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 20 of 911 for “"agonist"”.
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Molecular Signaling and Agonist Discovery for GPR52
… GPR52 activation, and discovery of biased GPR52 agonists. GPR52 was determined to couple to both Gs and Golf to increase cAMP signaling, with constitutive activity driven by Gs. GPR52 is co-expressed with D2 dopamine receptors, and in vitro studies show crosstalk at the level of adenylyl cyclase …
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Collagen Anchoring Agonist Antibodies for Cancer Immunotherapy
… in preclinical mouse models is the use of agonist antibodies targeting costimulatory, or activating, receptors on effector immune cells, particularly CD8⁺ T cells. Translation of these therapeutics into the clinic has been hampered by severe, sometimes fatal, on-target, off-tumor …
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Agonist-Induced Conformational Changes In The Nmda Receptor
<p>NMDA receptors are ligand-gated ion channels that mediate a number of physiological and pathological phenomena within the mammalian central nervous system. Under the typical course of activation, these receptors bind to glycine and glutamate molecules and undergo a series of conformational …
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Engineered Anti-CD40 Agonist Antibody for Cancer Vaccine Delivery
… responses. We synthesized an anti-mouse CD40 agonistic–monovalent streptavidin fusion antibody (αCD40-mSAs), which enables targeted delivery of biotinylated neoantigen peptides to APCs in draining lymph nodes (dLNs). αCD40-mSAs were validated for mSA expression and demonstrated strong binding …
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Cd4 T Cell Activation And Ox40 Agonist Immunotherapy In Tuberculosis
… A short course of immunotherapy with an agonist monoclonal antibody targeting OX40+ cells during early infection transiently expanded CD4 T cell numbers and shifted their phenotype towards parenchymal protective cells, which decreased the lung bacterial burden and extended host survival, …
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ASSESSMENT OF NEUROTENSIN RECEPTOR AGONIST EFFECTS ON FEAR-POTENTIATED STARTLE
… administration of the NTS<sub>1</sub> receptor agonist PD149163 has exhibited anxiolytic effects in male rats. The present study sought to further evaluate the potential anxiolytic effects of PD149163 by assessing this compound in both male and female C57BL/J6 mice using the fear-potentiated …
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The Rac-GEF P-Rex1 Regulates Agonist-Induced GPCR Trafficking
… P-Rex overexpression blocks the first step of agonist-induced S1PR1 endocytosis - receptor phosphorylation - independently of catalytic Rac-GEF activity (unpublished). My PhD builds on this previous research providing a comprehensive insight into the role of P-Rex1 in GPCR trafficking. Upon …
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Searching for structural determinants of agonist selectivity in nicotinic acetylcholine receptors
… (Nic). Activation of these receptors by partial agonists is considered as a valid strategy to intervene therapeutically in the aforementioned dysfunctions. For clinical scenarios such as Nic addiction receptor subtype-specificity may increase clinical efficacy by decreasing off-target effects. …
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Characterization of Novel Liver X Receptor Inverse Agonist in Breast Cancers
… Moreover, LXR inhibition using the inverse agonist SR9243 has been shown to disrupt glycolysis, de novo lipogenesis, and induce antitumor immunity. In our lab, we discovered another cancer-specific LXR inverse agonist, GAC0001E5 (1E5), in pancreatic ductal adenocarcinoma (PDAC). Treatment …
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Das Antiepileptikum Gabapentin (Neurontin) als Agonist an ATP-sensitiven Kalium-Kanälen
… durch Glibenclamid, einem Kalium-ATP-Kanal-Antagonist aufgehoben. Ebenso wie Gabapentin hemmt auch Pinazidil, ein Kalium-ATP-Kanal-Öffner, die Freisetzung von [3H]-Noradrenalin. Dies bietet einen Hinweis darauf, daß Gabapentin seine Wirkung über die Modulation von Kalium-ATP-Kanälen entfaltet. …
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Tumor-Specific STING Agonist Synthesis via a Two-Component Prodrug System
… tumor-specific or conditionally activated STING agonists for enhanced safety and efficacy. Herein, we explored an unconventional prodrug activation strategy for on-tumor synthesis of a potent agonist. Starting from the scaffold of MSA2, a non-CDN synthetic agonist that requires non-covalent …
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Coordination of lower limb movement utilizing the agonist-antagonist myoneural interface
The agonist-antagonist myoneural interface is a novel surgical construct that shows promise as a method of providing persons with amputation proprioceptive sensation of movement and force. This thesis aims to quantify the volitional coordination capabilities of the agonist- antagonist myoneural …
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Design and evaluation of a biomimetic agonist-antagonist active knee prosthesis
… actuators positioned in parallel in an agonist-antagonist configuration. This investigation hypothesizes that the biomimetic active-knee prosthesis, with a variable impedance control, can improve unilateral transfemoral amputee locomotion in level-ground walking, reducing the metabolic …
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Basal and agonist activated calcium sensitization pathways in murine gastrointestinal smooth muscles
… smooth muscle field; does exogenously applied agonist in the myobath and neural release of agonist induce similar Ca2+ sensitization signaling changes in GI smooth muscle. In carrying out these projects, contractions of GI smooth muscles were determined using standard myobath - isometric force …
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Regulation of the cGAS-STING Pathway: Non-Agonist Activation and Cellular Trafficking
… In the settings of cancer immunotherapy, STING agonists induce strong anti-tumor immunity in preclinical models and synergize with radiation, chemotherapy, and immune checkpoint inhibitor therapy. Evaluation of STING agonists in human clinical trials is ongoing, although early results did not …
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A Novel Phytoestrogen that Acts as an Agonist for Human Estrogen Receptors.
Estrogen is the natural agonist of the estrogen receptor (ER). However, certain plant-derived compounds or phytoestrogens have been identified that mimic estrogens and act as agonists and/or antagonists of ERs, depending on subtype and target tissue. Understanding how phytoestrogens interact with …
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ANTIDEPRESSANT EFFECTS OF THE NTS1 AGONIST PD149163 IN THE FORCED SWIM TEST
… of the neurotensin NTS<sub>1</sub> receptor agonist PD149163 and the tricyclic antidepressant drug imipramine on immobility in the forced swim test and on locomotor activity in an open field in mice. PD149163 decreased the total time spent immobile at doses of 0.1 mg/kg and 1.0 mg/kg, without …
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Acute effects of dynamic stretching on flexibility and agonist-antagonist muscle activity
… was to delineate the effects of ADS on AROM and agonist-antagonist mean and peak EMG. The ADS protocol involved three sets of ten repetitions of leg kicks while in the supine position with the pelvis and contralateral limb fixed in extension. Participants moved the leg at the hip in a kicking …
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