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Search results for: PEPTIDE%20CONJUGATES
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Synthesis of conjugates of Combretastatin A-4 with tuftsin derivatives as potential anticancer agents
PublicationZaprezentowano syntezę nowych koniugatów Combretastatyny A-4 z pochodnymi tuftsyny i retro-tuftsyny, jako potencjalnych związków przeciwnowotworowych.
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Synthesisand cytotoxic activity of conjugates of muramyl and normuramyl dipeptides with batracylin derivatives
PublicationOpisano syntezę analogów MDP oraz nor-MDP modyfikowanych w części peptydowej batracyliną i pochodnymi batracyliny. Opracowano udoskonaloną metodę syntezy batracyliny. Zaproponowana metoda pozwala na otrzymanie BAT w skali multi-gramowej. Zsyntetyzowane analogi nie wykazały aktywności cytotoksycznej w badaniach prowadzonych w NCI (Bethesda, USA). W testach in vitro przeprowadzonych w Akademii Medycznej w Gdańsku dwa analogi redukowały...
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Synthesis and antitumor activity of conjugates of muramyldipeptide or normuramyldipeptide with hydroxyacridine/acridone derivatives
PublicationOpisano syntezę analogów MDP oraz nor-MDP modyfikowanych w części peptydowej pochodnymi hydroksyakrydyny/akrydonu i dwóch analogów modyfikowanych pochodnymi 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny. Tylko związki zawierające pochodne 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny wykazały wysoką aktywność cytotoksyczną badaną na 60 liniach ludzkich komórek nowotworowych, na nowotwór prostaty i AIDS-related lymphoma (ARL). Związek...
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Biodegradable macromolecular conjugates of citropin: Synthesis, characterization and in vitro efficiency study
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Synthesis of conjugates of amino-combretastatin with tuftsin derivatives as potential anticancer agents
PublicationOpisano syntezę nowych koniugatów 3'-N-(tuftsyno lub retro-tuftsyno)-amino-kombretastatyny jako potencjalnych związków przeciw-nowotworowych. Do syntezy amino-kombretastatyny (amino-CA-4) wykorzystano reakację Wittiga a koniugatów metodę DPPA. Mamy nadzieję, że połączenie pochodnych tuftsyny z amino-CA-4 wpłynie na polepszenie właściwości terapeutycznych CA-4.
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Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives
PublicationNew conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2′,3′-O-isopropylidene protected and free hydroxyl...
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Antimicrobial peptides (AMPs) as drug candidates: a patent review (2003–2015)
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Counter-ion effect on antistaphylococcal activity and cytotoxicity of selected antimicrobial peptides
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Porcine myofibrillar proteins as potential precursors of bioactive peptides – an in silico study
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Determination of long-chain aldehydes using a novel quartz crystal microbalance sensor based on a biomimetic peptide
PublicationThere is an increasingly popular trend aimed at improvement of fundamental metrological parameters of sensors via implementation of materials mimicking biological olfactory systems. This study presents investigation on usefulness of the peptide mimicking HarmOBP7 region as a receptor element of the piezoelectric sensor for selective analysis of long-chain aldehydes. Identification of odorant binding proteins creates new possibilities...
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Generation and Characterization of a DNA-GCN4 Oligonucleotide-Peptide Conjugate: The Impact DNA/Protein Interactions on the Sensitization of DNA
PublicationRadiotherapy, the most common therapy for the treatment of solid tumors, exerts its effects by inducing DNA damage. To fully understand the extent and nature of this damage, DNA models that mimic the in vivo situation should be utilized. In a cellular context, genomic DNA constantly interacts with proteins and these interactions could influence both the primary radical processes (triggered by ionizing radiation) and secondary reactions,...
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Least Squares Estimators of Peptide Species Concentrations Based on Gaussian Mixture Decompositions of Protein Mass Spectra
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Molecular dynamics study of a gelsolin-derived peptide binding to a lipid bilayer containing phosphatidylinositol 4,5-bisphosphate
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UNRES-Dock—protein–protein and peptide–protein docking by coarse-grained replica-exchange MD simulations
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99mTc-Galacto-RGD2: A Novel 99mTc-Labeled Cyclic RGD Peptide Dimer Useful for Tumor Imaging
PublicationThis study sought to evaluate [99mTc(HYNIC-Galacto-RGD2)-(tricine)(TPPTS)] (99mTc-Galacto-RGD2: HYNIC = 6-hydrazinonicotinyl; Galacto-RGD2 = Glu[cyclo[Arg-Gly-Asp-D-Phe-Lys(SAA-PEG2-(1,2,3-triazole)-1-yl-4-ethylamide)]]2 (SAA = 7-amino-L-glycero-L-galacto-2,6-anhydro-7-eoxyheptanamide, and PEG2 = 3,6-dioxaoctanoic acid); and TPPTS = trisodium triphenylphosphine-3,3',3''-trisulfonate) as a new radiotracer for tumor imaging. Galacto-RGD2...
