A5003741778- Photochromic and Fluorescence Chemistry
- Photoreceptor and optogenetics research
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Olfactory and Sensory Function Studies
- Synthesis of Indole Derivatives
- Protein purification and stability
- Receptor Mechanisms and Signaling
- Chemistry and Chemical Engineering
- Neurobiology and Insect Physiology Research
- Chemical Synthesis and Reactions
- HIV/AIDS drug development and treatment
- Retinal Development and Disorders
- Carbohydrate Chemistry and Synthesis
- Asymmetric Synthesis and Catalysis
- Crystallography and molecular interactions
- DNA and Nucleic Acid Chemistry
- Molecular Sensors and Ion Detection
- Advanced biosensing and bioanalysis techniques
- bioluminescence and chemiluminescence research
- Radical Photochemical Reactions
University of Regensburg
2018-2024
Peptide hydrazides are widely applied as precursors of peptide thioesters, valuable building blocks for the synthesis proteins by native chemical ligation. In addition, they can be selective modification cargo or carrier molecules using hydrazone ligation technique. this work, we describe key aspects solid phase on hydrazine 2CT and resin. Special attention is paid to optimization synthetic procedures "preferred" "usable" organic solvents. Thus, 2-CTC resin loading with Fmoc-hydrazine...
The desire to photocontrol molecular properties ranging from materials pharmacology using light as an external trigger with high spatiotemporal resolution led the development of a broad range photochromic scaffolds. Among them, azobenzenes are synthetically well accessible and show excellent fatigue resistance. Their vary substitution pattern for different heteroarenes. However, photochromism 3(5)-substituted-1H-pryazoles has not yet been investigated, although this compound class offers...
Background and Purpose Anion‐selective Cys‐loop receptors (GABA glycine receptors) provide the main inhibitory drive in CNS. Both types of receptor operate via chloride‐selective ion channels, though with different kinetics, pharmacological profiles, localization. Disequilibrium their function leads to a variety disorders, which are often treated allosteric modulators. The few available GABA channel blockers effectively suppress currents neurons, but systemic administration is highly toxic....
Abstract Optogenetic and photopharmacological tools to manipulate neuronal inhibition have limited efficacy reversibility. We report the design, synthesis, biological evaluation of Fulgazepam, a fulgimide derivative benzodiazepine that behaves as pure potentiator ionotropic γ‐aminobutyric acid receptors (GABA A Rs) displays full reversible photoswitching in vitro vivo. The compound enables high‐resolution studies GABAergic neurotransmission, phototherapies based on localized, acute, neuroinhibition.
Azobenzene-based light-controllable derivatives of 2-phenylethyl β-<sc>d</sc>-thiogalactoside as<italic>trans</italic>-active competitive inhibitors for β-galactosidase from<italic>Escherichia coli</italic>.
The solid-phase peptide synthesis (SPPS) of the C-terminal sequence hGH with one extra Tyr attached to its N-terminus (total 16 residues a disulfide bridge) has been accomplished for first time by optimizing several synthetic parameters. First all, two Ser (positions 9 and 13 molecule) have introduced as single amino acid, Fmoc-Ser(ψMe,Mepro)-OH, demonstrating that acylation these hindered moieties is possible. This allows us avoid use corresponding dipeptides, Fmoc-AA-Ser(ψMe,Mepro)-OH,...
Gamma aminobutyric acid type A receptors (GABA
The serotonin 5-hydroxytryptamine 3 receptor (5-HT R) plays a unique role within the seven classes of family, as it represents only ionotropic receptor, while other six members are G protein-coupled receptors (GPCRs). 5-HT is related to chemo-/radiotherapy provoked emesis and dysfunction leads neurodevelopmental disorders psychopathologies. Since development first antagonist in early 1990s, range highly selective potent drugs expanded based on various chemical structures. Nevertheless,...
Photopharmacology is a unique approach that through combination of photochemistry methods and advanced life science techniques allows the study control specific biological processes, ranging from intracellular pathways to brain circuits. Recently, first photochromic channel blocker anion-selective GABAA receptors, azobenzene-nitrazepam-based compound (Azo-NZ1), has been described. In present study, using patch-clamp technique in heterologous system mice slices, site-directed mutagenesis...
The histamine H1 G protein-coupled receptor (GPCR) plays an important role in allergy and inflammation. Existing drugs that address the differ their chemical structure, pharmacology, side effects. Light-controllable spatial temporal activity regulation of photochromic ligands may contribute to a better mechanistic understanding development improved correlations between ligand structure pharmacologic We report ligands, which were investigated organ-pharmacological assay. Initially, five...
Common protocols for the loading of 2-CTC and MBH-Br resins presume application DCM, THF, or DMF; these solvents are considered as undesirable in accordance with modern regulatory rules. An alternative option implies usage rather expensive 2-MeTHF. Herein, we describe an EtOAc/AcN (1:1) mixture efficient solvent incorporation first amino acid. We show that suggested reaction conditions ensure a level comparable to 2-MeTHF, DMF. The described procedure was designed kilogram-scale synthesis...
The Cover Feature shows the organ-pharmacological investigation of photochromic azobenzene-based antagonists at native G-protein-coupled histamine H1 receptor (H1R) expressed in smooth muscles guinea pig ileum. molecular structure most active antagonist is highlighted its two isomeric states, which can be interconverted from trans to cis via irradiation with blue light and back isomerized by thermal relaxation resulting a difference antagonistic activity factor 46. silhouette background...
ABSTRACT Glycine receptors (GlyRs) are indispensable to maintain excitatory/inhibitory balance in neuronal circuits controlling reflex and rhythmic motor behaviors. Here we have developed Glyght, the first GlyR ligand controlled with light. It is selective over other cys-loop receptors, active vivo , displays an allosteric mechanism of action. The photomanipulation glycinergic neurotransmission opens new avenues understand inhibitory intact animals, develop drug-based phototherapies.
The γ -aminobutyric acid gated chloride channel represents the major mediator of inhibitory neurotransmission in mammalian central nervous system and its dysfunction is related to severe diseases like epilepsy depression, which can be relieved by application allosteric modulators. However, drugs’ potential side-effects limit their for long-term treatment. Applying light as external stimulus modify pharmacophore’s activity, emerged field photopharmacology, provides a non-invasive tool with...
The <i>γ</i>-aminobutyric acid gated chloride channel represents the major mediator of inhibitory neurotransmission in mammalian central nervous system and its dysfunction is related to severe diseases like epilepsy depression, which can be relieved by application allosteric modulators. However, drugs’ potential side-effects limit their for long-term treatment. Applying light as external stimulus modify pharmacophore’s activity, emerged field photopharmacology, provides a...