Gaining Insights into Specific Drug Formulation Additives for Solubilizing a Potential Anti-Alzheimer Disease Drug B4A1
| العنوان: | Gaining Insights into Specific Drug Formulation Additives for Solubilizing a Potential Anti-Alzheimer Disease Drug B4A1 |
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| المؤلفون: | Anna Grafl, Marcus Pickhardt, Hans G. Börner, Eckhard Mandelkow, Katharina Linkert, Frank Polster, Carmen Lawatscheck |
| المصدر: | Macromolecular Bioscience Macromolecular bioscience 17(10), 1700109 (2017). doi:10.1002/mabi.201700109 |
| بيانات النشر: | Wiley, 2017. |
| سنة النشر: | 2017 |
| مصطلحات موضوعية: | Polymers and Plastics, Peptide, 02 engineering and technology, Pharmaceutical formulation, 01 natural sciences, Polyethylene Glycols, chemistry [Nootropic Agents], chemistry.chemical_compound, chemical synthesis [Peptides], Materials Chemistry, drug therapy [Alzheimer Disease], metabolism [Nootropic Agents], Nootropic Agents, media_common, chemistry.chemical_classification, Drug Carriers, Aniline Compounds, 021001 nanoscience & nanotechnology, Small molecule, 3. Good health, Solutions, chemistry [Polyethylene Glycols], Biochemistry, Biological Assay, 0210 nano-technology, chemistry [Aniline Compounds], Biotechnology, chemistry [Sensory System Agents], Drug, Drug Compounding, media_common.quotation_subject, chemistry [Peptides], MAPT protein, human, tau Proteins, Bioengineering, 010402 general chemistry, Biomaterials, Protein Aggregates, Alzheimer Disease, ddc:570, PEG ratio, Humans, chemical synthesis [Drug Carriers], metabolism [Aniline Compounds], metabolism [Sensory System Agents], chemistry [tau Proteins], technology, industry, and agriculture, Combinatorial chemistry, 0104 chemical sciences, Drug Liberation, antagonists & inhibitors [tau Proteins], Solubility, chemistry, Solubilization, Sensory System Agents, Peptides, Ethylene glycol, Conjugate |
| الوصف: | The pharmacological profiles of small molecule drugs are often challenged by their poor water solubility. Sequence-defined peptides attached to poly(ethylene glycol) (PEG) offer opportunities to overcome these difficulties by acting as drug-specific formulation additives. The peptide-PEG conjugates enable specific, noncovalent drug binding via tailored peptide/drug interactions as well as provide water solubility and drug shielding by well-solvated PEG-blocks. A systematic set of specific solubilizers for B4A1 as a potential anti-Alzheimer disease drug is synthesized and variations involve the length of the PEG-blocks as well as the sequences of the peptidic drug-binding domain. The solubilizer/B4A1 complexes are studied in order to understand contributions of both PEG and peptide segments on drug payload capacities, drug/carrier aggregate sizes, and influences on inhibition of the Tau-protein aggregation in an in vitro assay. |
| تدمد: | 1616-5187 |
| DOI: | 10.1002/mabi.201700109 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::724efbc0ba6a44d110363760bb20f955 https://doi.org/10.1002/mabi.201700109 |
| Rights: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....724efbc0ba6a44d110363760bb20f955 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 16165187 |
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| DOI: | 10.1002/mabi.201700109 |