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 6 of 6 for “"Bivalent Ligand"”.
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DEVELOPMENT OF ANTAGONISTS TARGETING CHEMOKINE RECEPTOR CCR5 AND THE CHEMOKINE RECEPTOR CCR5 – MU OPIOID RECEPTOR HETERODIMER
… prostate cancer cell lines. In addition, a bivalent ligand containing both a mu opioid receptor (MOR) and a CCR5 antagonist pharmacophore was designed and synthesized in order to study the pharmacological profile of the putative CCR5-MOR heterodimer and its relation with NeuroAIDS. The …
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Advances in myotonic dystrophy type 1 drug discovery through design of novel ligands and mechanism establishment
… (Chapter 2) and a small library of dimeric ligands (Chapter 3) leading to an optimized bivalent ligand. These novel ligands target CUGexp RNA and are able to inhibit the CUGexp⋅MBNL1 interaction in cells that model DM1. In a DM1 cell model these ligands were found to disperse CUGexp …
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Elucidating the role of the EGFR-family members in cell motility through the use of novel engineered bivalent ligands
… are similar in structure; each contains a ligand binding domain, a transmembrane region, and a phosphotyrosine cytosolic domain. Upon ligand binding, each of the family members dimerizes in a homo- or heterotypic manner to initiate signaling cascades that influence migration and …
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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 …
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Design and Synthesis of Novel Benzodiazepines
Bivalent drug design is an efficient strategy for increasing potency and selectivity of many drugs. We devised a strategy to prepare agonist-benzodiazepine heterodimers that could simultaneously bind to agonist and BZD sites of the GABAAR. We synthesized a benzodiazepine-MPEG model compound that …
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New alkylpiperazines as 5-HT7R ligands
… sono state identificate differenti classi di ligandi ad alta affinità ma non selettivi. Nell’ultima decade, notevoli sforzi sono stati fatti per scoprire nuovi agenti selettivi e i derivati long-chain aril-piperazininici rappresentano una fra le classi più promettenti, in quanto mostrano …