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Search results for: DIPEPTIDYL PEPTIDASE I
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Structure–activity relationships study on biological activity of peptides as dipeptidyl peptidase IV inhibitors by chemometric modeling
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Dipeptidyl Peptidase IV Inhibitory Peptides Generated in Dry-Cured Pork Loin during Aging and Gastrointestinal Digestion
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Meat Proteins as Dipeptidyl Peptidase IV Inhibitors and Glucose Uptake Stimulating Peptides for the Management of a Type 2 Diabetes Mellitus In Silico Study
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Neutrophil proteinase 3 and dipeptidyl peptidase I (cathepsin C) as pharmacological targets in granulomatosis with polyangiitis (Wegener granulomatosis)
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Molecular docking studies towards development of novel Gly-Phe analogs for potential inhibition of Cathepsin C (dipeptidyl peptidase I).
PublicationCathepsin C is a cysteine protease required for activation of various pro-inflammatory serine proteases and, essentially, is of interest as a therapeutic target. Cathepsin C coordinate system was employed as a model to study the interaction of some already available inhibitors of Cathepsin C. Compounds containing Gly-Phe fragment with functional groups at its ends were designed by knowledge based approach. Using AutoDock and...
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Synthesis and antiproliferative activity of conjugates of adenosine with muramyl dipeptide and nor-muramyl dipeptide derivatives
PublicationWe synthesized a series of MDP(D,D) and nor-MDP(D,D) derivatives conjugated with adenosine through a spacer as potential immunosuppressants. New conjugates were evaluated on two leukemia cell lines (Jurkat and L1210) and PBMC from healthy donors.
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Synthesis of conjugates of muramyl dipeptide and nor-muramyl dipeptide derivatives with adenosine as potential immunosuppressant
PublicationZaprezentowano syntezę koniugatów adenozyny z pochodnymi muramylo- i nor-muramylodipeptydów zawierających w części peptydowej D-aminokwasy (D-Ala, D-Val, D-Ser, D-Pro, D-2-ABA). Jako substrat zastosowano rybozyd 6-chloropuryny, który łączono poprzez 1,2-diaminoetan z odpowiednimi pochodnymi MDP lub nor-MDP w obecności EDCI i HOBt. Struktury otrzymanych związków zostały potwierdzone widmami 1H i 13C NMR (500 MHz), widmami MS oraz...
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Synthesis of conjugates of muramyl dipeptide and nor-muramyl dipeptide derivatives with adenosine as potential immunosuppressants
PublicationPrzedstawiono syntezę koniugatów pochodnych muramylodipeptydu (MDP) i nor-MDP z adenozyną jako potencjalnych związków o działaniu immunosupresyjnym. Jako substrat zastosowano rybozyd 6-chloropuryny, który łączonp poprzez 1,2-diaminoetan z pochodną MDP lub nor-MDP. Do syntezy wykorzystano pochodne MDP zawierające w części peptydowej D-aminokwasy (D-Ala, D-Val, D-Ser, D-Pro, D-2-ABA). Jako odczynniki sprzęgające zastosowano EDCI...
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Synthesis and biological activity of tuftsin, its analogues and conjugates containing muramyl dipeptides of nor-muramyl dipeptides
PublicationOpisano syntezę koniugatów MDP oraz nor-MDP modyfikowanych w części peptydowej tuftsyną oraz pochodną tuftsyny zawierającą grupę nitrową. Zsyntetyzowane związki zostały przebadane in vitro na ludzkich monocytach i limfocytach w Akademii Medycznej w Gdańsku. Niektóre z nich wykazały szybsze i skuteczniejsze działanie w porównaniu z tuftsyną.
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Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase
PublicationThe antifungal activity of 5‐hydroxy‐4‐oxo‐L‐norvaline (HONV), exhibited under conditions mimicking human serum, may be improved upon incorporation of this amino acid into a dipeptide structure. Several HONV‐containing dipeptides inhibited growth of human pathogenic yeasts of the Candida genus in the RPMI‐1640 medium, with minimal inhibitory concentration values in the 32 to 64 μg mL−1 range. This activity was not affected by multidrug...
