Search results for " Inhibitor"
showing 10 items of 3219 documents
Electrostatic complementarity in pseudoreceptor modeling based on drug molecule crystal structures: the case of loxistatin acid (E64c)
2015
After a long history of use as a prototype cysteine protease inhibitor, the crystal structure of loxistatin acid (E64c) is finally determined experimentally using intense synchrotron radiation, providing insight into how the inherent electronic nature of this protease inhibitor molecule determines its biochemical activity. Based on the striking similarity of its intermolecular interactions with those observed in a biological environment, the electrostatic potential of crystalline E64c is used to map the characteristics of a pseudo-enzyme pocket.
Protonation of Tyrosine Kinase Inhibitor Lapatinib: A Theoretical and Experimental Study
2019
The protonation process of tyrosine kinase inhibitor lapatinib was studied by means of 1HNMR and UV/Vis spectroscopy joint with the theoretical calculations at DFT and semi-empirical levels. DFT/M06-2X geometries were used to describe and compare the different cationic forms of lapatinib, while ZINDO/S-CI method performed on those geometries allowed for the interpretation of experimental UV/Vis spectra of lapatinib at various pH. We found that at low pH two different dicationic forms (N2N1 and N1N3) of lapatinib were present in ethanol and DMSO-d6 solutions. The first protonation, however, occurred on the aliphatic N1 in DMSO-d6, while in ethanol solutions most probably the quinazoline nitr…
Effect of different concentrations of specific inhibitor of matrix metalloproteinases on the shear bond strength of self-adhesive resin cements to de…
2017
Background Considering the probability of chemical and enzymatic reactions between matrix metalloproteinases (MMPs) in the dentin structure and their specific inhibitors, the aim of the present study was to evaluate the effect of different concentrations of specific inhibitor of MMPs (galardin) on the shear bond strength of self-adhesive resin cements to dentin. Material and Methods Forty-eight sound human premolars were mounted in self-cured acrylic resin after removal of the enamel on the buccal and lingual surfaces. The dentin surfaces achieved were polished and prepared with 600-grit silicon carbide paper. The samples were divided into 3 groups (n=16) based on the concentration of galar…
Two maize Kip-related proteins differentially interact with, inhibit and are phosphorylated by cyclin D–cyclin-dependent kinase complexes
2017
Highlight Maize Kip-related proteins can be differentially phosphorylated by different cyclin D–cyclin-dependent kinase complexes and this influences their performance as cyclin-dependent kinase inhibitors.
Phosphinotripeptidic Inhibitors of Leucylaminopeptidases
2021
Phosphinate pseudopeptide are analogs of peptides containing phosphinate moiety in a place of the amide bond. Due to this, the organophosphorus fragment resembles the tetrahedral transition state of the amide bond hydrolysis. Additionally, it is also capable of coordinating metal ions, for example, zinc or magnesium ions. These two properties of phosphinate pseudopeptides make them an ideal candidate for metal-related protease inhibitors. This research investigates the influence of additional residue in the P2 position on the inhibitory properties of phosphinopeptides. The synthetic strategy is proposed, based on retrosynthetic analysis. The N-C-P bond formation in the desired compounds is …
Oxylipin mediated stress response of a miraculin-like protease inhibitor in Hexanoic acid primed eggplant plants infested by Colorado potato beetle
2017
Insect-plant interactions are governed by a complex equilibrium between the mechanisms through which plant recognize insect attack and orchestrate downstream signaling events that trigger plant defense responses, and the mechanisms by which insects overcome plant defenses. Due to this tight and dynamic interplay, insight into the nature of the plant defense response can be gained by analyzing changes in the insect herbivores digestive system upon plant feeding. In this work we have identified a Solanum melongena miraculin-like protease inhibitor in the midgut juice of Colorado potato larvae feeding on eggplant plants treated with the natural inducer of plant defenses hexanoic acid. We analy…
Antifungal and antimycotoxigenic activity of hydrolyzed goat whey on Penicillium spp: An application as biopreservation agent in pita bread
2020
Abstract Whey is a by-product of the cheese industry, yet it contains proteins that have a high nutritional value and are an important source of antifungal peptides. Food deterioration caused by toxigenic fungi is one of the challenges of food safety. In this context, trypsin was used to hydrolyse goat milk whey at 37. The resultant peptides were characterised by LC–ESI–TOF-MS. Antifungal activity of the goat milk whey hydrolysate (HGW) was determined against 10 toxigenic fungi from the genus Penicillium, in solid and liquid media. Furthermore, HGW was used as an ingredient for bread elaboration. Bread elaborated with HGW and inoculated with toxigenic fungi was included in a shelf-life stud…
Applicability of a single‐use bioreactor compared to a glass bioreactor for the fermentation of filamentous fungi and evaluation of the reproducibili…
2021
Abstract The implementation of single‐use technologies offers several major advantages, e.g. prevention of cross‐contamination, especially when spore‐forming microorganisms are present. This study investigated the application of a single‐use bioreactor in batch fermentation of filamentous fungus Penicillium sp. (IBWF 040‐09) from the Institute of Biotechnology and Drug Research (IBWF), which is capable of intracellular production of a protease inhibitor against parasitic proteases as a secondary metabolite. Several modifications to the SU bioreactor were suggested in this study to allow the fermentation in which the fungus forms pellets. Simultaneously, fermentations in conventional glass b…
Wild
2021
Graphical abstract
Functional and Pharmacological Analyses of the Role of Penicillium digitatum Proteases on Virulence
2019
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