A5018936167- Organophosphorus compounds synthesis
- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Peptidase Inhibition and Analysis
- Phosphorus compounds and reactions
- DNA and Nucleic Acid Chemistry
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Carbohydrate Chemistry and Synthesis
- Analytical Chemistry and Chromatography
- Supramolecular Self-Assembly in Materials
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Machine Learning in Bioinformatics
- Asymmetric Hydrogenation and Catalysis
- Molecular spectroscopy and chirality
- Molecular Sensors and Ion Detection
- Monoclonal and Polyclonal Antibodies Research
- Glycosylation and Glycoproteins Research
- Antimicrobial Peptides and Activities
- Cancer Immunotherapy and Biomarkers
- CAR-T cell therapy research
- Synthesis and characterization of novel inorganic/organometallic compounds
- Axial and Atropisomeric Chirality Synthesis
- Surface Chemistry and Catalysis
- Enzyme function and inhibition
AGH University of Krakow
2017-2024
Wrocław University of Science and Technology
2011-2024
University of Wrocław
2011
Institute of Organic Chemistry
2003
University of Opole
2000
Abstract Blockade of the immunoinhibitory PD‐1/PD‐L1 pathway using monoclonal antibodies has shown impressive results with durable clinical antitumor responses. Anti‐PD‐1 and anti‐PD‐L1 have now been approved for treatment a number tumor types, whereas development small molecules targeting immune checkpoints lags far behind. We characterized two classes macrocyclic‐peptide inhibitors directed at pathway. show that these macrocyclic compounds act by directly binding to PD‐L1 they are capable...
Urease inhibitors are considered promising compounds for the treatment of ureolytic bacterial infections, particularly infections resulting from Helicobacter pylori in gastric tract. Herein, we present synthesis and inhibitory activity novel highly effective organoselenium as Sporosarcina pasteurii ureases. These studied represent a class competitive reversible urease inhibitors. The most active compound, 2-phenyl-1,2-benzisoselenazol-3(2H)-one (ebselen), displayed Ki values equal to 2.11...
The entry of the SARS-CoV-2 virus into a human host cell begins with interaction between viral spike protein (S protein) and angiotensin-converting enzyme 2 (hACE2). Therefore, possible strategy for treatment this infection is based on inhibiting two abovementioned proteins. Compounds that bind to S at interface alpha-1/alpha-2 helices ACE2 PD Subdomain I are particular interest. We present stepwise optimisation helical peptide foldamers containing trans-2-aminocylopentanecarboxylic acid...
Abstract Peptide foldamers containing both cis ‐β‐aminocyclopentanecarboxylic acid and α‐amino residues combined in various sequence patterns (ααβ, αααβ, αβααβ, ααβαααβ) were screened using CD NMR spectroscopy for the tendency to form helices. ααβ‐Peptides found fold into an unprecedented well‐defined 16/17/15/18/14/17‐helix. By extending length of or shifting a fragment from one terminus another ααβ‐peptides, balance between left‐handed right‐handed helix populations present solution can be...
Alpha-cyclodextrin was shown to be convenient chemical shift reagent for determination of the enantiomeric composition alpha-hydroxyphosphonic acids by means 31P NMR. The developed methodology appeared reliable, repetitive, easy perform and simple interpretation. Enantiomeric discrimination in NMR spectra 12 13 studied hydroxyphosphonates achieved, with baseline separation resonances obtained eight compounds. In those cases, nonequivalence values ranged from 0.069 0.313 ppm. studies showed...
The incorporation of cyclopentane-based beta-amino acid in the sequence peptide forming coiled-coil induced formation nanofibrils.
Abstract Quinines phosphorylated at the C‐9 hydroxyl group (diphenyl and diethyl phosphates) were synthesized validated as novel effective chiral solvating agents in two alternative methods based on 1 H 31 P NMR spectroscopy. Tested with a representative set of racemic analytes, title compounds induced shift nonequivalence effects signals values up to 0.1–0.2 ppm for 3,5‐dinitrobenzoyl‐substituted amino acids. In terms enantiodifferentiation extent application range, introduction phosphate...
Because of their unique 3D arrangement, naturally occurring Cinchona alkaloids and synthetic derivatives have found wide-ranging applications in chiral recognition. Recently, we determined the enantioselective properties C-9-phosphate mixed triesters quinine as versatile solvating agents nuclear magnetic resonance (NMR) spectroscopy. In current study, introduce new zwitterionic members this class molecules containing a negatively charged phosphate moiety (i.e., ethyl, n-butyl phenyl hydrogen...
Although the construction of peptides with well-defined three-dimensional structures and predictable functions, including biological activity, using conformationally constrained β-amino acids has been shown to be a very successful strategy, their broad application is limited by access appropriate building blocks. In particular, trans- cis-stereoisomers 2-aminocyclopentanecarboxylic acid (ACPC) are high interest. The scalable synthesis all four stereoisomers Fmoc derivatives ACPC presented...
Despite their importance in biology and industry, organophosphorus compounds appear quite rarely as an object of supramolecular chemistry studies. Development synthetic methods enabled to design synthesize complex structures thus develop chemistry. In this review, a state-of art showing current progress application host molecules bearing phosphate, phosphonate, phosphinate or phosphine oxide entities is presented. These structural elements are involved formation specific nets hydrogen bonds...
Peptide foldamers have been studied for over two decades and numerous sequence patterns shown to form well-defined three-dimensional arrangements in solution. In particular, helices of various geometries described. this article, different concepts concerning the construction helical foldameric peptides, which possibility governing sense formed helix was evidenced, are presented discussed.
The impact of constrained beta-amino acid substitutions on the conformational stability two model miniproteins was evaluated.
Abstract Blockade of the immunoinhibitory PD‐1/PD‐L1 pathway using monoclonal antibodies has shown impressive results with durable clinical antitumor responses. Anti‐PD‐1 and anti‐PD‐L1 have now been approved for treatment a number tumor types, whereas development small molecules targeting immune checkpoints lags far behind. We characterized two classes macrocyclic‐peptide inhibitors directed at pathway. show that these macrocyclic compounds act by directly binding to PD‐L1 they are capable...
Abstract Indirect UV detection capillary electrophoresis (CE) was used for the separation of aminoalkanephosphonic acid (AP) enantiomers by applying commercially available cyclodextrins as chiral discriminators. The results show that depends on pH background electrolyte, molar ratio cyclodextrin to aminophosphonic acid, and type applied selector. Optimization process conditions allowed enantiomeric baseline or partial 12 out 14 α‐aminophosphonic acids studied. This CE might therefore be...
Abstract Numerous beta‐amino acid containing peptides forming secondary structures have been already described, however the design of higher‐order remains poorly explored. The methodology allowing construction sequence patterns few rigid element was proposed and experimentally validated. On basis 9/10/9/12‐helix cis ‐2‐aminocyclopentanecarboxylic (cis‐ACPC) residues arranged in an ααββ pattern, a conformationally stable helix‐turn‐helix structure designed. connection between two helices also...
The influence of aqueous solution pD on stereoselective complexation N-benzyloxycarbonylaminophosphonic acids with alpha-cyclodextrin was investigated by means nuclear magnetic resonance spectroscopy. highest enantiodiscrimination achieved at close to the pKa less acidic hydroxyl group phosphonic moiety analytes (6.5-7.5). This effect results from differentiation (up 0.28 unit) upon applied chemical shift reagent. Moreover, analysis 2D-ROESY spectra proved that host-guest inclusion mode is...