A5092074819- Bioactive Compounds and Antitumor Agents
- Mitochondrial Function and Pathology
- Synthesis of Organic Compounds
- Synthesis and biological activity
- Autophagy in Disease and Therapy
- Cancer therapeutics and mechanisms
- Synthesis and properties of polymers
- ATP Synthase and ATPases Research
- Natural Compound Pharmacology Studies
- Click Chemistry and Applications
- Phytochemicals and Antioxidant Activities
- Synthetic Organic Chemistry Methods
- Computational Drug Discovery Methods
- Multicomponent Synthesis of Heterocycles
- Acute Lymphoblastic Leukemia research
- Plant biochemistry and biosynthesis
- Acute Myeloid Leukemia Research
- Ion Channels and Receptors
- Endoplasmic Reticulum Stress and Disease
- Chemical Synthesis and Analysis
- Histone Deacetylase Inhibitors Research
- Carbohydrate Chemistry and Synthesis
TU Dresden
2023-2024
In response to the pressing global challenge of antibiotic resistance, time efficient design and synthesis novel antibiotics are immense need. Polycyclic polyprenylated acylphloroglucinols (PPAP) were previously reported effectively combat a range gram-positive bacteria. Although exact mode action is still not clear, we conceptualized late-stage divergent approach expand our natural product-based PPAP library by 30 additional entities perform SAR studies against methicillin-resistant...
Polycyclic polyprenylated acylphloroglucinols (PPAPs) comprise a large group of compounds mostly plant origin. The best-known compound is hyperforin from St. John's wort with its antidepressant, antitumor and antimicrobial properties. Chemical synthesis PPAP variants allows the generation improved activity compatibility. Here we studied two synthetic PPAP-derivatives, 23 53, as to their activity. While insoluble in water, sodium salt, water-soluble. In vitro, both exhibited good...
Pre-SARS-CoV-2, tuberculosis was the leading cause of death by a single pathogen. Repetitive exposure Mycobacterium tuberculosis(Mtb) supported development multidrug- and extensively drug-resistant strains, demanding novel drugs. Hyperforin, natural type A polyprenylated polycyclic acylphloroglucinol from St. John's wort, exhibits antidepressant antibacterial effects also against Mtb. Yet, Hyperforin's instability limits utility in clinical practice. Here, we present photo- bench-stable B...
Selective modulation of TRPC6 ion channels is a promising therapeutic approach for neurodegenerative diseases and depression. A significant advancement showcases the selective activation through metalated type-B PPAP, termed PPAP53. This success stems from PPAP53's 1,3-diketone motif facilitating metal coordination. PPAP53 water-soluble as potent hyperforin, gold standard in this field. In contrast to type-A, PPAPs offer advantages such gram-scale synthesis, easy derivatization, long-term...
Polycyclic polyprenylated acylphloroglucinols (PPAPs) comprise a large group of compounds mostly plant origin. The best-known compound is hyperforin from St. John's wort with its antidepressant, antitumor and antimicrobial properties. chemical synthesis PPAP variants allows the generation improved activity compatibility. Here, we studied two synthetic PPAP-derivatives, water-insoluble PPAP23 water-soluble sodium salt PPAP53. In vitro, both exhibited good against methicillin-resistant
Abstract The synaptic vesicle glycoprotein 2A (SV2A) is a transmembrane protein of vesicles. It involved in key functions neurons, focused on the regulation neurotransmitter release. Here we report three novel findings suggesting completely new role SV2A. First, demonstrate that SV2A localized at outer mitochondrial membrane (OMM) using confocal and super-resolution microscopy. Second, Inactivation our cell animal models leads to fragmented mitochondria. In addition, also affects basal...
<title>Abstract</title> The synaptic vesicle glycoprotein 2A (SV2A) is a transmembrane protein of vesicles. It involved in key functions neurons, focused on the regulation neurotransmitter release. Here we report three novel findings suggesting completely new role SV2A. First, demonstrate that SV2A localized at outer mitochondrial membrane (OMM) using confocal and super-resolution microscopy. Second, Inactivation our cell animal models leads to fragmented mitochondria. In addition, also...
Before the emergence of SARS-CoV-2, tuberculosis (TB) was leading cause infectious disease mortality worldwide. Like all antibiotic-exposed bacteria Mycobacterium (Mtb) developed multidrug-resistant (MDR) and exten-sively drug-resistant (XDR) strains which require new antibiotics with novel mechanism actions. Hyperforin, a natural type-A polyprenylated polycyclic acylphloroglucinol (PPAP) isolated from St. John’s wort, is known for its antibacterial, antidepressant antimycobacterial...
The selective modulation of TRPC6 ion channels has emerged as a promising therapeutic approach for treating neuro-degenerative diseases and depression. Here, we present significant advancement in this field by demonstrating the se-lective activation using metallated type-B PPAP, designated PPAP53. success PPAP53 is attributed to utilization 1,3-diketone motif PPAPs metal coordination. exhibit water solubility equipotent activity compared hyperforin, which natural product considered gold...