Search results for: PEPTIDE CONJUGATES
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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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The molecular function of kallikrein‐related peptidase 14 demonstrates a key modulatory role in advanced prostate cancer
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Copper(II) coordination properties of GxG peptides: Key role of side chains of central residues on coordination of formed systems; combined potentiometric and ITC studies
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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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Neutrophil proteinase 3 and dipeptidyl peptidase I (cathepsin C) as pharmacological targets in granulomatosis with polyangiitis (Wegener granulomatosis)
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Anna Lisowska-Oleksiak prof. dr hab.
PeopleAnna Lisowska-Oleksiak, born in 1952, has been working at GUT since 1977. Currently is employed at the Faculty of Chemistry as a full professor. She was employed as a research assistant at the University of St Andrews in the group of C. A. Vincent and P.G. Bruce (1991-1994). She completed a two-month research internship in CEA Grenoble (2011). Anna Lisowska-Oleksiak obtained her MSc in chemistry at Nicolaus Copernicus University...
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Terapetyczne działanie peptydów stosowanych w preparatach kosmetycznych na starzejacą się skórę
PublicationW publikacji opisano obecnie stosowane na rynku kosmetycznym peptydy, które można podzielić na trzy grupy: peptydy rozkurczające (tzw. neuropeptydy), transportujące i sygnałowe (stymulujące). Wśród peptydów rozkurczających możemy wymienić: acetylo-heksapeptyd-3 (nazwa rynkowa Argireline), pentapeptyd-3 (nazwa rynkowa Leuphasyl) oraz acetylo-oktapeptyd-1 (nazwa rynkowa SNAP-8). Peptydy transportujące to niezwykle interesująca grupa...
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Cu(II) complexes with peptides from FomA protein containing -His-Xaa-Yaa-Zaa-His and -His-His-motifs. ROS generation and DNA degradation
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Fluconazole resistant Candida auris clinical isolates have increased levels of cell wall chitin and increased susceptibility to a glucosamine-6-phosphate synthase inhibitor
PublicationIn 2009 Candida auris was first isolated as fungal pathogen of human disease from ear canal of a patient in Japan. In less than a decade, this pathogen has rapidly spread around the world and has now become a major health challenge that is of particular concern because many strains are resistant to multiple class of antifungal drugs. The lack of available antifungals and rapid increase of this fungal pathogen provides an incentive...
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Structural properties of hydration shell around various conformations of simple polypeptides
PublicationIn this paper we investigate structural properties of water within the solvation shell around the peptide core created by a well-defined conformation of polypeptide chain. The following secondary structures are investigated: linear (straight chain), and three helices PII (polyproline-like), 310, and α. We propose using the two-particle contribution to entropy as a rational measure of the water structural ordering within the solvation...
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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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Kallikrein-Related Peptidase 14 Activates Zymogens of Membrane Type Matrix Metalloproteinases (MT-MMPs)—A CleavEx Based Analysis
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Inhibitory syntazy glukozamino-6-fosforanu o zwiększonej lipofilowości i ich peptydy - synteza i właściwości biologiczne
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Effect of in vitro gastro‐pancreatic digestion on antioxidant activity of low‐molecular‐weight (<3.5 kDa) peptides from dry‐cured pork loins with probiotic strains of LAB
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The structurally similar TRFH domain of TRF1 and TRF2 dimers shows distinct behaviour towards TIN2
PublicationThe telomere repeat binding-factor 1 and 2 (TRF1 and TRF2) proteins of the shelterin complex bind to duplex telomeric DNA as homodimers, and the homodimerization is mediated by their TRFH (TRF-homology) domains. We performed molecular dynamic (MD) simulations of the dimer forms of TRF1TRFH and TRF2TRFH in the presence/absence of the TIN2TBM (TIN2, TRF-interacting nuclear protein 2, TBM, TRF-binding motif) peptide. The MD results...
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A Novel Biological Role for Peptidyl-Arginine Deiminases: Citrullination of Cathelicidin LL-37 Controls the Immunostimulatory Potential of Cell-Free DNA
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Kallikrein-related peptidase 14 activates zymogens of membrane type matrix metalloproteinases (MT-MMPs) - a CleavEx library-based analysis
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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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‘Acridines’ as New Horizons in Antifungal Treatment
PublicationFrequent fungal infections in immunocompromised patients and mortality due to invasive mycosis are important clinical problems. Opportunistic pathogenic Candida species remain one of the leading causes of systemic mycosis worldwide. The repertoire of antifungal chemotherapeutic agents is very limited. Although new antifungal drugs such as lanosterol 14α-demethylase and β-glucan synthase inhibitors have been introduced into clinical...
