A5052178512- Protein Kinase Regulation and GTPase Signaling
- PI3K/AKT/mTOR signaling in cancer
- Synthesis and bioactivity of alkaloids
- Cancer-related Molecular Pathways
- Synthesis and Reactivity of Heterocycles
- Cell death mechanisms and regulation
- Neuroscience and Neuropharmacology Research
- Marine Sponges and Natural Products
- Supramolecular Chemistry and Complexes
- Bioactive Compounds and Antitumor Agents
- Cancer, Lipids, and Metabolism
- Ubiquitin and proteasome pathways
- Chronic Lymphocytic Leukemia Research
- Insect Resistance and Genetics
- Viral Infectious Diseases and Gene Expression in Insects
- Drug Transport and Resistance Mechanisms
- Prostate Cancer Treatment and Research
- Liver Disease Diagnosis and Treatment
- Neuropeptides and Animal Physiology
- Pain Mechanisms and Treatments
- CRISPR and Genetic Engineering
- Epilepsy research and treatment
- Phytochemical compounds biological activities
- Synthesis and Properties of Aromatic Compounds
- Liver Disease and Transplantation
Assiut University
2012-2025
University of Siegen
2025
University of Münster
2019-2024
University Hospital Cologne
2022
University of Cologne
2019-2022
Abstract The fall armyworm, Spodoptera frugiperda , is a highly invasive pest that poses severe threats to food crop production worldwide. Several methods have been applied control armyworm infestations, including egg parasitoids, chemical insecticides, and transgenic crops expressing Bacillus thuringiensis (Bt) toxins. However, the currently available are either poorly effective or facing challenges such as resistance development environmental concerns. rapidly evolving molecular tools of...
The human phosphatidylinositol 4-phosphate 5-kinase type I α (hPIP5K1α) plays a key role in the development of prostate cancer. In this work, seventeen derivatives natural diterpene totarol were prepared by copper(I)-catalysed Huisgen 1,3-dipolar cycloaddition reaction correspondingO-propargylated with aryl or alkyl azides and screened for their inhibitory activities toward hPIP5K1α. Five compounds, 3a, 3e, 3f, 3i, 3r, strongly inhibited enzyme activity IC
The α2δ-1 subunit of voltage-gated calcium channels binds to gabapentin and pregabalin, mediating the analgesic action these drugs against neuropathic pain. Extracellular matrix proteins from thrombospondin (TSP) family have been identified as ligands in CNS. This interaction was found be crucial for excitatory synaptogenesis neuronal sensitisation which turn can inhibited by gabapentin, suggesting a potential role pathogenesis Here, we provide information on biochemical properties direct...
The human phosphatidylinositol 4‐phosphate 5‐kinase type I α (hPIP5K1α) participates in the phosphoinositide‐3‐kinase/protein kinase B/mammalian target of rapamycin signaling pathway. Despite evidence that hPIP5K1α plays a role development prostate cancer (PCa), only one inhibitor is known to date. With aim identifying new inhibitors, nonradiometric assay for measurement enzyme activity was developed. based on separation fluorescently labeled substrate phosphatidylinositol‐4‐phosphate...
Protein kinase CK2 is involved in regulating cellular processes, such as cell cycle, proliferation, migration, and apoptosis, making it an attractive anticancer target. We previously described a prenyloxy-substituted indeno[1,2-b]indole (5-isopropyl-4-(3-methylbut-2-enyloxy)-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione (4p)) very potent inhibitor of holoenzyme (IC50 = 25 nM). Here, we report the broad-spectrum activity 4p provide substantial progress on its pharmacokinetic properties....
Abstract Recent studies have shown the involvement of GluN2A subunit‐containing NMDA receptors in various neurological and pathological disorders. In X‐ray crystal structure, TCN‐201 ( 1 ) analogous pyrazine derivatives 2 3 adopt a U‐shape (hairpin) conformation within binding site formed by ligand domains GluN1 subunits. order to mimic resulting π/π‐interactions two aromatic rings site, [2.2]paracyclophane system was designed lock these parallel orientation. Acylation 5 with oxalyl chloride...
Animal models and clinical studies suggest an influence of angiotensin II (AngII) on the pathogenesis liver diseases via renin-angiotensin system. AngII application increases portal blood pressure, reduces bile flow, permeability tight junctions. Establishing subcellular localization receptor type 1 (AT1R), main receptor, helps to understand effects liver. We localized AT1R in situ human porcine gallbladder by immunohistochemistry. In order do so, we characterized commercial anti-AT1R...
Highly pleiotropic and constitutively active protein kinase CK2 is a key target in cancer therapy, but only one small‐molecule inhibitor has reached clinical trials—CX‐4945. In this study, we present the indeno[1,2‐ b ]indole derivative 5‐isopropyl‐4‐methoxy‐7‐methyl‐5,6,7,8‐tetrahydroindeno[1,2‐ ]indole‐9,10‐dione ( 5a‐2 ) that decreased intracellular activity A431, A549, LNCaP tumor cell lines analogous to CX‐4945 (> 75% inhibition at 20 µ m similarly blocked CK2‐specific Akt...
The highly pleiotropic and constitutively active serine/threonine protein kinase CK2 is considered a key target in cancer. indeno[1,2-b]indole scaffold was previously shown to provide derivatives exhibiting strong inhibition satisfactory drug-like characteristics. In this work, we evaluated one 4,5,7-trisubstituted derivative for its intracellular of activity the accompanying effects on proliferation, migration apoptosis cancer cells. compound...
Phosphoinositides are a family of tiny cellular lipids formed through series phosphorylation processes catalyzed by enzymes termed phosphatidylinositol-phosphate kinases (PIPKs). The phosphatidylinositol 4-phosphate 5-kinase type 1 α (PIP5K1α) is the main isoform responsible for generating membrane pools phosphatidylinositol-4,5-bisphosphate (PIP2), which, in turn, serves as substrate well-established cancer-relevant target, 3-kinases (PI3Ks). Recent studies provide strong evidence key role...