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 7 of 7 for “"bivalent ligands"”.
-
Synthesis and Biological Evaluation of Coactivator Binding Inhibitors and Bivalent Ligands for the Estrogen Receptor
The synthesis of steroidal bivalent ligands for ER is also reported. Two estradiol molecules were connected through a phenylethynyl linkage with chemical tethers of varying composition and length. The binding properties of the bivalent ligands for ER were measured. Moderate relative binding …
-
Elucidating the role of the EGFR-family members in cell motility through the use of novel engineered bivalent ligands
… This thesis describes the use of engineered bivalent ligands to systematically manipulate receptor dimerization, perturb downstream signaling processes, and affect phenotypic outcomes. Results showed that biasing away from an EGFR-HER-2 with a bivalent ligand reduces cell motility …
-
Design, synthesis, and biochemical evaluation of three types of hexestrol-based probes for estrogen receptor: Fluorine-18 radiopharmaceuticals, bivalent ligands and diazirine photoaffinity reagents
… such as fluorine-18 radiopharmaceuticals, bivalent ligands, and affinity labels, provide information toward a better understanding of ER localization, structure, and function. We have prepared two fluorinated analogs of 2-oxohexestrol as potential diagnostic imaging agents for ER-responsive …
-
The synthesis of 5-HT2 receptor designed multiple ligands to investigate the role of the 5-HT2AR and the 5-HT2CR in cocaine addiction
… order to target these GPCR dimers and oligomers bivalent ligands have been synthesized. Previously synthesized bivalent ligands have demonstrated increased affinity and potency when compared to administration of the monomers. The aim of this project is to synthesis homodimeric 5-HT2A R …
-
Modulating cell behavior with engineered HER-receptor ligands
… dimer pairs. The canonical physiological ligands for the HER family receptors are monomeric, allowing occupied receptors to freely homodimerize or heterodimerize. The premise of this work is that engineered bivalent ligands can drive specific dimerization events to enhance or inhibit …
-
Protein-Protein Interactions with Serotonin G Protein Coupled Receptors: Novel Targets for Neurotherapeutics Drug Discovery
… the development of selective orthosteric ligands is challenging and has led to the loss of many promising therapeutic candidates from the drug development pipeline due to adverse events attributed to off-target effects. Therefore, alternative strategies to develop GPCR drugs with enhanced …
-
Engineering novel antibody-based molecules to probe the role of the immunoglobulin hinge and generate a potential cancer vaccine
… upper hinge lengths were generated. Rigid bivalent ligands or “molecular rulers” (dsNIP-DNA) comprising defined lengths of double stranded DNA with NIP covalently attached to both ends were produced. ELISA tests demonstrated that anti-NIP human IgG1 bound to dsNIP-DNA. Through employment of …