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Renal Regulation of Potassium Homeostasis in Calves in the First Week of Life Including the Role of Atrial Natriuretic Peptide
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Investigation of Serine‐Proteinase‐Catalyzed Peptide Splicing in Analogues of Sunflower Trypsin Inhibitor 1 (SFTI‐1)
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Synthesis, Chemical Characterization and Multiscale Biological Evaluation of a dimericcRGD Peptide for Targeted Imaging of αVβ3 Integrin Activity
PublicationCyclic peptides containing the Arg-Gly-Asp (RGD) sequence have been shown to specifically bind the angiogenesis biomarker α V β3 integrin. We report the synthesis, chemical characterization, and biological evaluation of two novel dimeric cyclic RGD-based molecular probes for the targeted imaging of α V β3 activity (a radiolabeled version, 64Cu-NOTA-PEG4-cRGD2, for PET imaging, and a fluorescent version, FITC-PEG4-cRGD2, for in...
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Prediction of Bioactive Peptides From Chicken Feather and Pig Hair Keratins Using In Silico Analysis Based on Fragmentomic Approach
PublicationBackground: Keratin is among the most abundant structural proteins of animal origin, however it remains broadly underutilized. Objective: Bioinformatic investigation was performed to evaluate selected keratins originating from mass-produced waste products, i.e., chicken feathers and pig hair, as potential sources of bioactive peptides. Methods: Pepsin, trypsin, chymotrypsin, papain, and subtilisin were used for in silico keratinolysis...
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Synthetic strategies in construction of organic low molecular-weight carrier-drug conjugates
PublicationInefficient transportation of polar metabolic inhibitors through cell membranes of eukaryotic and prokaryotic cells precludes their direct use as drug candidates in chemotherapy. One of the possible solutions to this problem is application of the ‘Trojan horse’ strategy, i.e. conjugation of an active substance with a molecular carrier of organic or inorganic nature, facilitating membrane penetration. In this work, the synthetic...
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Synthesis of conjugates of MDP and nor-MDP linked to tuftsin derivatives as potential immunomodulators
PublicationZsyntetyzowano nowe koniugaty muramylodipeptydu (MDP) i nor-muramylo-dipeptydu (nor-MDP) z pochodnymi tuftsyny zawierającymi wiązanie izopeptydowe na epsilon-aminowej grupie lizyny jako potencjalne immunomodulatory. Do syntezy wykorzystano metodę mieszanych bezwodników z chloromrówczanem izobutylu i N-metylomorfoliną w bezwodnym DMF. Końcowe produkty charakteryzowno za pomocą NMR, analizy elementarnej i analizy aminokwasowej na...
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Solid phase synthesis of conjugates of tuftsin analogues with 1-nitro-acridine derivatives
PublicationZsyntetyzowano na fazie stałej koniugaty 1-nitro-akrydyny z pochodnymi tuftsyny modyfikowanymi na grupie epsilon-aminowej lizyny prostymi aminokwasami, np. alaniną, valiną, beta-alaniną. Końcowe produkty były charakteryzowane za pomocą MS, NMR, analizy elementarnej i przekazane do badań ich aktywności przeciwnowotworowej.
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Release systems based on self-assembling RADA16-I hydrogels with a signal sequence which improves wound healing processes
PublicationSelf-assembling peptides can be used for the regeneration of severely damaged skin. They can act as scaffolds for skin cells and as a reservoir of active compounds, to accelerate scarless wound healing. To overcome repeated administration of peptides which accelerate healing, we report development of three new peptide biomaterials based on the RADA16-I hydrogel functionalized with a sequence (AAPV) cleaved by human neutrophil elastase...
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Structural changes of a simple peptide—Trpzip-1—in aqueous solutions and the corresponding hydration phenomena under the influence of temperature
PublicationTrpzip-1, a simple β-hairpin, is a rare example of peptide with stable secondary structure and can be a convenient model to study temperature-related processes that potential prion or amyloid proteins undergo. Although its sequence is simple, the exact processes which the peptide undergoes in aqueous solutions are quite complex and not well understood. The selection of well-established experimental (DSC, FTIR) and theoretical methods...
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Understanding the interactions between protein stabilizers and the peptide bond through the analysis of the volumetric and compressibility properties for the model systems
PublicationThis work confirms our earlier supposition, that volumetric and acoustic parameters for simple model proposed by us are directly related to stabilizing/destabilizing effect of osmolytes on proteins structure. The apparent molar volumes, V and the apparent molar isentropic compressions, KS,, of glycine and N,N,N –trimethylglycine (betaine) were determined from densities and speed of sound measurements in aqueous solution of N-methylacetamide...
