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.
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Showing 1 to 7 of 7 for “"Proton coupled folate transporter"”.
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The proton-coupled folate transporter: biology and therapeutic applications to cancer
<p>Folates are essential cofactors of tumor cell proliferation and survival required for nucleotide biosynthesis and amino acid metabolism. In cancer therapy, inhibition of folate-dependent metabolic pathways has been achieved through the use of antifolates. Unfortunately, the efficacy of many …
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Synthesis of novel 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as selective and potent anti-tumor agents
<p>In last few decades many folate analogs have been discovered and several compounds are successfully being used as anticancer agents. Methotrexate (MTX), pemetrexed (PMX), raltitrexed (RTX): are a few examples of classical antifolates that are currently in clinical use. Although these compounds …
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Sustained release nanoparticles containing acyclovir prodrugs for ocular herpes simplex keratitis and characterization of folate transport proteins in a corneal epithelial cell line
… increases the affinity of prodrug to the peptide transporter protein. Entrapment efficiency values of L-valine-L-valine-ACV and L-valine-D-valine-ACV were optimal with PLGA 75:25 and PLGA 65:35 polymers, respectively. In vitro release of prodrugs from nanoparticles exhibited a biphasic release …
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Design and Synthesis of Pyrimidine Based Fused Heterocyclics in the Potential Treatment of Cancer and Opportunistic Infection
… or resistant to this treatment. Dihydrofolate reductase (DHFR) is an essential enzyme that provides folate cofactor for DNA, RNA, and methionine biosynthesis. Hence, selectively inhibiting pjDHFR is an important strategy for effective treatment of infection by the pathogen. …
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Pyrrolo[2,3-d]pyrimidine Classical Antifolates for Targeted Cancer Chemotherapy- Applications of Bioisosteric and Regioisomeric Substitutions for Improved Tumor-Selectivity and Potency
… of resistance.</p> <p>Clinically used antifolates methotrexate (<strong>MTX</strong>; DHFR inhibitor), pemetrexed (<strong>PMX</strong>; TS and GARFTase inhibitor), pralatrexate (<strong>PTX</strong>; DHFR inhibitor), and raltitrexed (<strong>RTX</strong>; TS inhibitor), have two major …
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Target Based Design and Synthesis of Fused Pyrimidines in the Potential Treatment of Cancer and Opportunistic Infection
… selective <em>Pneumocystis jirovecii</em> dihydrofolate reductase (pjDHFR) inhibitors for pneumocystis pneumonia (PCP) infection; (b) inhibitors of microtubule polymerization and multiple receptor tyrosine kinase (RTK) for potential treatment of cancer; and (c) substrates for tumor-targeted …
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Classical Antifolates: Synthesis of 5-Substituted, 6-Substituted and 7-Substituted Pyrrolo[2,3-d]Pyrimidines as Targeted Anticancer Therapies
… research progress in the area of classical antifolates as the targeted anticancer therapies.</p><p> In this study, twelve series of classical 5-, 6- and 7-substituted pyrrolo[2, 3-d]pyrimidines were designed and synthesized. Extensive structure modifications of the pyrrolo[2, 3-d] pyrimidine …