sun Hee Moon, Ahmed E Yousef
A new bacterial isolate, Paenibacillus sp. OSY-N, showed potent antimicrobial activity against Gram-negative and Gram-positive bacteria. Antimicrobials produced by this strain were purified by reverse-phase high performance liquid chromatography (HPLC). Structural analysis, using mass spectrometry (MS), of a single active HPLC fraction revealed two known cyclic lipopeptides, BMY-28160 and permetin A, a new cyclic lipopeptide, and the linear counterparts of these cyclic compounds. The latter were designated as paenipeptin A, B and C, respectively...
February 25, 2017: FEMS Microbiology Letters
https://www.readbyqxmd.com/read/28332450/nuclear-medicine-in-patients-with-net-radiolabeled-somatostatin-analogues-and-their-brothers
#8
Vincenzo Cuccurullo, Maria Rosaria Prisco, Giuseppe Danilo Di Stasio, Luigi Mansi
Although Somastostatin (SS) scintigraphy (SRS) has been introduced many years ago, it remains the most diffuse radionuclide diagnostic tool in patients with neuroendocrine tumours (NETs). Being SS receptors (SSTR) expressed in the majority of NETs, radiolabeled SS analogues (SS-A) provide high diagnostic accuracy, mainly in patients with gastro-entero-pancreatic (GEP) tumors. SSTR are the best target for radiotracers used either for diagnostic and therapeutic purposes in NETs due to their presence on the surface of neoplastic cells of clinical interest...
March 23, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28331187/cross-beta-nanostructures-based-on-dinaphthylalanine-gd-conjugates-loaded-with-doxorubicin
#9
Carlo Diaferia, Eliana Gianolio, Teresa Sibillano, Flavia Anna Mercurio, Marilisa Leone, Cinzia Giannini, Nicole Balasco, Luigi Vitagliano, Giancarlo Morelli, Antonella Accardo
Very recently we proposed novel di- and tetra-phenylalanine peptides derivatized with gadolinium complexes as potentials supramolecular diagnostic agents for applications in MRI (Magnetic Resonance Imaging). It was observed that in very short FF dipeptide building blocks, the propensity to aggregate decreases significantly after modification with bulky moiety such as Gd-complexes, thus limiting their potential as CAs. We hypothesized that the replacement of the Phe side chain with more extended aromatic groups could improve the self-assembling...
March 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28330252/organic-solvent-tolerant-metallo-protease-of-novel-isolate-serratia-marcescens-ppb-26-production-and-characterization
#10
Shikha Thakur, Nirmal Kant Sharma, Neerja Thakur, Savitri, Tek Chand Bhalla
Proteases are a class of enzymes that catalyze hydrolysis of peptide bonds of proteins. In this study, 221 proteolytic bacterial isolates were obtained by enrichment culture method from soils of various regions of Himachal Pradesh, India. From these a hyper producer of protease was screened and identified by morphological and physiological testing and by 16S rDNA sequence as Serratia marcescens PPB-26. Statistical optimization of physiochemical parameters enhanced the protease production by 75 %. Protease of S...
December 2016: 3 Biotech
https://www.readbyqxmd.com/read/28329269/proteomics-highlights-decrease-of-matricellular-proteins-in-left-ventricular-assist-device-therapy%C3%A2
#11
Jasmin Hasmik Shahinian, Bettina Mayer, Stefan Tholen, Kerstin Brehm, Martin L Biniossek, Hannah Füllgraf, Selina Kiefer, Ulrike Heizmann, Claudia Heilmann, Florian Rüter, Martin Grapow, Oliver Thomas Reuthebuch, Friedrich Eckstein, Friedhelm Beyersdorf, Oliver Schilling, Matthias Siepe
OBJECTIVES: We investigated the impact of mechanical unloading with a left ventricular assist device (LVAD) on the myocardial proteome. METHODS: We collected 11 patient-matched samples of myocardial left ventricular tissue of patients with non-ischaemic dilate cardiomyopathy, harvested at time of LVAD implant ('pre-LVAD') and heart transplant ('post-LVAD'). Samples were studied by quantitative proteomics. Further we performed histological assessment of deposited collagens and immune infiltration in both pre- and post-LVAD samples...
