AIMing towards Improved Antitumor Efficacy‡
| Autor: | Mariusz P. Gajewski, Donald S. Backos, Alison K. Kearns, Howard D. Beall, Kevin C. Rider, Sascha Stump, Matthew J. Weaver, Nicholas R. Natale, Philip Reigan, Chun Li |
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| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Clinical Biochemistry
Pharmaceutical Science Antineoplastic Agents Apoptosis Molecular Dynamics Simulation Crystallography X-Ray Biochemistry Article law.invention Structure-Activity Relationship Confocal microscopy law Cell Line Tumor Drug Discovery medicine Humans Molecular Biology Cell permeability Binding Sites Oligonucleotide Chemistry Circular Dichroism Organic Chemistry Telomere medicine.disease Amides G-Quadruplexes Biophysics Molecular Medicine Nucleic Acid Conformation Glioblastoma |
| Popis: | Using the structure–activity relationship emerging from previous Letter, and guided by pharmacokinetic properties, new AIMs have been prepared with both improved efficacy against human glioblastoma cells and cell permeability as determined by fluorescent confocal microscopy. We present our first unambiguous evidence for telomeric G4-forming oligonucleotide anisotropy by NMR resulting from direct interaction with AIMs, which is consistent with both our G4 melting studies by CD, and our working hypothesis. Finally, we show that AIMs induce apoptosis in SNB-19 cells. |
| Databáze: | OpenAIRE |
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