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Antimicrobial Activity of Chimera Peptides Composed of Human Neutrophil Peptide 1 (HNP-1) Truncated Analogues and Bovine Lactoferrampin
PublicationThree chimera peptides composed of bovine lactoferrampin and the analogue of truncated human neutrophil peptide 1 were synthesized by the solid-phase method. In two compounds peptide chains were connected via isopeptide bond, whereas in the third one disulfide bridge served as a linker. All three chimeras displayed significantly higher antimicrobial activity than the constituent peptides as well as their equimolar mixtures. The...
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Synthesis of conjugates of muramyl dipeptide and nor-muramyl dipeptide with retro-tuftsin (Arg-Pro-Lys-ThrOMe) as potential immunostimulants.
PublicationOpisano syntezę nowych koniugatów muramylodipeptydu i nor-muramylo-dipeptydu z estrem metylowym tuftsyny o odwróconej sekwencji (Arg-Pro-Lys-Thr-OMe)jako potencjalnych immunostymulantów. Synteza tych połączeń została przeprowadzona zgodnie z zasadami chemii peptydów.
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Peptydowe koniugaty antrachinonów i ich aktywność biologiczna = Peptidyl anthraquinone conjugates and its biological activity
PublicationW artykule opisano syntezę i aktywność biologiczną peptydowych koniugatów antrachinonów. Koniugaty takie są nie tylko potencjalnymi chemoterapeutykami, ale także odgrywają rolę barwnych ligandów w metodach oczyszczania białek, technikach histochemicznych i badaniu helikalnej struktury DNA z zastosowaniem spektroskopii UV i UV-Vis.
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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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New conjugates of muramyl dipeptide and nor-muramyl dipeptide linked to tuftsin and retro-tuftsin derivatives significantly influence their biological activity
PublicationOpisano syntezę nowych koniugatów MDP i nor-MDP z pochodnymi tuftsyny i retro-tuftsyny zawierającymi wiązanie izopeptydowe pomiędzy epsilon-aminową grupą lizyny, a karboksylową grupą Ala, Gly czy Val. Zbadano ich aktywność biologiczną, m.in. profil cytokinowy.
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Biological activity of conjugates of muramyl dipeptides with batracylin derivatives
PublicationZaprezentowano immunomodulacyjne właściwości nowych koniugatów batracyliny (BAT) z pochodnymi muramylodipeptydów wobec subpopulacji leukocytów krwi obwodowej hodowanych w obecności komórek linii nowotworowych. Leukocyty izolowane były z krwi obwodowej uzyskanej od zdrowych ochotników. Zbadane koniugaty MDP lub nor-MDP z batracyliną wykazały silniejsze własności hamujące proliferację komórek wybranych linii nowotworowych (K562,...
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Biological activity of conjugates of muramyl dipeptides with batracylin derivatives
PublicationW artykule opisano aktywność biologiczną koniugatów muramylo-dipeptydów z batracyliną lub pochodnymi batracyliny. Badania przeprowadzone w Akademii Medycznej w Gdańsku miały na celu oznaczenie immunomodulacyjnych właściwości tych koniugatów wobec subpopulacji leukocytów krwi obwodowej hodowanych w obecności komórek nowotworowych (K562, WEHI164, Ab melanoma). Leukocyty izolowane były z krwi obwodowej uzyskanej od zdrowych ochotników....
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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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Structure-based design and in vivo anti-arthritic activity evaluation of a potent dipeptidyl cyclopropyl nitrile inhibitor of cathepsin C
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Conjugates of tuftsin and muramyl dipeptide as stimulators of monocyte-derived dendritic cells
PublicationOstatnio coraz częściej bada się związki oddziałujące na komórki dendrytyczne. Muramylodipeptyd i jego analogi przyspieszają dojrzewanie i aktywację komórek dendrytycznych. Do naszych badań otrzymaliśmy komórki dendrytyczne na drodze ekspansji z monocytów krwi obwodowej. Właściwa suplementacja hodowli monocytów czynnikami wzrostowymi - GM-CSF i IL-4, pozwoliła na uzyskanie niedojrzałych komórek dendrytycznych, które stymulowano...
