A5053287872- Biochemical and Structural Characterization
- Peptidase Inhibition and Analysis
- Radiopharmaceutical Chemistry and Applications
- Monoclonal and Polyclonal Antibodies Research
- Chemical Synthesis and Analysis
- Chemical Reactions and Isotopes
- Forensic Toxicology and Drug Analysis
- Lung Cancer Treatments and Mutations
- HER2/EGFR in Cancer Research
- Cancer Treatment and Pharmacology
- Neuroscience and Neuropharmacology Research
- Glycosylation and Glycoproteins Research
- Neuroendocrine Tumor Research Advances
- Cannabis and Cannabinoid Research
- Receptor Mechanisms and Signaling
- Botulinum Toxin and Related Neurological Disorders
- Neurotransmitter Receptor Influence on Behavior
- Enzyme Production and Characterization
- Synthesis and Biological Evaluation
- Antibiotic Resistance in Bacteria
- Pharmacological Receptor Mechanisms and Effects
- Asymmetric Hydrogenation and Catalysis
- Lanthanide and Transition Metal Complexes
- Antimicrobial Peptides and Activities
Roche (Switzerland)
2020-2024
Massachusetts Institute of Technology
2014-2015
Johannes Gutenberg University Mainz
2007-2013
ETH Zurich
2013
Sanofi (Germany)
2009
Synthetic extracellular matrices are widely used in regenerative medicine and as tools building vitro physiological culture models. hydrogels display advantageous physical properties, but challenging to modify with large peptides or proteins. Here, a facile, mild enzymatic postgrafting approach is presented. Sortase-mediated ligation was conjugate human epidermal growth factor fused GGG motif (GGG-EGF) poly(ethylene glycol) (PEG) containing the sortase LPRTG substrate. The reversibility of...
Conventional thermal and microwave conditions were compared for hydrogen-deuterium (H/D) exchange reactions of aminobenzoic acids catalysed by NaBD(4)-activated Pd/C or RhCl(3) with D(2)O as the deuterium source. We also investigated different metal catalysts (including Pd/C, Pt/C) under an efficient H/D aromatic heterocyclic compounds. Even higher incorporations obtained Pt/C catalyst mixtures due to previously observed synergistic effect. Finally, we have applied these optimised one-step...
Radiolabeled hybrid ligands with defined distances between an agonist and antagonist for the gastrin-releasing peptide receptor were found to have excellent tumor-targeting properties. Oligoprolines served as rigid scaffolds that allowed tailoring of 10, 20, 30 Å recognition elements. In vitro in vivo studies revealed ligand a distance 20 elements exhibits highest yet observed tumor cell uptake retention time prostate cancer cells.
The methamphetamine molecule has a chiral center and exists as 2 enantiomers, d-methamphetamine (the more active enantiomer) l-methamphetamine less enantiomer). d-Methamphetamine is associated with intense stimulant effects higher abuse liability. objective of this study was to measure the pharmacokinetics for comparison both (-)-cocaine in baboon brain peripheral organs assess saturability pharmacologic specificity binding.d- were labeled (11)C via alkylation norprecursors (11)C-methyl...
Monoacylglycerol lipase (MAGL) is a key enzyme involved in the metabolism of endogenous signaling ligand 2-arachidonoylglycerol, neuroprotective endocannabinoid intimately linked to central nervous system (CNS) disorders associated with neuroinflammation. In quest for novel MAGL inhibitors, focused screening approach on Roche library subset provided reversible benzoxazinone hit exhibiting high efficiency. The subsequent design three-dimensional
Recent reports have claimed a superior performance of HEPES buffer in comparison to alternative systems for 67/68 Ga labeling aqueous media. In this paper we report spectroscopic ( 1 H and 71 NMR), radiochemical, mass spectrometry theoretical modeling studies on the 3+ /HEPES system (HEPES = N ‐2‐hydroxyethylpiperazine‐ ′‐2‐ethanesulfonic acid) performed with aim elucidating potential contribution 68/67 radiolabeling process. Our results demonstrate that acts as weakly but competitive...
Described is the development and application of a versatile semisynthetic strategy, based on combination sortase-mediated coupling tetrazine ligation chemistry, which can be exploited for efficient incorporation tunable functionality into chimeric recombinant proteins. To demonstrate scope method, assembly set bivalent ligands, integrate members epidermal growth factor (EGF) ligand family, described. By using series EGFs with variable intraligand spacing, differences in structure were...
Abstract Described is the development and application of a versatile semisynthetic strategy, based on combination sortase‐mediated coupling tetrazine ligation chemistry, which can be exploited for efficient incorporation tunable functionality into chimeric recombinant proteins. To demonstrate scope method, assembly set bivalent ligands, integrate members epidermal growth factor (EGF) ligand family, described. By using series EGFs with variable intraligand spacing, differences in structure...