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Full-Text Articles in Pharmaceutics and Drug Design

Evaluation Of A Drug Delivery System Based On Cyclodextrins For Cancer Therapy, Caroline Mendes Jan 2018

Evaluation Of A Drug Delivery System Based On Cyclodextrins For Cancer Therapy, Caroline Mendes

Doctoral

Due to the side-effects caused by regular chemotherapy, the development of drug delivery systems that can specifically target cancer cells and deliver the therapeutic dose is required. In this study, a folate-derivative of β-cyclodextrin has been studied as a vehicle for targeting folate receptors (FR) and delivering the chemotherapeutic drug methotrexate (MTX). FRs can be considered key cell membrane targets since they are commonly over-expressed in cancer cells and play an important role in cancer development and progression. Cyclodextrins (CDs) are cyclic oligosaccharides with a unique structure that allows them to form inclusion complexes with guest molecules, increasing their aqueous ...


Synthesis Of 2,4,6-Substituted Pyrrolo[2,3-D]Pyrimidines As Potential Anticancer Agents, Si Yang Dec 2017

Synthesis Of 2,4,6-Substituted Pyrrolo[2,3-D]Pyrimidines As Potential Anticancer Agents, Si Yang

Electronic Theses and Dissertations

This thesis mainly focuses on the introduction of the background and work have been done in the areas of antifolates development, such as folate function, its three uptake mechanisms inside human cells, antifolates’ role in chemotherapy, et. al. In addition, the Structure-Activity-Relationship design rationale for the series of antifolates will also be discussed. Nevertheless, the details of synthesizing these pyrrolo[2,3-d]pyrimidines as potential antifolates have been described, including chemistry reviews on the pyrrolo[2,3-d]pyrimidine scaffold, and the challenges encountered and the solutions how to solve or improve in order to achieve better yield.


Combination Photodynamic Therapy And Chemotherapy For Temozolomide-Resistant Glioblastoma, Janel Kydd, Rahul Jadia, Prakash Rai May 2017

Combination Photodynamic Therapy And Chemotherapy For Temozolomide-Resistant Glioblastoma, Janel Kydd, Rahul Jadia, Prakash Rai

UMass Center for Clinical and Translational Science Research Retreat

Polymer based nanoparticles (NPs) are useful vehicles for drug therapy in treating glioblastoma because of their ideal characteristics such as small size, to cross the blood-brain barrier, and bind to overexpressed transferrin receptors via peptide conjugation and surface modification of NPs. The use of a photosensitizer drug such as verteporfin, or BPD, in combination with a repurposed drug, Cediranib (CED), prepared as a nanoparticle therapy will provide the medical field with new research on the possible ways to treat glioblastoma. BPD-CED-loaded NPs have the potential to induce cytotoxicity in glioblastoma cells by 1) remotely triggering BPD through photodynamic therapy by ...


Overcoming Innate And Acquired Therapy Resistance By Targeting Dna Repair In Human Cancer Cells, Mateusz Rytelewski Dec 2015

Overcoming Innate And Acquired Therapy Resistance By Targeting Dna Repair In Human Cancer Cells, Mateusz Rytelewski

Electronic Thesis and Dissertation Repository

Genomic instability and a high mutation rate lead to heterogeneity in human tumors. Mathematical modelling predicts that these characteristics promote acquired resistance to cytotoxic and targeted therapies, by increasing the likelihood that resistant subpopulations exist at the start of treatment (and promoting the accumulation of de novo resistance mutations during treatment). As a result, genome plasticity promotes increased fitness on the population level, but individual tumor cells must nonetheless maintain a level of DNA integrity that allows for continued survival, particularly in the context of DNA-damaging therapy (which DNA repair counteracts). Thus, DNA repair proteins are a source of innate ...


Synthesis And Application Of The Doxaz-Marcks Prodrug, Alla Balabanova Jan 2015

Synthesis And Application Of The Doxaz-Marcks Prodrug, Alla Balabanova

Undergraduate Honors Theses

Chemotherapeutic prodrugs have demonstrated success in killing cancer cells; however they also pose harm to healthy cells. The objective of this project was to synthesize an improved prodrug that is selectively activated only in the cancer microenvironment, thus minimally affecting healthy tissue. A photolabile linker was hypothesized to achieve said objective. The Yin group discovered that the MARCKS-ED peptide can localize to the exosome via curvature sensing and electrostatic interactions. In addition, the Koch group determined that Doxazolidine (Doxaz) is more cytotoxic than its clinical drug precursor. Also, no cancer cell lines have shown resistance to this anthracycline. Based on ...