February 20, 2017: European Journal of Cardio-thoracic Surgery
https://www.readbyqxmd.com/read/28328161/synthesis-in-vitro-evaluation-and-68-ga-radiolabeling-of-cdp1-towards-pet-ct-imaging-of-bacterial-infection
#12
Jyotibon Dutta, Sooraj Baijnath, Anou M Somboro, Savania Nagiah, Fernando Albericio, Beatriz G de la Torre, Biljana Marjanovic-Painter, Jan Rijn Zeevaart, Mike Sathekge, Hendrik G Kruger, Anil Chuturgoon, Tricia Naicker, Thomas Ebenhan, Thavendran Govender
Bacterial infections are a major concern in the human health sector due to poor diagnosis and development of multi drug resistant strains. PET/CT provides a means for the noninvasive detection and localization of the infectious foci; however, the radiotracers available are either cumbersome to prepare or their exact contribution towards the imaging is not yet established. Human antimicrobial peptides are of interest for development as PET radiotracers as they are an integral component of the immune system, non-immunogenic towards the recipient and show selectivity towards pathogens such as bacteria...
March 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28327729/direct-palladium-mediated-on-resin-disulfide-formation-from-allocam-protected-peptides
#13
Thilini D Kondasinghe, Hasina Y Saraha, Samantha B Odeesho, Jennifer L Stockdill
The synthesis of disulfide-containing polypeptides represents a long-standing challenge in peptide chemistry, and broadly applicable methods for the construction of disulfides are in constant demand. Few strategies exist for on-resin formation of disulfides directly from their protected counterparts. We present herein a novel strategy for the on-resin construction of disulfides directly from Allocam-protected cysteines. Our palladium-mediated approach is mild and uses readily available reagents, requiring no special equipment...
March 22, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28326729/-study-of-human-leucine-rich-amelogenin-peptide-and-its-regulation-of-mineralization-by-cryogenic-transmission-electron-microscopy
#14
Tian Kun, Feng Xiaoyun, Du Qin, Liao Chuhang, Ren Xiaohua
OBJECTIVE: Recombinant human leucine-rich amelogenin peptide (LRAP) was studied by cryogenic transmission electron microscopy (TEM); evaluation focused on its self-assembly and crystal growth in vitro. METHODS: Human LRAP was recombined through prokaryotic expression vector pCold-SUMO and transformed into Escherichia coli BL21plys to acquire purified proteins. Cryogen TEM recorded assembly and self-assembling of LRAP from pH 3.5 to pH 8.0, and the hydroxyapatite crystal growth in the mixture of LRAP protein solution and artificial saliva was observed using TEM and selected area electron diffraction...
February 1, 2017: Hua Xi Kou Qiang Yi Xue za Zhi, Huaxi Kouqiang Yixue Zazhi, West China Journal of Stomatology
https://www.readbyqxmd.com/read/28326635/structure-enabled-discovery-of-a-stapled-peptide-inhibitor-to-target-the-oncogenic-transcriptional-repressor-tle1
#15
Sally McGrath, Marcello Tortorici, Ludovic Drouin, Savade Solanki, Lewis Vidler, Isaac Westwood, Peter Gimeson, Rob vanMontfort, Swen Hoelder
TLE1 is an oncogenic transcriptional co-repressor that exerts its repressive effects through binding of transcription factors. Inhibition of this protein-protein interaction represents a putative cancer target but no small molecule inhibitors have been published for this challenging interface. In this manuscript, we report the structure enabled design and synthesis of a constrained peptide inhibitor of TLE1. Our design featured introduction of a four carbon atom linker into the peptide epitope found in many TLE1 binding partners...