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Whole-genome sequencing and antimicrobial potential of bacteria isolated from Polish honey
PublicationThe aim of this study was the whole-genome analysis and assessment of the antimicrobial potential of bacterial isolates from honey harvested in one geographical location—the north of Poland. In total, 132 strains were derived from three honey samples, and the antimicrobial activity of CFAM (cell-free after-culture medium) was used as a criterion for strain selection and detailed genomic investigation. Two of the tested isolates...
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Właściwości otoczki hydratacyjnej wokół różnych konformacji poliseryny - analiza wyników dynamiki molekularnej
PublicationRozpuszczalnik w istotny sposób wpływa na preferencje peptydu do przyjmowania określonej struktury drugorzędowej. Przykładem tego może być fakt, iż w przypadku polialaniny stabilność konformacji helikalnej w wodzie jest niższa aniżeli w próżni, podczas gdy w przypadku poliseryny mamy do czynienia ze zjawiskiem odwrotnym. W celu lepszego zrozumienia tego zjawiska badano właściwości otoczek hydratacyjnych dookoła czterech konformacji...
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Analiza in silico bioaktywnych peptydów pochodzących z keratyny z piór drobiowych
PublicationKeratyna należy do najbardziej powszechnie występujących białek strukturalnych pochodzenia zwierzęcego. Stanowi ok. 90% masy piór wytwarzanych w dużych ilościach przez przemysł drobiarski. Ten odpadowy produkt pozostaje w dużym stopniu niezagospodarowany. Celem pracy była analiza bioinformatyczna pierwszorzędowej struktury keratyny z piór kurzych pod kątem występowania w niej peptydów bioaktywnych....
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Design, Synthesis, and Enzymatic Evaluation of Novel ZnO Quantum Dot-Based Assay for Detection of Proteinase 3 Activity
PublicationHerein, the synthesis and application of functionalized quantum dot-based protease probes is described. Such probes are composed of nontoxic ZnO nanocrystals decorated by amino groups followed by linker and labeled peptide attachment. Spherical NH2-terminated ZnO quantum dots (QDs) with the average size ranging from 4 to 8 nm and strong emission centered at 530 nm were prepared using the sol−gel method. The fluorescence of ZnO...
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Pigment production and secretion by psychrotolerant yeast-like fungi at 25 °C for 2 days
Open Research DataThree strains, named Red, Pink and Black, were grown in five different media with the following compositions: 1% peptone K, 2% glucose; 2% peptone K, 2% glucose; 1% yeast extract, 2% glucose; 1% peptone K, 1% yeast extract, 2% glucose; 1% peptone K, 2% yeast extract, 2% glucose (YPD) for 2 days at 25°C with shaking 180 rpm. The cultures were then centrifuged...
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Pigment production and secretion by psychrotolerant yeast-like fungi at 15 °C for 4 days
Open Research DataThree strains, named Red, Pink and Black, were grown in five different media with the following compositions: 1% peptone K, 2% glucose; 2% peptone K, 2% glucose; 1% yeast extract, 2% glucose; 1% peptone K, 1% yeast extract, 2% glucose; 1% peptone K, 2% yeast extract, 2% glucose (YPD) for 4 days at 15°C with shaking 180 rpm. The cultures were then centrifuged...
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Pigment production and secretion by psychrotolerant yeast-like fungi at 20 °C for 2 days
Open Research DataThree strains, named Red, Pink and Black, were grown in five different media with the following compositions: 1% peptone K, 2% glucose; 2% peptone K, 2% glucose; 1% yeast extract, 2% glucose; 1% peptone K, 1% yeast extract, 2% glucose; 1% peptone K, 2% yeast extract, 2% glucose (YPD) for 2 days at 20°C with shaking 180 rpm. The cultures were then centrifuged...
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Pigment production and secretion by psychrotolerant yeast-like fungi at 15 °C for 2 days
Open Research DataThree strains, named Red, Pink and Black, were grown in five different media with the following compositions: 1% peptone K, 2% glucose; 2% peptone K, 2% glucose; 1% yeast extract, 2% glucose; 1% peptone K, 1% yeast extract, 2% glucose; 1% peptone K, 2% yeast extract, 2% glucose (YPD) for 2 days at 15°C with shaking 180 rpm. The cultures were then centrifuged...
