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Daniela S Ferreira et al.
Advanced healthcare materials, 4(4), 602-612 (2014-11-22)
The use of peptide engineering to develop self-assembling membranes that are responsive to cellular enzyme activities is reported. The membranes are obtained by combining hyaluronan (HA) and a rationally designed peptide amphiphile (PA) containing a proteolytic domain (GPQGIWGQ octapeptide) sensitive
Christoph Hirschhäuser et al.
Organic letters, 14(18), 4846-4849 (2012-09-06)
Expedient routes to three classes of novel spiro-fused pyrrolidine, piperidine, and indoline heterocycle scaffolds are described. These three-dimensional frameworks, which conform to the "rule of three", are suitably protected to allow for site-selective manipulation and functionalization. Different modes of substrate
Charity Wayua et al.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 56(1), 113-119 (2014-12-17)
Tumor-specific targeting ligands were recently exploited to deliver both imaging and therapeutic agents selectively to cancer tissues in vivo. Because the cholecystokinin 2 receptor (CCK2R) is overexpressed in various human cancers (e.g., lung, medullary thyroid, pancreatic, colon, and gastrointestinal stromal
Hongying Su et al.
Dalton transactions (Cambridge, England : 2003), 41(48), 14480-14483 (2012-10-31)
The aza-semi-crown pentadentate ligand rigidified by pyridine and piperidine rings was designed and synthesized. It can react with Mn(II) in water to form complex with improved longitudinal relaxivity, leading to efficient signal intensity enhancement of vascular vessels under a clinical
Nitin J Pawar et al.
The Journal of organic chemistry, 77(18), 7873-7882 (2012-08-10)
The Jocic-Reeve and Corey-Link type reaction of dichloromethyllithium with suitably protected 5-keto-hexofuranoses followed by treatment with sodium azide and sodium borohydride reduction gave 5-azido-5-hydroxylmethyl substituted hexofuranoses 7a-c with required geminal dihydroxymethyl group. Removal of protecting groups and converting the C-1
Lars Erik Uggerhøj et al.
FEBS letters, 588(17), 3291-3297 (2014-07-27)
The inclusion of peptoid monomers into antimicrobial peptides (AMPs) increases their proteolytic resistance, but introduces conformational flexibility (reduced hydrogen bonding ability and cis/trans isomerism). We here use NMR spectroscopy to answer how the insertion of a peptoid monomer influences the
Elisabeth T Hennessy et al.
Science (New York, N.Y.), 340(6132), 591-595 (2013-05-04)
The manipulation of traditionally unreactive functional groups is of paramount importance in modern chemical synthesis. We have developed an iron-dipyrrinato catalyst that leverages the reactivity of iron-borne metal-ligand multiple bonds to promote the direct amination of aliphatic C-H bonds. Exposure
Rubiralta M, et al.
Piperidine: Structure, Preparation, Reactivity, and Synthetic Applications of Piperidine and its Derivatives, 43 (2013)
Susanne Kirchhof et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 96, 217-225 (2015-08-09)
Eight-armed PEG was functionalized with furyl and maleimide groups (8armPEG20k-Fur and 8armPEG20k-Mal); degradable hydrogels were obtained by cross-linking via Diels-Alder chemistry. To increase the stability to degradation, the macromonomers were modified by introducing a hydrophobic 6-aminohexanoic acid spacer between PEG
David Giganti et al.
Nature communications, 5, 4833-4833 (2014-09-11)
The Plasmodium subtilase SUB1 plays a pivotal role during the egress of malaria parasites from host hepatocytes and erythrocytes. Here we report the crystal structure of full-length SUB1 from the human-infecting parasite Plasmodium vivax, revealing a bacterial-like catalytic domain in
Magdalena Pezzoni et al.
Bio-protocol, 8(11), e2869-e2869 (2018-06-05)
Bacteria in nature and as pathogens commonly face oxidative stress which causes damage to proteins, lipids and DNA. This damage is produced by the action of reactive oxygen species (ROS) such as hydrogen peroxide (H2O2), singlet oxygen, superoxide anion and
Urban Švajger et al.
Cancer immunology, immunotherapy : CII, 64(1), 15-27 (2014-09-26)
The tumor microenvironment represents a burden that hampers the proper activation of immune cells, including the dendritic cells (DCs). It is, therefore, desired that the important characteristics of a given anticancer drug candidate be seen as consisting not solely of
Sander R Piersma et al.
Journal of proteomics, 127(Pt B), 247-258 (2015-04-07)
Robust phosphopeptide enrichment methods with minimal fractionation are required to profile signaling network analysis in cancer cell lines and tissues. We assessed performance of single-shot LC-MS/MS label-free phosphoproteomics using TiOx-based phosphopeptide enrichment and report phosphopeptide identification reproducibility (75.8%), depth of
Chiara Testa et al.
Journal of medicinal chemistry, 57(22), 9424-9434 (2014-10-28)
Side chain-to-side chain cyclizations represent a strategy to select a family of bioactive conformations by reducing the entropy and enhancing the stabilization of functional ligand-induced receptor conformations. This structural manipulation contributes to increased target specificity, enhanced biological potency, improved pharmacokinetic
Ewa Radzikowska et al.
Organic & biomolecular chemistry, 13(1), 269-276 (2014-11-05)
Chimeric oligonucleotides containing phosphodiester and phosphorothioate linkages have been obtained using the solid phase synthesis. The oligonucleotide parts possessing natural internucleotide phosphate bonds were assembled using commercially available nucleoside 3'-O-(2-cyanoethyl-N,N-diisopropylamino)phosphoramidites 7 whereas the phosphorothioate segment was built using nucleoside 3'-O-(2-thio-1,3,2-oxathiaphospholanes)
Roberto Alcántara et al.
