A5030984251- Computational Drug Discovery Methods
- Cholinesterase and Neurodegenerative Diseases
- Synthesis and biological activity
- Enzyme function and inhibition
- Pharmacological Receptor Mechanisms and Effects
- Alzheimer's disease research and treatments
- Crystallization and Solubility Studies
- Histone Deacetylase Inhibitors Research
- Cell Adhesion Molecules Research
- Zebrafish Biomedical Research Applications
- RNA Interference and Gene Delivery
- Neuroinflammation and Neurodegeneration Mechanisms
- Tryptophan and brain disorders
- X-ray Diffraction in Crystallography
- Neuroscience and Neuropharmacology Research
- Receptor Mechanisms and Signaling
- Epigenetics and DNA Methylation
- S100 Proteins and Annexins
Columbia University Irving Medical Center
2024
Yeditepe University
2018-2022
German Center for Neurodegenerative Diseases
2021-2022
The risk of developing Alzheimer's disease (AD) significantly increases in individuals carrying the APOEε4 allele. Elderly cognitively healthy with also exist, suggesting presence cellular mechanisms that counteract pathological effects APOEε4; however, these are unknown. We hypothesized carriers without dementia might carry genetic variations could protect them from APOEε4-mediated AD pathology. To test this, we leveraged whole-genome sequencing (WGS) data National Institute on Aging...
Drug development efforts that focused on single targets failed to provide effective treatment for Alzheimer's disease (AD). Therefore, we designed cholinesterase inhibition (ChEI)-based multi-target-directed ligands (MTDLs) simultaneously target AD-related receptors. We built a library of 70 compounds, sequentially screened ChEI, and determined σ1R, σ2R, NMDAR-GluN2B binding affinities, P2X7R antagonistic activities. Nine fulfilled in silico drug-likeness criteria did not display toxicity...
The success rate of novel drug candidates in clinical trials relies on the safety and efficacy data preclinical studies. Although cell-based assays are widely used, complexity an vivo system to mimic human disease pathophysiology is essential. Despite wide usage rodent models for discovery, increasing repertoire animal that allow investigation various pathological mechanisms with a unique operational strength discovery required. Zebrafish, teleost vertebrate, its high similarity tissue...
Objective and Method: A new series of benzothiazole-piperazine derivatives was synthesized a complete chemical characterization the novel compounds provided. In vitro cytotoxic activities were screened against colorectal (HCT-116), breast (MCF-7) hepatocellular (Huh7) cancer cell lines by Sulforhodamine B assay. Result Discussion: All showed activity lines. Dihalo substituted benzylpiperazine (2a, 2e) had highest in all tested addition, acetylcholinesterase (AChE) butyrylcholinesterase...
Background: Infectious diseases are a major threat in the developing world and discovery of novel antimicrobial agents remains to be crucial due acquired resistance by microorganisms. Additionally, various can prevented with antioxidant as they eliminate harmful effects reactive oxygen species. Objective: In this study, it was aimed synthesize compounds bearing N-(6- methoxybenzothiazol-2-yl)-3-(4-substitued piperazinyl)propanamide backbone that had activities. Mechanisms activity were...
The pivotal role of the myeloid ecotropic viral integration site 1 (MEIS1) transcriptional factor was reported in cardiac regeneration and hematopoietic stem-cell (HSC) regulation with our previous findings. MEIS1 as a promising target context pharmacological inhibition, we identified potent (MEIS) inhibitor, MEISi-1, to induce murine human HSC expansion ex vivo vivo. In this work, performed lead optimization on MEISi-1 by synthesizing 45 novel analogues. Structure-activity relationship...