A5059635297- Organophosphorus compounds synthesis
- Peptidase Inhibition and Analysis
- Protease and Inhibitor Mechanisms
- Chemical Synthesis and Analysis
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Phosphorus compounds and reactions
- Genomics, phytochemicals, and oxidative stress
- Synthesis and biological activity
- Monoclonal and Polyclonal Antibodies Research
- Click Chemistry and Applications
- Neuropeptides and Animal Physiology
- Animal health and immunology
- Asymmetric Hydrogenation and Catalysis
- Glutathione Transferases and Polymorphisms
- Cell Adhesion Molecules Research
- Sulfur-Based Synthesis Techniques
- Synthesis and characterization of novel inorganic/organometallic compounds
- Synthesis and Reactions of Organic Compounds
- Osteoarthritis Treatment and Mechanisms
- Bone health and treatments
- Multicomponent Synthesis of Heterocycles
- Synthesis and Characterization of Heterocyclic Compounds
- Carbohydrate Chemistry and Synthesis
- Pneumocystis jirovecii pneumonia detection and treatment
- Ubiquitin and proteasome pathways
Wrocław University of Science and Technology
2013-2022
AGH University of Krakow
2017-2022
University of Wrocław
2012
Georgia Institute of Technology
1989-1994
Institute of Organic Chemistry
1978-1981
Peptidyl derivatives of diphenyl (alpha-aminoalkyl)phosphonates have been synthesized and are effective specific inhibitors serine proteases at low concentrations. Z-PheP(OPh)2 irreversibly reacts with chymotrypsin (kobsd/[I] = 1200 M-1 s-1) does not react two elastases. The best inhibitor for most chymotrypsin-like enzymes including bovine chymotrypsin, cathepsin G, rat mast cell protease II is the tripeptide Suc-Val-Pro-PheP(OPh)2 which corresponds to sequence an excellent p-nitroanilide...
Diaryl esters of α-aminophosphonates are a group low molecular weight inhibitors serine proteases. For over 30 years these molecules have captured the attention biochemists and medicinal chemists due to their similarity transition state peptide bond cleavage observed in enzymatic reactions (transition analogs) as well high potency action. High reactivity toward proteases complete lack activity against cysteine or threonine give great advantage other classes such chloromethyl ketones peptidyl...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTNovel amidine-containing peptidyl phosphonates as irreversible inhibitors for blood coagulation and related serine proteasesJozef Oleksyszyn, Bogdan Boduszek, Chih-Min Kam, James C. PowersCite this: J. Med. Chem. 1994, 37, 2, 226–231Publication Date (Print):January 1, 1994Publication History Published online1 May 2002Published inissue 1 January 1994https://pubs.acs.org/doi/10.1021/jm00028a004https://doi.org/10.1021/jm00028a004research-articleACS...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDipeptide Phosphonates as Inhibitors of Dipeptidyl Peptidase IVBogdan Boduszek, Jozef Oleksyszyn, Chih-Min Kam, Joe Selzler, Robert E. Smith, and James C. PowersCite this: J. Med. Chem. 1994, 37, 23, 3969–3976Publication Date (Print):November 1, 1994Publication History Published online1 May 2002Published inissue 1 November 1994https://doi.org/10.1021/jm00049a016RIGHTS & PERMISSIONSArticle Views638Altmetric-Citations90LEARN ABOUT THESE...
Betulin and betulinic acid are naturally occurring pentacyclic triterpenes showing cytotoxicity towards a number of cancer cell lines. These compounds can be found in the bark many plants. In this report we have compared cytotoxic activity crude birch extract purified betulin human gastric carcinoma (EPG85-257) pancreatic (EPP85-181) drug-sensitive drug-resistant (daunorubicin mitoxantrone) Our results show significant differences sensitivity between lines depending on compound used, suggest...
The mechanistic details of the pathogenesis Chlamydia, an obligate intracellular pathogen global importance, have eluded scientists due to scarcity traditional molecular genetic tools investigate this organism. Here we report a chemical biology strategy that has uncovered first essential protease for Identification and application unique CtHtrA inhibitor (JO146) cultures Chlamydia resulted in complete loss viable elementary body formation. JO146 treatment during replicative phase development...
Herein, we present the synthesis and measurement of inhibitory activity novel peptidyl derivatives α-aminoalkylphosphonate diaryl esters as human neutrophil elastase inhibitors. Their selectivity against other serine proteases, including porcine pancreatic elastase, chymotrypsin, trypsin, was also demonstrated. We describe preparation single peptide diastereomers. The most active selective compound developed possessed a kinact/KI 2353000 M–1 s–1, which is potent irreversible inhibitor...
Carbonylverbindungen (I) und Benzylurethan (II) ergeben in siedendem Eisessig mit Phosphortrichlorid nach Hydrolyse 1-Aminoalkanphosphonsauren (III) Dichlorphosphanen (IV) 1-Aminoalkanphosphinsauren (V).
Early detection of cancer development is crucial for successful therapy and monitoring patient outcome. Various immunodiagnostic methods are able to detect pathological changes in the human body ahead symptomatic manifestation disease. Most immunological examinations based on specific tumor markers fluids. Of various cancer-specific proteins used breast diagnostics, one most commonly applied antigen 15-3 (CA 15-3). An elevation its serum level (>25-40 U/ml) usually correlates with...
Aminopeptidase N/CD13 (EC 3.4.11.2) is suggested to play a role in cancer cells invasion, and its activity can be inhibited using specific inhibitors. CD13 inhibitors evoke apoptosis of CD13-positive cells. However, expression has not been described specimens obtained from ovarian carcinomas. Thus, the present study, significance was examined samples cancers. The analyses were performed on sections originating 73 tumor (43 primary laparotomies [PL] 30 secondary cytoreductions [SCRs])....
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTReaction of porcine pancreatic elastase with 7-substituted 3-alkoxy-4-chloroisocoumarins: design potent inhibitors using the crystal structure complex formed 4-chloro-3-ethoxy-7-guanidinoisocoumarinJames C. Powers, Jozef Oleksyszyn, S. Lakshmi Narasimhan, Chih Min Kam, R. Radhakrishnan, and E. F. Meyer, Jr.Cite this: Biochemistry 1990, 29, 12, 3108–3118Publication Date (Print):March 1, 1990Publication History Published online1 May 2002Published...
Measurement of serum prostate specific antigen (PSA) concentrations remains one the leading methods for diagnosing cancer. We developed and evaluated an immunoglobulin Y (IgY)-based ELISA to measure total PSA (tPSA) in human that could be used as alternative commercially available vitro diagnostic assays rely on mouse monoclonal IgG.A sandwich based anti-PSA IgY antibody was developed. ability detect free complexed at same molar ratio. The assay optimized, its analytical performance verified...
A series of 3-alkoxy-7-amino-4-chloroisocoumarins with various 3-alkoxy substituents have been prepared and evaluated as inhibitors human leukocyte elastase (HLE). In addition, a new acyl, urea, carbamate derivatives 7-amino-4-chloro-3-methoxyisocoumarin (1), 7-amino-4-chloro-3-propoxyisocoumarin (3), 7-amino-4-chloro-3-(2-bromoethoxy)isocoumarin (6) synthesized. Most the synthesized compounds are very potent HLE kobs/[I] values between 10(4) 10(6) M-1 s-1. Hydrophobic on 7-amino position...