A5051441647- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Peptidase Inhibition and Analysis
- Organophosphorus compounds synthesis
- Neuropeptides and Animal Physiology
- Chemical Synthesis and Analysis
- Phosphorus compounds and reactions
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Click Chemistry and Applications
- Polyamine Metabolism and Applications
- Catalytic Cross-Coupling Reactions
- Sulfur-Based Synthesis Techniques
- Fungal Plant Pathogen Control
- Protein Hydrolysis and Bioactive Peptides
- Oral and gingival health research
- Animal Nutrition and Physiology
- Garlic and Onion Studies
Wrocław University of Science and Technology
2017-2022
AGH University of Krakow
2017-2022
Inhibitory activity of 14 phosphonic analogues phenylglycine, substituted in aromatic ring by fluorine and chlorine, was determined towards porcine aminopeptidase N. The obtained data served as a basis for studying their interaction with the enzyme modelled use Schrödinger Release 2018 program. observed linearity between Gibbs free energy differences inhibitory constants indicated usefulness this binding mode compared bovine lens leucine aminopeptidase. Although both enzymes differ...
The inhibitory activity of 14 racemic phosphonic acid analogs phenylglycine, substituted in aromatic rings, towards porcine aminopeptidase N (pAPN) and barley seed was determined experimentally. obtained patterns the against two enzymes were similar. data served as a basis for studying binding modes these inhibitors by pAPN using molecular modeling. It found that their aminophosphonate fragments bound highly uniform manner difference affinities most likely resulted from mode substitution...
The incorporation of dehydroamino acid or fragments oxazole into peptide chain is accompanied by a distorted three-dimensional structure and additionally enables the introduction non-typical side-chain substituents. Thus, such compounds could be building blocks for obtaining novel foldamers and/or artificial enzymes (artzymes). In this paper, effective synthetic procedures leading to blocks-tetrapeptides containing glycyldehydroalanine, glycyldehydrophenylalanine, glycyloxazole subunits-are...
A library of phosphonic acid analogs phenylalanine substituted with fluorine, chlorine and trifluoromethyl moieties on the aromatic ring was synthesized evaluated for inhibitory activity against human (hAPN) porcine (pAPN) aminopeptidases. Fluorogenic screening indicated that these are micromolar or submicromolar inhibitors, both enzymes being more active hAPN. In order to better understand mode action most compounds, molecular modeling used. It confirmed aminophosphonic portion enzyme is...
GRAPHICAL ABSTRACTDiethyl boronobenzylphosphonates as substrates in Suzuki–Miyaura reactionAll authorsAgata Rydzewska, Anna Mangold, Weronika Wanat & Paweł Kafarskihttps://doi.org/10.1080/10426507.2017.1284845Published online:25 May 2017
A library of novel phosphonic acid analogues homophenylalanine and phenylalanine, containing fluorine bromine atoms in the phenyl ring, have been synthesized. Their inhibitory properties against two important alanine aminopeptidases, human (hAPN, CD13) porcine (pAPN) origin, were evaluated. Enzymatic studies comparison with literature data indicated higher potential over phenylalanine derivatives towards both enzymes. inhibition constants submicromolar range for hAPN micromolar pAPN,...