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Prof dr hab Adam Lesner
Employment
- 1995 - present professor at Chemistry
Publications
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total: 116
Catalog Publications
Year 1997
Year 2000
Year 2001
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Chromogenic Substrates of Bovine β-Trypsin: The Influence of an Amino Acid Residue in P1 Position on Their Interaction with the Enzyme
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Synthesis, activity on NK-3 tachykinin receptor and conformational solution studies of scyliorhinin II analogs modified at position 16
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Year 2002
Year 2004
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A simple method for selection of trypsin chromogenic substrates using combinatorial chemistry approach
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Microarray analysis of differentially expressed genes in cells resistant to HIV-1
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Monoubiquitinated Histone H1B Is Required for Antiviral Protection in CD4+T Cells Resistant to HIV-1
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Year 2007
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Design of serine proteinase inhibitors by combinatorial chemistry using trypsin inhibitor SFTI‐1 as a starting structure
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Inhibition of HIV‐1 or bacterial activation of macrophages by products of HIV‐1‐resistant human cells
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New chromogenic substrates of human neutrophil cathepsin G containing non-natural aromatic amino acid residues in position P1 selected by combinatorial chemistry methods
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Selection of New Chromogenic Substrates of Serine Proteinases Using Combinatorial Chemistry Methods
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Trypsin inhibitors from the garden four o’clock (Mirabilis jalapa) and spinach (Spinacia oleracea) seeds: Isolation, characterization and chemical synthesis
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Year 2008
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Design of selective substrates of proteinase 3 using combinatorial chemistry methods
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Designing of Substrates and Inhibitors of Bovine α-Chymotrypsin with Synthetic Phenylalanine Analogues in Position P1
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Development of sensitive cathepsin G fluorogenic substrate using combinatorial chemistry methods
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New potent cathepsin G phosphonate inhibitors
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Peptomeric analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds
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The influence of substrate peptide length on human β‐tryptase specificity
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Year 2009
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Application of specific cell permeable cathepsin G inhibitors resulted in reduced antigen processing in primary dendritic cells
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Identification of X-DING-CD4, a new member of human DING protein family that is secreted by HIV-1 resistant CD4+ T cells and has anti-viral activity
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Introduction of non-natural amino acid residues into the substrate-specific P1 position of trypsin inhibitor SFTI-1 yields potent chymotrypsin and cathepsin G inhibitors
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Low-Molecular-Weight Aldehyde Inhibitors of Cathepsin G
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Year 2010
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Analogues of Trypsin Inhibitor SFTI-1 with Disulfide Bridge Substituted by Various Length of Carbonyl Bridges
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Highly Specific Substrates of Proteinase 3 Containing 3-(2-Benzoxazol-5-yl)-l-alanine and Their Application for Detection of This Enzyme in Human Serum
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Implication of the disulfide bridge in trypsin inhibitor SFTI-1 in its interaction with serine proteinases
PublicationFourteen monocyclic analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds were synthesized by the solid-phase method. The purpose of this work was to establish the role of a disulfide bridge present in inhibitor's side chains of Cys3 and Cys11 in association with serine proteinases. This cyclic fragment was replaced by the disulfide bridges formed by L-pencillamine (Pen), homo-L-cysteine (Hcy), N-sulfanylethylglycine...
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Inhibitory activity of double‐sequence analogues of trypsin inhibitor SFTI‐1 from sunflower seeds: an example of peptide splicing
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Selection of peptomeric inhibitors of bovine α-chymotrypsin and cathepsin G based on trypsin inhibitor SFTI-1 using a combinatorial chemistry approach
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Substrate specificity and inhibitory study of human airway trypsin-like protease
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The new fluorogenic substrates of neutrophil proteinase 3 optimized in prime site region
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Year 2011
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Analogues of trypsin inhibitor SFTI-1 modified in the conserved P1′ position by synthetic or non-proteinogenic amino acids retain their inhibitory activity
PublicationA series of linear and monocyclic (with a disulfide bridge only) analogues of trypsin inhibitor SFTI-1 modified in the P-1 and/or P-1' positions were synthesized by the solid-phase method. In the substrate specificity P-1 position, Phe or N-benzylglycine (Nphe) were introduced, whereas the conserved Ser6 in Bownam-Birk (BBI) inhibitors was replaced by Hse (L-homoserine), Nhse [N-(2-hydroxyethyl)glycine], Sar, and Ala. Kinetic studies...
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Introduction of Pro and Its Analogues in the Conserved P1 Position of Trypsin Inhibitor SFTI-1 Retains Its Inhibitory Activity
PublicationA number of monocyclic SFTI-1 analogues modified in the conserved inhibitor P1 position by Pro, its L-hydroxyproline (Hyp) derivative as well as mimetics with different ring size were synthesized by the solid-phase method. Replacement of Ser6 by Pro, Hyp, and a four-member ring, L-azetidine-2-carboxylic acid (Aze), retained trypsin or chymotrypsin inhibitory activity. The determined association equilibrium constants of these analogues...
Year 2012
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Editorial(Hot Topic: Proteolysis in Health and Disease)
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Future of Protease Activity Assays
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Inhibitory and antimicrobial activities of OGTI and HV-BBI peptides, fragments and analogs derived from amphibian skin
PublicationA series of linear and cyclic fragments and analogs of two peptides (OGTI and HV-BBI) isolated from skin secretions of frogs were synthesized by the solid-phase method. Their inhibitory activity against several serine proteinases: bovine beta-trypsin, bovine alpha-chymotypsin, human leukocyte elastase and cathepsin G from human neutrophils, was investigated together with evaluation of their antimicrobial activities against Gram-negative...
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Pegylated Fluorescent Peptides as Substrates of Proteolytic Enzymes
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Reporter Fluorescent Molecules in Biological Systems: The Current Overview
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Substrate specificity of Staphylococcus aureus cysteine proteases – Staphopains A, B and C
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Surface plasmon resonance imaging biosensor for cathepsin G based on a potent inhibitor: Development and applications
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Three Wavelength Substrate System of Neutrophil Serine Proteinases
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Year 2013
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A new proteinase 3 substrate with improved selectivity over human neutrophil elastase
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Adrenal Secretory Protease
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Biochemical and Structural Characterization of SplD Protease from Staphylococcus aureus
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Hybrid analogues of SFTI-1 modified in P1 position by β- and γ-amino acids and N-substituted β-alanines
PublicationA series of compounds containing either non-proteinogenic beta-/gamma-amino acids or N-substituted beta-alanine residues (beta-peptoid units) in P-1 specificity position were synthesized based on the structure of sunflower trypsin inhibitor 1 (SFTI-1). The compounds were synthesized on a solid support; the N-substituted beta-alanines (beta Nhlys and beta Nhphe) were introduced into a peptidomimetic chain via a two-step approach...
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Inhibitors of cathepsin G: a patent review (2005 to present)
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Microarrays and Dynamics of Fluorescent Dyes
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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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Temperature-induced changes of HtrA2(Omi) protease activity and structure
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Year 2014
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