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Full-Text Articles in Laboratory and Basic Science Research

Kinetic And Dynamic Insights Into The Substrate Interactions And Catalysis Of Factor Inhibiting Hif-1 (Fih-1), Cristina B. Martin Jul 2016

Kinetic And Dynamic Insights Into The Substrate Interactions And Catalysis Of Factor Inhibiting Hif-1 (Fih-1), Cristina B. Martin

Doctoral Dissertations

inhibiting HIF-1 (FIH-1) modulates the master regulator of hypoxia sensing, hypoxia inducible factor-1 (HIF-1), by transcriptional repression making it an attractive potential target for treatment of hypoxia-related diseases. Given that similar enzymes are present within the cell and that they have other important physiological roles, defining the therapeutic window by which it can be selectively targeted becomes an issue. Consequently, it’s necessary to have a deeper understanding of the substrate interactions in FIH-1 that contributes to catalysis as this is one avenue that can be explored for future therapeutic investigations. The overall goal of this dissertation is to gain kinetic …


Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego Amado Torres Aug 2014

Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego Amado Torres

Doctoral Dissertations

Proteins have the capacity to bind specific sets of compounds known as ligands, these are small molecules with a recurrent theme in their molecular design that is a characteristic exploited here to (i) identify particular affinities of small molecules for proteins with the aim of using them as ligands, inhibitors, or targeting moieties in more complex systems by means of a methodology that screens small molecules based on protein affinity; (ii) decorate a self-assembling supramolecular system at different positions, making it responsive to a complementary protein with the aim of exploring differences in disassembly and sensitivity of the release of …