March 22, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28326133/versatile-synthesis-of-the-signaling-peptide-glorin
#16
Robert Barnett, Daniel Raszkowski, Thomas Winckler, Pierre Stallforth
We present a versatile synthesis of the eukaryotic signaling peptide glorin as well as glorinamide, a synthetic analog. The ability of these compounds to activate glorin-induced genes in the social amoeba Polysphondylium pallidum was evaluated by quantitative reverse transcription PCR, whereby both compounds showed bioactivity comparable to a glorin standard. This synthetic route will be useful in conducting detailed structure-activity relationship studies as well as in the design of chemical probes to dissect glorin-mediated signaling pathways...
2017: Beilstein Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28326005/bioactivity-of-food-peptides-biological-response-of-rats-to-bovine-milk-whey-peptides-following-acute-exercise
#17
Carolina Soares Moura, Pablo Christiano Barboza Lollo, Priscila Neder Morato, Eder Muller Risso, Jaime Amaya-Farfan
Background: Several physiologically beneficial effects of consuming a whey protein hydrolysate (WPH) have been attributed to the greater availability of bioactive peptides. Aims: The aim was to investigate the effect of four branched-chain amino acid- (BCAA-)containing dipeptides, present in WPH, on immune modulation, stimulation of HSP expression, muscle protein synthesis, glycogen content, satiety signals and the impact of these peptides on the plasma free amino acid profiles. Methods: The animals were divided in groups: control (rest, without gavage), vehicle (water), L-isoleucyl-L-leucine (lle-Leu), L-leucyl-L-isoleucine (Leu-lle), L-valyl-Lleucine (Val-Leu), L-leucyl-L-valine (Leu-Val) and WPH...
2017: Food & Nutrition Research
https://www.readbyqxmd.com/read/28323366/nonribosomal-peptide-synthesis-principles-and-prospects
#18
REVIEW
Roderich D Süssmuth, Andi Mainz
Nonribosomal peptide synthetases (NRPSs) are large multienzyme machineries that assemble numerous peptides with large structural and functional diversity. These peptides include more than 20 marketed drugs, such as antibacterials (penicillin, vancomycin), antitumor compounds (bleomycin), and immunosuppressants (cyclosporine). Over the past few decades biochemical and structural biology studies have gained mechanistic insights into the highly complex assembly line of nonribosomal peptides. This Review provides state-of-the-art knowledge on the underlying mechanisms of NRPSs and the variety of their products along with detailed analysis of the challenges for future reprogrammed biosynthesis...
March 27, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28320614/synthesis-of-a-glcnacylated-arginine-building-block-for-the-solid-phase-synthesis-of-death-domain-glycopeptide-fragments
#19
Siyao Wang, Leo Corcilius, Phillip P Sharp, Richard J Payne
Herein we describe the synthesis of glycopeptide fragments from the death domains of TRADD and FADD bearing the recently discovered Nω-GlcNAc-β-arginine post-translational modification. TRADD and FADD glycopeptides were accessed through the use of a suitably protected synthetic glycosylamino acid 'cassette' that could be directly incorporated into conventional solid phase peptide synthesis (SPPS) protocols.
March 7, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28319665/synthesis-of-four-disulfide-insulin-analogs-via-sequential-disulfide-bond-formation
#20
Fangzhou Wu, John P Mayer, Vasily G Gelfanov, Fa Liu, Richard D DiMarchi
Naturally-occurring, multiple cysteine-containing peptides are a structurally unique class of compounds with a wide range of therapeutic and diagnostic applications. The development of reliable, and precise chemical methods for their preparation is of paramount importance to facilitate exploration of their utility. We report an efficient approach based on stepwise, sequentially directed disulfide bond formation, exemplified here by the synthesis of four-disulfide bond containing insulin analogs. The cysteine protections consisted of tert-butylthiol (StBu), thiol-trimethoxyphenyl (STmp), trityl (Trt), 4-methoxytrityl (Mmt), S-acetamidomethyl (Acm) and tert-butyl (tBu)...
March 20, 2017: Journal of Organic Chemistry
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