A5103264552- Click Chemistry and Applications
- Chemical Synthesis and Analysis
- Protein Kinase Regulation and GTPase Signaling
- Microbial Natural Products and Biosynthesis
- Computational Drug Discovery Methods
- Peptidase Inhibition and Analysis
- Estrogen and related hormone effects
- Blood disorders and treatments
- Cancer therapeutics and mechanisms
- Carbohydrate Chemistry and Synthesis
- Cancer Treatment and Pharmacology
- Steroid Chemistry and Biochemistry
- Palliative Care and End-of-Life Issues
- Neutrophil, Myeloperoxidase and Oxidative Mechanisms
- Synthetic Organic Chemistry Methods
- Enzyme Catalysis and Immobilization
- Biochemical and Molecular Research
- Clinical practice guidelines implementation
- Artificial Intelligence in Healthcare and Education
- Cancer survivorship and care
- Protein Structure and Dynamics
- Nitric Oxide and Endothelin Effects
- Ubiquitin and proteasome pathways
- Lung Cancer Diagnosis and Treatment
- Enzyme function and inhibition
Fraunhofer Institute for Industrial Mathematics
2022-2023
Max Planck Institute of Molecular Physiology
2009-2017
TU Dortmund University
2011-2017
Max Planck Society
2009
University of Tübingen
2008
Finding the target: Activity-based proteomic profiling probes based on depalmitoylation inhibitors palmostatin B and M (see picture) have been synthesized were found to target acyl protein thioesterase 1 (APT1) 2 (APT2) in cells.
Sequence homology indicates the existence of three human cytosolic acyl protein thioesterases, including APT1 that is known to depalmitoylate H- and N-Ras. One them lysophospholipase-like 1 (LYPLAL1) on one hand predicted be closely related but other might also function as a potential triacylglycerol lipase involved in obesity. However, its role remained unclear. The 1.7 Å crystal structure LYPLAL1 reveals fold very similar APT1, expected, features shape active site precludes binding...
In the third place: Inspired by tetrahydroisoquinoline (THIQ) alkaloid noscapine, inhibitors of tubulin polymerization that bind to a site different from colchicine and vinca binding sites have been synthesized. One compound is more potent than noscapine in HeLa cells can overcome resistance chemotherapeutics.
Abstract Ras proteins are of importance in cell proliferation, and hence their mutated forms play causative roles many kinds cancer different tissues. Inhibition the Ras‐depalmitoylating enzyme acyl protein thioesterases APT1 ‐2 is a new approach to modulating cycle. Here we present boronic borinic acid derivatives as class potent nontoxic APT inhibitors. These compounds were detected by extensive library screening using chemical arrays turned out inhibit human competitive mode. Furthermore,...
Abstract Neutrophils are short‐lived leukocytes that migrate to sites of infection as part the acute immune response, where they phagocytose, degranulate, and form neutrophil extracellular traps (NETs). During NET formation, nuclear lobules neutrophils disappear chromatin expands and, accessorized with neutrophilic granule proteins, is expelled. NETs can be pathogenic in, for example, sepsis, cancer, autoimmune cardiovascular diseases. Therefore, identification inhibitors formation great...
A library of small tetrahydroisoquinoline ligands, previously identified via structure- and chemistry-based hierarchical organization scaffolds in tree-like arrangements, has been generated as novel estrogen receptor agonistic fragments traditional medicinal chemistry exploration. The approach described allowed for the rapid evaluation a structure−activity relationship ligands concerning affinity β subtype selectivity. structural biological insights obtained from aid understanding larger...
Abstract This publication presents a solution approach to oncological aftercare for cancer patients by means of artificial intelligence (AI) methods. shall support in overcoming the after-effects therapy effectively with suitable supportive actions and health-care professionals goal-oriented planning these actions. Different AI methods are used analyzing patients’ needs depending on available health data monitoring Decision effective based results analysis. The is realized form web...