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Full-Text Articles in Physical Sciences and Mathematics
Chyd1 Solution Phase Synthesis Optimization And The Development Of A Novel Human Growth Hormone Antagonist And Agonist, Philip Murray
Chyd1 Solution Phase Synthesis Optimization And The Development Of A Novel Human Growth Hormone Antagonist And Agonist, Philip Murray
USF Tampa Graduate Theses and Dissertations
Inhibiting protein-protein interactions to achieve a therapeutically desired effect has been a goal in the field of drug discovery for decades. Recently, advances in peptidomimetics have led researches to the use of cyclized peptides to achieve this goal. Cyclization of linear peptides restricts the number of conformations of the peptide, increasing the peptide's affinity to binding to the desired target. Cyclization also stabilizes the peptide, allowing the peptide to be resistant to proteases. This study explores the optimization of solution phase synthesis of an important integrin-mediated cell adhesion cyclic peptide for the therapeutic inhibition of multiple myeloma, cHYD1. cHYD1 was …
Design And Synthesis Of Beta-Hairpin Peptidomimetics For Modulating Integrin Mediated Cell Adhesion, Abeta Fibrillogenesis And P53-Mdm2 Protein-Protein Interactions, Priyesh Jain
USF Tampa Graduate Theses and Dissertations
Inhibiting therapeutically important protein-protein interactions has been a tremendous challenge for medicinal chemists. The folded 3D structures of peptides and proteins, mainly comprise secondary structural elements i.e α-helices and β-sheet have created an opportunity to design small molecules and peptidomimetic inhibitors of protein-protein interaction (PPI). Hence, information about the formation and stabilization of these secondary structures is vital for designing future drugs. In this dissertation, several cyclic beta-hairpin peptidomimetics that mimic the recognition surface have been designed and synthesized as inhibitors for different targets such as integrin mediated extracellular matrix -cell adhesion in multiple myeloma, p53-MDM2 PPI, amyloid beta fibrillogenesis …