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Structural and dynamic properties of water within the solvation layer around various conformations of the glycine-based polypeptide
PublicationSeveral conformations of the solvated glycine-based polypeptides were investigated using molecular dynamics simulations. Some properties of water in the neighbouring space around these molecules were investigated. It was found, that water forms a well-defined layer - the first solvation shell - around the peptide molecule, and thickness of this layer is independent of the peptide structure, and it equals to approximately 0.28 nm....
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Transport deficiency is the molecular basis of Candida albicans resistance to antifungal oligopeptides
Publication(FMDP), an inhibitor of glucosamine-6-phosphate synthase, exhibited growth inhibitory activity against Candida albicans, with minimal inhibitory concentration values in the 0.05–50 mg/L range. Uptake by the peptide permeases was found to be the main factor limiting an anticandidal activity of these compounds. Di- and tripeptide containing FMDP (F2 and F3) were transported by Ptr2p/Ptr22p peptide transporters (PTR) and FMDP-containing...
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Fluorescent analogs of trypsin inhibitor SFTI-1 isolated from sunflower seeds-synthesis and applications
PublicationThis article describes the synthesis and enzymatic study of newly synthesized analogs of trypsin inhibitors SFTI-1 that were fluorescent labeled on their N-terminal amino groups. Two fluorescent derivatives of benzoxazole (3-[2-(4-diphenylaminophenyl) benzoxazol-5-yl]-L-alanine[(4NPh(2)) Ph] Box-Ala and 3-[2-(2', 4', 5'-trimethoxyphenyl) benzoxazol-5-yl]-l-alanine-[2,4,5-(OMe)3Ph] Box-Ala) were used as efficient fluorescent labels....
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Unspecified peptic ulcer as acute or chronic, without haemorrhage or perforation - Male, 55 - Tissue image [12050630013036061]
Open Research DataThis is the histopathological image of STOMACH tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Unspecified peptic ulcer as acute or chronic, without haemorrhage or perforation - Male, 55 - Tissue image [12050630013026341]
Open Research DataThis is the histopathological image of STOMACH tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Structural and Dynamic Properties of Water within the Solvation Layer around Various Conformations of the Glycine-based Polypeptide
PublicationSeveral conformations of the solvated glycine-based polypeptides were investigated using molecular dynamics simulations. Some properties of water in the neighboring space around these molecules were investigated. It was found that water forms a well-defined layer—the first solvation shell—around the peptide molecule, and thickness of this layer is independent of the peptide structure and is equal to approximately 0.28 nm. Within...
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublicationImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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Phase I and phase II metabolism simulation of antitumor-active 2-hydroxyacridinone with electrochemistry coupled on-line with mass spectrometry.
PublicationHere, we report the metabolic profile and the results of associated metabolic studies of 2-hydroxyacridinone (2-OH-AC), the reference compound for antitumor-active imidazo- and triazoloacridinones. Electrochemistry coupled with mass spectrometry was applied to simulate the general oxidative metabolism of 2-OH-AC for the first time. The reactivity of 2-OH-AC products to biomolecules was also examined. The usefulness of the electrochemistry...
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Exploiting the S4–S5 Specificity of Human Neutrophil Proteinase 3 to Improve the Potency of Peptidyl Di(chlorophenyl)-phosphonate Ester Inhibitors: A Kinetic and Molecular Modeling Analysis
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Sławomir Milewski prof. dr hab. inż.
PeopleSławomir Milewski, born in 1955 in Puck, Poland, graduated in 1979 in Chemistry from the Faculty of Chemistry, Gdańsk University of Technology (GUT). In 1984 was employed at the Department of Pharmaceutical Technology and Biochemistry. In 1985 he got his PhD, in 1994 became a DSc (habilitation) and in 2002 got the professorship in chemical sciences. Currently he is a full professor and Head of the Department of Pharmaceutical Technology...
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The time-dependent cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to cancer LNCaP cells
Open Research DataThe time-dependent (1, 24, 48, and 72 h) cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to cancer LNCaP cells performed by Confocal Laser Scanning Microscopy (63× magnification; ZEISS LSM T-PMT, Magdeburg, Germany). Based on the fluorescence properties of these compounds, green and orange fluorescence...
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The time-dependent cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to cancer H460 cells
Open Research DataThe time-dependent (1, 24, 48, and 72 h) cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to cancer H460 cells performed by Confocal Laser Scanning Microscopy (63× magnification; ZEISS LSM T-PMT, Magdeburg, Germany). Based on the fluorescence properties of these compounds, green and orange fluorescence...