STAR protocols, 2(4), 100878-100878 (2021-10-05)
Here, we describe a detailed step-by-step protocol to detect SARS-CoV-2 RNA using RT-PCR-mediated amplification and CRISPR/Cas-based visualization. The optimized assay uses basic molecular biology equipment such as conventional thermocyclers and transilluminators for qualitative detection. Alternatively, a fluorescence plate reader can
Do-Wan Shim et al.
PloS one, 10(5), e0126871-e0126871 (2015-05-29)
Antimicrobial peptides (AMPs), also called host defense peptides, particularly those with amphipathic helical structures, are emerging as target molecules for therapeutic development due to their immunomodulatory properties. Although the antimicrobial activity of AMPs is known to be exerted primarily by
Stancho Stanchev et al.
Journal of peptide science : an official publication of the European Peptide Society, 20(9), 725-735 (2014-06-13)
The antimicrobial 40-amino-acid-peptide lucifensin was synthesized by native chemical ligation (NCL) using N-acylbenzimidazolinone (Nbz) as a linker group. NCL is a method in which a peptide bond between two discreet peptide chains is created. This method has been applied to
Marta Soler et al.
Inorganic chemistry, 54(22), 10542-10558 (2015-10-28)
The conjugation of redox-active complexes that can function as chemical nucleases to cationic tetrapeptides is pursued in this work in order to explore the expected synergistic effect between these two elements in DNA oxidative cleavage. Coordination complexes of biologically relevant
Xuwang Chen et al.
Bioorganic & medicinal chemistry, 20(12), 3856-3864 (2012-05-18)
A novel series of piperidine-linked amino-triazine derivatives were designed, synthesized and evaluated for in vitro anti-HIV activity as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. Screening results indicated that most compounds showed excellent activity against wild-type
P Ricardo Girling et al.
Organic & biomolecular chemistry, 9(9), 3105-3121 (2011-03-11)
A review into the aza-Diels-Alder reaction, mainly concentrating on literature examples that form piperidin-4-ones from the reaction of imines and electron rich dienes or enones, either through a Lewis acidic/Brønsted acid approach or through the use of an organocatalyst. This
M K Prashanth et al.
Bioorganic & medicinal chemistry letters, 22(23), 7065-7070 (2012-10-20)
A series of piperamide derivatives (8a-j) was synthesized with various substituted piperidine and piperazine compounds. The prepared compounds were evaluated for antibacterial activity against gram-positive and gram-negative bacteria and antifungal activity by disc diffusion method. The antioxidant activity of the
Cátia Fernandes-Cerqueira et al.
Arthritis research & therapy, 17, 155-155 (2015-06-11)
We have previously identified endogenously citrullinated peptides derived from fibrinogen in rheumatoid arthritis (RA) synovial tissues. In this study, we have investigated the auto-antigenicity of four of those citrullinated peptides, and explored their feasibility to target anti-citrullinated protein/peptide antibodies (ACPA).
Kentaro Futatsugi et al.
Bioorganic & medicinal chemistry letters, 23(1), 194-197 (2012-11-28)
A novel GPR119 agonist based on the 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole scaffold was designed through lead optimization starting from pyrazole-based GPR119 agonist 1. The design is centered on the conformational restriction of the core scaffold, while minimizing the change in spatial relationships of
Liz O'Donovan et al.
Nucleic acid therapeutics, 25(1), 1-10 (2014-11-21)
We describe two new methods of parallel chemical synthesis of libraries of peptide conjugates of phosphorodiamidate morpholino oligonucleotide (PMO) cargoes on a scale suitable for cell screening prior to in vivo analysis for therapeutic development. The methods represent an extension
Jae H Park et al.
Journal of medicinal chemistry, 57(15), 6623-6631 (2014-07-16)
The aqueous solution structure of protoxin II (ProTx II) indicated that the toxin comprises a well-defined inhibitor cystine knot (ICK) backbone region and a flexible C-terminal tail region, similar to previously described NaSpTx III tarantula toxins. In the present study
Shezeng Li et al.
Pest management science, 68(12), 1546-1552 (2012-06-12)
Pythium ultimum is a plant pathogen that causes significant yield losses on many economically important crops. Chemical treatment has been used for disease control. In searching for alternatives, venom piperidine and piperideine alkaloids from red imported fire ants were tested
Lisa Pollaro et al.
Molecular cancer therapeutics, 14(1), 151-161 (2014-11-09)
Monoclonal antibodies have long in vivo half-lives and reach high concentrations in tumors but cannot access all regions in the tissue, whereas smaller ligands such as peptides distribute better but are limited by low concentrations due to fast renal clearance.
Yang Li et al.
Macromolecular bioscience, 15(1), 52-62 (2014-12-06)
To address the downside of conventional photo-patterning which can alter the chemical composition of protein scaffolds, we developed a non-covalent photo-patterning strategy for gelatin (denatured collagen) hydrogels that utilizes UV activated triple helical hybridization of caged collagen mimetic peptide (caged
A Eckhard et al.
Pflugers Archiv : European journal of physiology, 467(12), 2571-2588 (2015-07-26)
Volume homeostasis of the cochlear endolymph depends on radial and longitudinal endolymph movements (LEMs). LEMs measured in vivo have been exclusively recognized under physiologically challenging conditions, such as experimentally induced alterations of perilymph osmolarity or endolymph volume. The regulatory mechanisms
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