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 11 of 11 for “"Molecular pharmacology"”.
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Synthesis and Molecular Pharmacology of the Diazonamides
Diazonamide A is structurally novel, marine-derived natural product potently capable of inhibiting the growth of the cultured human cancer cell lines in vitro. Following the eassignment of diazonamide structure in 2001, we began a program to understand the compound's cellular mode of action. I …
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Molecular pharmacology of an insect GABA receptor
Cys-loop receptors are ligand-gated ion channels that are involved in fast synaptic neurotransmission in the central and peripheral nervous system. The Cys-loop receptor RDL (‘resistant to dieldrin’) is a GABA-gated chloride channel from Drosophila melanogaster and is a major target site for …
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Functional cell biology and molecular pharmacology of ATP sensitive potassium channels.
Adenosine triphosphate (ATP) sensitive potassium channels (K ATP) transduce changes in cellular metabolism into changes in membrane potential. Activation of K ATP channels causes vascular smooth muscle to hyperpolarize. This leads to a relaxation of the pre-contracted muscle. Inhibition of K ATP …
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Investigating the molecular pharmacology of class A and B G protein-coupled receptors
G protein-coupled receptors (GPCRs) possess an inherent ability to bind to an extremely diverse range of ligands and activate multiple downstream signalling pathways. It is becomingly increasingly evident, however, that for many GPCRs, the exact downstream signalling cascade(s), and the extent of …
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FUNCTIONAL SELECTIVITY DOWNSTREAM OF Gαi/o-COUPLED RECEPTORS
… symptoms is minimal. In this work we studied the molecular pharmacology of aripiprazole and showed that the compound displays ligand bias for modulation of G proteins, being a partial agonist for Gαi/o and a robust antagonist for Gβγ signaling. We have also examined the activation of immediate …
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Chemoligand therapy for metastatic castration-resistant prostate cancer
… radiopharmaceutical-guided drug development and molecular pharmacology <em>in vitro</em>, I discovered a chemoligand with high affinity to PSMA (<em>K</em><sub>d </sub>= 2.5 [1.5-3.9] nM) that disrupts the mitotic spindle, causes erratic mitosis, and induces cell and clonal death. Image-guided …
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Characterisation of novel alpha1-adrenoceptor ligands
… design, structure-activity relationship, and molecular pharmacology methods were used to identify α1A-AR subtype selective compounds with reduced 5-HT1A-R off-target affinity. In silico database screening identified 2 structurally novel compounds with nanomolar affinity for the α1A-AR, and 4 …
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COMBINATORIAL MOLECULAR PHARMACOLOGICAL AND PRECLINICAL STUDIES OF AN EPIGENETIC ANTICANCER DRUG, 3-DEAZANEPLANOCIN A, IN RATS
… support that DZNep not only can serve as a molecular pharmacological tool to probe the complex interaction between epigenetic events but also hopefully become a potential chemotherapeutic agent for the clinical application.
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Investigation into the Bronchoprotective and Anti-inflammatory Properties of RGS2
The clinical management of asthma involves treatment with inhaled corticosteroids (ICS) and long-acting β2-adrenoceptor agonists (LABAs). Regulator of G-protein signalling (RGS) 2 inhibits signalling from Gq protein-coupled receptors. In humans, combinations of a glucocorticoid and a LABA …
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Novel Insights into CB1 Receptor Signaling and the Anabolic Role of Cannabinoid Receptors in Bone
… in osteoblastic cells to gain insights into molecular pathways that may help to explain the effects of the endocannabinoid system (ECS) in bone development. Our data was generated by running time course experiments with MC3T3-E1 cells under the influence of SR141716A, SR144528 or both in …