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Cis/trans conformational equilibrium across the N-methylphenylalanine2- N-methylphenylalanine3 peptide bond of arginine vasopressin analogs
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Molecular dynamics study of amyloid formation of two Abl-SH3 domain peptides
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Antinociceptive and Cytotoxic Activity of Opioid Peptides with Hydrazone and Hydrazide Moieties at the C-Terminus
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Nanoparticles associated with antimicrobial peptides (AMPs) promising combination for biomedical and veterinary applications
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A Novel Delivery System for the Controlled Release~of Antimicrobial Peptides: Citropin 1.1 and Temporin A
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Synthesis of new conjugates of MDP and nor-MDP with retro-tuftsin derivatives as potential immunomodulators
PublicationZsyntetyzowano nowe analogi muramylodipeptydu (MDP) i nor-muramylo-dipeptydu (nor-MDP) z pochodnymi retro-tuftsyny jako potencjalne immunomodulatory. Przedstawiono także syntezę odpowiednich pochodnych retro-tuftsyny. Do syntezy wykorzystano metodę mieszanych bezwodników z chloromrówczanem izobutylu i N-metylomorfoliną w bezwodnym DMF.
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Synthesis of functionalized new conjugates of batracylin with tuftsin/ retro-tuftsin derivatives and their biological evaluation
PublicationNew batracylin conjugates with tuftsin/retro-tuftsin derivatives were designed and synthesized using T3P as a coupling agent. The conjugates possess an amide bond formed between the carboxyl group of heterocyclic molecule and the N-termini of the tuftsin/retro-tuftsin chain. The in vitro cytotoxic activity of the new analogues and their precursors was evaluated using a series of human and murine tumor cells. BAT conjugates containing...
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Influence of Dimerization of Lipopeptide Laur-Orn-Orn-Cys–NH2 and an N-terminal Peptide of Human Lactoferricin on Biological Activity
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Binding modes of a new epoxysuccinyl–peptide inhibitor of cysteine proteases. Where and how do cysteine proteases express their selectivity?
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Lipidated Analogs of the LL-37-Derived Peptide Fragment KR12—Structural Analysis, Surface-Active Properties and Antimicrobial Activity
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Inhibitory activity of double‐sequence analogues of trypsin inhibitor SFTI‐1 from sunflower seeds: an example of peptide splicing
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Peptide bond modification. I. Simple and efficient method of Boc-Gly[CH(OH)CH2]Gly-OH synthesis.
PublicationZaprezentowano prostą i efektywną metodę syntezy obu enancjomerów t-butoksykarbonylo chronionego pseudo dipeptydu (R) oraz (S)-Boc-Gly[CH(OH)CH2]Gly-OH.
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Relative quantification of pork and beef in meat products using global and species-specific peptide markers for the authentication of meat composition
PublicationWe used global and species-specific peptide markers for a relative quantitative determination of pork and beef in raw and processed meat products made of the two meat species. Four groups of products were prepared (i.e., minced raw meats, sausages, raw and fried burgers) in order to represent products with different extents of food processing. In each group, the products varied in the pork/beef proportions. All products were analysed...
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Development of a Peptide Derived from Platelet-Derived Growth Factor (PDGF-BB) into a Potential Drug Candidate for the Treatment of Wounds
PublicationObjective: This study evaluated the use of novel peptides derived from platelet-derived growth factor (PDGF-BB) as potential wound healing stimulants. One of the compounds (named PDGF2) was subjected for further research after cytotoxicity and proliferation assays on human skin cells. Further investigation included evaluation of: migration and chemotaxis of skin cells, immunological and allergic safety, the transcriptional analyses...
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Efficient parallel algorithms in global optimization of potential energy functions for peptides, proteins, and crystals
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An animal model of the procognitive properties of cysteine protease inhibitor and immunomodulatory peptides based on colostrum.
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Antimicrobial Activity of Selected Antimicrobial Peptides Against Planktonic Culture and Biofilm of Acinetobacter baumannii
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Sample Concentration of Charged Small Molecules and Peptides in Capillary Electrophoresis by Micelle to Cyclodextrin Stacking
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Bioactive peptides from beef products fermented by acid whey – in vitro and in silico study
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Effect of probiotic bacteria on antiradical activity of peptides isolated from dry-cured loins
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Current state of a dual behaviour of antimicrobial peptides-Therapeutic agents and promising delivery vectors
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Molecular basis and quantitative assessment of TRF1 and TRF2 protein interactions with TIN2 and Apollo peptides
PublicationShelterin is a six-protein complex (TRF1, TRF2, POT1, RAP1, TIN2, and TPP1) that also functions in smaller subsets in regulation and protection of human telomeres. Two closely related proteins, TRF1 and TRF2, make high-affinity contact directly with double-stranded telomeric DNA and serve as a molecular platform. Protein TIN2 binds to TRF1 and TRF2 dimer-forming domains, whereas Apollo makes interaction only with TRF2. To elucidate...
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Synthesis and biological activity of novel mycophenolic acid conjugates containing nitro-acridine/acridone derivatives
PublicationOpracowano warunki reakcji kwasu mykofenolowego z aminowymi pochodnymi akrydyn i akrydonów. Tak otrzymane koniugaty zostały scharakteryzowane, a następnie przebadane in vitro pod względem aktywności przeciwbiałaczkowej oraz immunosupresyjnej.
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Cyclic Peptidic Furin Inhibitors Developed by Combinatorial Chemistry
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Design, synthesis and in vitro biological evaluation of a small cyclic peptide as inhibitor of vascular endothelial growth factor binding to neuropilin-1
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