Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
Results
Showing 1 to 12 of 12 for “"PCFT"”.
-
The proton-coupled folate transporter: biology and therapeutic applications to cancer
… (RFC) and proton-coupled folate transporter (PCFT). As PCFT is a folate-proton symporter with an acidic pH optimum, PCFT may provide a mechanism for targeting cytotoxic antifolates to tumors, based on their acidic microenvironments. To establish the feasibility of this approach, we …
-
Synthesis of novel 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as selective and potent anti-tumor agents
… (FRs) and/or Proton coupled folate transporter (PCFT). Because RFC is ubiquitous in the human body, the dose limiting toxicity is unavoidable for an antifolate if it is a substrate for RFC. To circumvent this challenge with antifolate chemotherapy, it is necessary to develop agents which are …
-
Approaches to modeling pathogen and natural organic matter removals in slow-rate biofilters
… or phenomenological colloidal filtration theory (pCFT), applies the 1937 Iwasaki solution to New England pilot scale E. coli observations. The derived pCFT was then calibrated through a series of experimental bench scale phases. Further pCFT validation came by way of a seamless application to …
-
Target Based Design and Synthesis of Fused Pyrimidines in the Potential Treatment of Cancer and Opportunistic Infection
… (RFC), Proton-Coupled Folate Transporter (PCFT) and/or Folate receptors (FR). Among several targeting strategies for cancer cells, selectively targeting through PCFT and FRs, over RFC have been successfully investigated. The next valid step in the field is to carry out a structure based …
-
Design and Synthesis of Pyrimidine Based Fused Heterocyclics in the Potential Treatment of Cancer and Opportunistic Infection
… β, and the proton-coupled folate transporter (PCFT). Among several targeting strategies for cancer cells, selectively targeting through PCFT and FRs, over RFC have been successfully investigated. To avoid dose-limiting toxicities, the next valid step in the field is to carry out a …
-
Pyrrolo[2,3-d]pyrimidine Classical Antifolates for Targeted Cancer Chemotherapy- Applications of Bioisosteric and Regioisomeric Substitutions for Improved Tumor-Selectivity and Potency
… etc.) and the proton-coupled folate transporter (PCFT) (ovarian and NSCLC). Our aim is to design classical antifolates for selective uptake by FRs and PCFT over RFC and inhibition of multiple folate metabolizing enzymes in their monoglutamate forms. Successful identification of such small molecule …
-
Classical Antifolates: Synthesis of 5-Substituted, 6-Substituted and 7-Substituted Pyrrolo[2,3-d]Pyrimidines as Targeted Anticancer Therapies
… to determine selective transport via FR or/and PCFT and tumor targeted antifolates with GARFTase or multiple folate metabolizing enzyme inhibition.</p><p> The design strategies employed include: variation of the side chain substitution position (5-, 6- and 7-substituted); variation of the side …
-
Sustained release nanoparticles containing acyclovir prodrugs for ocular herpes simplex keratitis and characterization of folate transport proteins in a corneal epithelial cell line
… (FR-α) and proton-coupled folate transporter (PCFT). This work demonstrated the functional and molecular presence of FR-α and PCFT in SIRC cells that can be utilized for enhanced uptake of folate conjugated nanoparticles and prodrugs. In a different study the differential expression of FR-α, …
-
Discovery of Pyrimidine-based Heterocycles as Single Agents With Combination Chemotherapy Potential And As Inhibitors Of Purine Nucleotide Biosynthesis For The Treatment of Cancer
… also reviews the synthesis of multi-transporter (PCFT and FR) selective 5-substituted pyrrolo[2, 3-<em>d</em>]pyrimidines as GARFTase inhibitors circumventing both dose-limiting toxicity and tumor resistance associated with most prescribed antitumor agents like pemetrexed.</p>
-
Folate: Friend or Foe? An investigation into the opposing roles of folate in glioma
… of the genes of interest; PTEN, FOLR1, RFC, PCFT, and MTHFR were analysed to determine differences between cell lines following treatment. The investigation showed that folic and folinic acid behaved differently depending on concentration used and the cell lines treated. Folic acid at 5 µg/ml …
-
Design and Synthesis of Pyrimidine Based Heterocycles as Potential Anti-cancer Agents with Combination Chemotherapeutic Potential or Targeted One Carbon Metabolism Inhibition and Anti-opportunistic Agents
… also reviews the synthesis of multi-transporter (PCFT and FR) selective 5-substituted pyrrolo[2,3-<em>d</em>]/[3,2-<em>d</em>]pyrimidines as targeted one-carbon metabolism enzymes (GARFTase/AICARFTase and/or SHMT2) inhibitors circumventing both dose-limiting toxicity and tumor resistance …
-
Synthesis of 2,4,6-Substituted Pyrrolo[2,3-d]pyrimidines as Potential Anticancer Agents
<p>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, <em>et. al</em>. In addition, the …