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The time-dependent cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal PNT1A cells
Open Research DataThe time-dependent (1, 24, 48, and 72 h) cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal PNT1A cells performed by Confocal Laser Scanning Microscopy (63× magnification; ZEISS LSM T-PMT, Magdeburg, Germany). Based on the fluorescence properties of these compounds, green and orange fluorescence...
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Optical fiber aptasensor for label-free bacteria detection in small volumes
PublicationHighly sensitive devices for fast bacteria detection are sought to be developed with the task of quantifying the worldwide problem of pathogenic bacteria and thus helping to take control over spreading bacterial infections. This work concerns a sensing solution based on microcavity in-line Mach-Zehnder interferometer (μIMZI) induced in an optical fiber. Such a device exhibits ultrahigh sensitivity to refractive index changes...
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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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In vitro enzyme kinetics and NMR-based product elucidation for glutathione S-conjugation of the anticancer unsymmetrical bisacridine C-2028 in liver microsomes and cytosol: major role of glutathione S-transferase M1-1 isoenzyme
PublicationThis work is the next step in studying the interplay between C-2028 (anticancer-active unsymmetrical bisacridine developed in our group) and the glutathione S-transferase/glutathione (GST/GSH) system. Here, we analyzed the concentration- and pH-dependent GSH conjugation of C-2028 in rat liver microsomes and cytosol. We also applied three recombinant human GST isoenzymes, which altered expression was found in various tumors. The...
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The time-dependent cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to cancer Du-145 cells
Open Research DataThe time-dependent (1, 24, 48, and 72 h) cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to cancer Du-145 cells performed by Confocal Laser Scanning Microscopy (63× magnification; ZEISS LSM T-PMT, Magdeburg, Germany). Based on the fluorescence properties of these compounds, green and orange fluorescence...
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The time-dependent cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal MRC-5 cells
Open Research DataThe time-dependent (1, 24, 48, and 72 h) cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal MRC-5 cells performed by Confocal Laser Scanning Microscopy (63× magnification; ZEISS LSM T-PMT, Magdeburg, Germany). Based on the fluorescence properties of these compounds, green and orange fluorescence...
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Multicopy Suppressor Analysis of Strains Lacking Cytoplasmic Peptidyl-Prolyl cis/trans Isomerases Identifies Three New PPIase Activities in Escherichia coli That Includes the DksA Transcription Factor
PublicationConsistent with a role in catalyzing rate-limiting step of protein folding, removal of genes encoding cytoplasmic protein folding catalysts belonging to the family of peptidyl-prolyl cis/trans isomerases (PPIs) in Escherichia coli confers conditional lethality. To address the molecular basis of the essentiality of PPIs, a multicopy suppressor approach revealed that overexpression of genes encoding chaperones (DnaK/J and GroL/S),...
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A novel chemiluminescent immunoassay for detection of Toxoplasma gondii IgG in human sera
PublicationThis study describes Toxoplasma gondii IgG chemiluminescent immunoassay (CLIA) based on the use of a novel immunochemical reagents in the form of the conjugates of original acridinium ester (AE) labels attached to antibodies and SAG2-GRA1-ROP1L chimeric antigen and shows that this test is useful for diagnostic purposes.
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The impact of methods the stochastic analysis on swimming safety of multihull floating units (Part 2)
PublicationIn part 2 the equations of the catamaran motion were divided into the system of two groups not conjugated with themselves containing the mutually conjugated equations. The feedback is obtained by the linear and nonlinear coefficients of dampening and coefficients of hydrostatic elasticity. The first group includes the symmetric movements (longitudinal movements), and the second group includes the antisymmetric movements (transverse)....
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Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIa and Aurora B
PublicationIn the search for new anticancer agents we designed and synthesized batracylin derivatives with linking synthetic amino acid side chains of different lengths and adenosine. Unexpectedly, we have found that in water and the culture media adenosine–amino acid–BAT conjugates form supramolecular structures and this prevents these compounds from entering cells. Consequently, these compounds exerted no biological activity when tested...
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The mechanism of internalization study of QDgreen−CD−FA−C−2028 conjugate at IC80 value to cancer (H460, Du-145, and LNCaP) and normal (MRC-5 and PNT1A) cells
Open Research DataThe influence of different endocytosis inhibitors on the internalization of QDgreen−CD−FA−C−2028 conjugate at IC80 value in cancer (H460, Du-145, and LNCaP) and normal (MRC-5 and PNT1A) cells. First, the cells were preincubated with: drug-free medium (no inhibitor), at 4 °C, 5 µM Cytochalasin D, 30 µM Amiloride, 80 µM Dynasore, 25 µM Pitstop 2 and 1.5...