A5069135539- Monoclonal and Polyclonal Antibodies Research
- Chemical Synthesis and Analysis
- Cell Adhesion Molecules Research
- Click Chemistry and Applications
- Synthesis and Catalytic Reactions
- Peptidase Inhibition and Analysis
- Biochemical and Structural Characterization
- Virus-based gene therapy research
- Ginseng Biological Effects and Applications
- Signaling Pathways in Disease
- RNA Interference and Gene Delivery
- Synthetic Organic Chemistry Methods
- Biological Activity of Diterpenoids and Biflavonoids
- Viral Infectious Diseases and Gene Expression in Insects
- Carbohydrate Chemistry and Synthesis
- Natural product bioactivities and synthesis
- Microbial Natural Products and Biosynthesis
Bielefeld University
2014-2020
University of Wollongong
2015
This work investigates the temperature-dependent micelle formation as well micellar structure of saponin aescin. The critical concentration ( c m ) aescin is determined from concentration-dependent autofluorescence (AF) Values between , AF (10 ∘ C) = 0.38 ± 0.09 mM and (50 0.32 0.13 were obtained. significance this method verified by tensiometry measurements. value within experimental error identical with values obtained T WP (23 0.33 0.02 mM). micelles was investigated small-angle X-ray...
Thirty two new binaphthyl-based, oxazole and thiazole peptidomimetics were prepared, which showed antibacterial activity (MICs 1–16 μg mL<sup>−1</sup>) against both Gram positive negative isolates.
Halogenated l- or d-tryptophan obtained by biocatalytic halogenation was incorporated into RGD peptides together with a variety of alkyl aryl boronic acids. Suzuki–Miyaura cross-coupling either in solution on-resin results side chain-to-tail-cyclized peptides, for example, biaryl moieties, providing new dimension structure–activity relationships. An array differing macrocycle size, the presence d-amino acid, N-methylation, connectivity between indole moiety and acid showed that, particular,...
Cryptophycins are potent tubulin polymerization inhibitors with picomolar antiproliferative potency in vitro and activity against multidrug-resistant (MDR) cancer cells. Because of neurotoxic side effects limited efficacy vivo, cryptophycin-52 failed as a clinical candidate treatment. However, this class compounds has emerged attractive payloads for tumor-targeting applications. In study, cryptophycin was conjugated to the cyclopeptide
Monomeric RGD peptides show unspecific fluid-phase uptake in cells, whereas multimeric are thought to be internalized by integrin-mediated endocytosis. However, a potential correlation between mechanism and molecular mass has been neglected so far. A dual derivatization of peptide c(RGDw(7Br)K) was performed investigate this. fluorescent probe installed chemoselective Suzuki-Miyaura cross-coupling the 7-bromotryptophan poly(ethylene glycol) (PEG) linker attached lysine residue. Flow...
Tryptophan (Trp) derivatives constitute important building blocks found in many natural products, peptides, and drugs. Accordingly, there is a high demand for suitable biocatalytic pathways providing selective derivatization of Trp like C–H functionalization or Cα-oxidation. The specific l-amino acid oxidase RebO from the actinomycete L. aerocolonigenes was harnessed chemoenzymatic oxidation substituted derivatives. An array potential substrates tested, several are being accepted with...
Most anticancer agents are hydrophobic and can easily penetrate the tumor cell membrane by passive diffusion. This may impede development of highly effective tumor-selective treatment options. A hydrophilic β-glucuronidase-cleavable linker was used to connect potent antimitotic agent cryptophycin-55 glycinate with αv β3 integrin ligand c(RGDfK). Incorporation self-immolative containing glucuronic acid results in lower cytotoxicity than that free payload, suggesting sugar linkers preclude...
The epidermal growth factor receptor (EGFR) plays a central role in the progression of many solid tumors. We used this validated target to analyze de novo design EGFR-binding peptides and their application for delivery complex payloads via rational viral vector. Peptides were computationally designed interact with EGFR dimerization interface. Two new reference (EDA peptide) chemically synthesized, binding ability characterized. Presentation these each 60 capsid proteins recombinant...
An array of l- and d-halotryptophans with different substituents at the indole moiety was synthesized employing either enzymatic halogenation by halogenases or incorporation haloindoles using tryptophan synthase. Introduction these Trp derivatives into RGD peptides as a benchmark system performed to investigate their influence on bioactivity. Halotryptophan-containing display increased affinity toward integrin αvβ3 enhanced selectivity over α5β1. In addition, bromotryptophan exploited...
Cyclic RGD peptides are well-known ligands of integrins. The integrins αV β3 and α5 β1 involved in angiogenesis, integrin is abundantly present on cancer cells, thus representing a therapeutic target. Hence, synthetic biophysical studies continuously being directed towards the understanding ligand-integrin interaction. In this context, development versatile strategies to obtain fluorescent building blocks that can add molecular diversity modular spectral characteristics while not...
Integrin ligands containing the tripeptide sequences Arg-Gly-Asp (RGD) and iso-Asp-Gly- Arg (isoDGR) were actively investigated as inhibitors of tumor angiogenesis directing unit in tumor-targeting drug conjugates. Reported herein is synthesis, two RGD one isoDGR cyclic peptidomimetics (1S,2R) (1R,2S) cis-2-amino-1-cyclopentanecarboxylic acid (cis-β-ACPC), using a mixed solid phase/solution phase synthetic protocol. The three examined vitro competitive binding assays to purified αvβ3 α5β1...
A range of substituted cycloalkene-1,1-dicarboxylates was synthesized through olefin metathesis starting from readily available acylic malonate precursors in an efficient fashion.As a catalyst, Grubbs II-type catalyst used these experiments, which were run water and gave the cyclic products with high conversions 94-100%.The catalytic amount 0.5-5 mol% dependent on structure material.The generality this reaction demonstrated as well its suitability for preparation five six-membered alkyl...