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Cyclic Dipeptides as Building Units of Nano- and Microdevices: Synthesis, Properties, and Structural Studies
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Solubilization of keratins and functional properties of their isolates and hydrolysates
PublicationThe keratinous wastes of the textile industry and poultry slaughterhouses may be used as sources of soluble keratins or hydrolysates. This review presents methods for processing raw keratin-based materials into bioproducts with functional and bioactive properties suitable for biomedical, cosmetic, food, and agricultural applications. Soluble keratin can be obtained by thermal treatment in some organic solvents, reduction, or oxidation...
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Study of the Interactions between Neurophysin II and Dipeptide Ligand by Means of Molecular Dynamics
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New conjugates of tuftsin and muramyl dipeptide as stimulators of human monocytes-derived dendritic cells
PublicationMuramyl dipeptide (MDP) and tuftsin are known biologically active compound displaying a significant influence on various cell populations of innate immune response. MDP, as a fragment of bacterial cell wall, stimulates not only macrophages and monocytes, but also dendritic cells. In contrast, little is known about tuftsin influence on these cells. Therefore it seemed vital to access whether tuftsin or its derivatives conjugated...
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Chemical modification of natural immunomodulators tuftsin and muramyl dipeptide significantly influence their biological activity
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Analogues of muramyl dipeptide (MDP) and tuftsin limit infection and inflammation in murine model of sepsis
PublicationBadano koniugaty MDP z tuftsyną oraz pochodną tuftsyny w leczeniu ciężkich infekcji bakteryjnych takich jak posocznica. Oceniano aktywność żerną komórek układu fagocytów jednojądrzastych, wpływ na klirens bakteryjny kluczowych organów wewnętrznych oraz ekspresję genów dla cytokin pro- i antyzapalnych charakterystycznych dla odpowiedzi immunologicznej w posocznicy i indukowanych działaniem analizowanych zwiazków. W badaniach in...
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Peptide modification with thiomalonoamide moiety
PublicationAbstract: Meldrum acid derivatives under the thermal decomposition are well known source of ketenes. Recently we investigated chemical properties of thiocarbamolyl meldrum acids. We found that 5-(α-alkylamino- α'-sulfhydryl)methylene Meldrum's acids hated in the presence of amines produce thiomalonamides. We used this reaction to the one pot synthesis of series of short peptides containing thiomalonoamide motif.
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Peptide Permeases in Candida albicans
PublicationAims: The aim of this work was to characterize oligopeptide uptake in Candida albicans mutants in which the genes encoding putative peptide permeases were selectively disrupted. Initial velocities of transport of model oligopeptides, (Ala)2, (Ala)3, (Ala)4, and sensitivity of mutants to antifungal oligopeptides containing N3-(4-methoxyfumaroyl)-L-2,3-diaminopropanoic acid (FMDP) were determined and compared to those of the wild-type...
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The role of antimicrobial peptides in selected dermatoses
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Rapid Screening of Antimicrobial Synthetic Peptides
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The Role of Counter-Ions in Peptides—An Overview
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Muramyl peptides - synthesis and biological activity
PublicationArtykuł przeglądowy opisujący syntezę i aktywność biologiczną muramylopeptydów.
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Muramyl dipeptide-based analogs as potential anticancer compounds: Strategies to improve selectivity, biocompatibility, and efficiency
PublicationAccording to the WHO, cancer is the second leading cause of death in the world. This is an important global problem and a major challenge for researchers who have been trying to find an effective anticancer therapy. A large number of newly discovered compounds do not exert selective cytotoxic activity against tumorigenic cells and have too many side effects. Therefore, research on muramyl dipeptide (MDP) analogs has attracted interest...
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Investigation of peptide splicing using two‐peptide‐chain analogs of trypsin inhibitor SFTI‐1
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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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Identification of Substrates of Cytoplasmic Peptidyl-Prolyl Cis/Trans Isomerases and Their Collective Essentiality in Escherichia Coli
PublicationProtein folding often requires molecular chaperones and folding catalysts, such as peptidyl-prolyl cis/trans isomerases (PPIs). The Escherichia coli cytoplasm contains six well-known PPIs, although a requirement of their PPIase activity, the identity of their substrates and relative enzymatic contribution is unknown. Thus, strains lacking all periplasmic and one of the cytoplasmic PPIs were constructed. Measurement of their PPIase...
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Pegylated Fluorescent Peptides as Substrates of Proteolytic Enzymes
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Molecular basis of TRF proteins and their interactions with peptides
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The molecular function of kallikrein‐related peptidase 14 demonstrates a key modulatory role in advanced prostate cancer
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Synthesis and SAR Studies of Antibacterial Peptidyl Derivatives Based upon the Binding Site of Human Cystatin C
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Synthesis and transport studies of model dipeptides with modified n-terminal amino groups into e. coli k12 mutant strains
Publicationotrzymano na drodze syntezy chemicznej kilka modelowych dipeptydów zawierających n-terminalna guanidynę oraz betainę. zbadano transport tych peptydów do komorek e. coli k12, posiadających zróżnicowane systemy transportowe. wyniki badań potwierdziły brak transportu do komórek bakteryjnych z wykorzystaniem permeaz peptydowych. dodatnio naładowana i silnie polarna grupa aminowa uniemożliwia efektywny transport tych związków do komórek...
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Targeting melanocortin receptor type 1 with small peptides
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Biodegradation of nodularin and other nonribosomal peptides by the Baltic bacteria
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Meat and fermented meat products as a source of bioactive peptides
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Effect of ectoine on hydration spheres of peptides–spectroscopic studies
PublicationIn this paper, we use FTIR spectroscopy to characterize the hydration water of ectoine, its interactions with two peptides–diglycine and NAGMA, and the properties of water molecules in the hydration spheres of both peptides changed by the presence of the osmolyte. We found that the interaction of ectoine with the peptide hydration shells had no effect on its own hydration sphere. However, the enhanced hydration layer of the osmolyte...
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Hydration of Simple Model Peptides in Aqueous Osmolyte Solutions
PublicationThe biology and chemistry of proteins and peptides are inextricably linked with water as the solvent. The reason for the high stability of some proteins or uncontrolled aggregation of others may be hidden in the properties of their hydration water. In this study, we investigated the effect of stabilizing osmolyte–TMAO (trimethylamine N-oxide) and destabilizing osmolyte–urea on hydration shells of two short peptides, NAGMA (N-acetyl-glycine-methylamide)...
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Amino Acid and Peptide‐Based Antiviral Agents
PublicationA significant number of antiviral agents used in clinical practice are amino acids, short peptides, or peptidomimetics. Among them, several HIV protease inhibitors (e. g. lopinavir, atazanavir), HCV protease inhibitors (e. g. grazoprevir, glecaprevir), and HCV NS5A protein inhibitors have contributed to a significant decrease in mortality from AIDS and hepatitis. However, there is an ongoing need for the discovery of new antiviral...
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Evaluating the antibacterial activity of muramyl dipeptide derivatives, retro-tuftsin derivatives, and anthraquinone oligopeptides against a range of pathogenic bacteria
PublicationSearch for new and efficient antibiotic is crucial because of microbial drug resistance and problems with side effects of the administered medication. In this study, we evaluate the in vitro microbiological activity of muramyl dipeptide derivatives, retro-tuftsin derivatives (i.e., tuftsin with reversed amino acid sequences), and combinations of retro-tuftsin derivatives with substituted anthraquinones. The potency of the investigated...
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Functionalized Peptide Fibrils as a Scaffold for Active Substances in Wound Healing
PublicationTechnological developments in the field of biologically active peptide applications in medicine have increased the need for new methods for peptide delivery. The disadvantage of peptides as drugs is their low biological stability. Recently, great attention has been paid to self-assembling peptides that can form fibrils. Such a formulation makes bioactive peptides more resistant to enzymatic degradation and druggable. Peptide fibrils...
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New Selective Peptidyl Di(chlorophenyl) Phosphonate Esters for Visualizing and Blocking Neutrophil Proteinase 3 in Human Diseases
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