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 20 of 21 for “"Cys-loop"”.
-
The identification of novel cys-loop receptor genes in Dirofilaria immitis
… – but anthelmintic resistance is emerging. Cys-loop ligand-gated ion channels are an untapped source for drug targets essential for nematode neurotransmission. This thesis presents the isolation and preliminary pharmacological characterization of three inhibitory D. immitis ion channels: …
-
Examination of intramolecular interactions between residues of the cys-loop GABA receptor Hco-UNC-49 from Haemonchus contortus
Haemonchus contortus is a parasitic nematode known to infect ruminant animals such as sheep, goats and cattle. Despite several different anthelmintic drugs available to control the spread of this infection, H. contortus has shown resistance to all of them. In order to combat the infection, a novel …
-
Investigation into the role of binding loop E on the function of the nematode cys-loop GABA receptor.
… objective, each amino acid residue in binding loop E was changed to a cysteine and analyzed via electrophysiology and the substituted cysteine accessibility method. It was found that of the 18 loop E mutants analyzed, His142, Ser144, Arg147, and Ser157, all played a role in channel activation …
-
Characterization of the ACC-1 Family of cys-loop ligand gated ion channels from the parasitic nematode Haemonchus contortus.
Nematode cys-loop ligand-gated ion channels (LGICs) have been extensively studied for decades because of their role in current anthelmintic action and potential as targets for future drugs. Many families of cys loop receptors have not yet been pharmacologically characterized in parasitic nematodes, …
-
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 …
-
Έκφραση μεταλλαγμένων τμημάτων του νικοτινικού υποδοχέα ακετυλοχολίνης και χρήση τους για την ανάπτυξη θεραπείας για τη μυασθένεια
… τους άκρο τη χαρακτηριστική κυστεϊνική θηλιά (Cys-loop) μεταξύ δύο συντηρημένων καταλοίπων κυστεΐνης, οι οποίες συνδέονται με δισουλφιδικό δεσμό. Οι νικοτινικοί υποδοχείς της ακετυλοχολίνης είναι μεγάλες διαμεμβρανικές πρωτεΐνες που αποτελούνται από πέντε ομόλογες υπομονάδες και χωρίζονται σε …
-
Influencia de campos electromagnéticos en las propiedades cinéticas de canales iónicos activados por neurotransmisores
… se encuentra la llamada familia de receptores Cys-loop que incluye a los receptores excitatorios nicotínico (AChR), de serotonina 5-HT3 y receptores inhibitorios GABAA y de glicina. Desde hace un tiempo, se ha discutido la posibilidad de que los campos magnéticos estáticos (CME) o …
-
Isolation and partial characterization of three acetylcholine-gated chloride channels in Haemonchus contortus
… drug resistance in H. contortus populations. The Cys-loop superfamily of ligand gated ion channels are well recognized as critical drug targets for many invertebrate specific compounds. With the rise in resistance seen worldwide to existing anthelmintics, novel drug targets must be identified so …
-
The heteromeric 5-HT3A/B receptor:the effect of 5-HT3B subunits on receptor structure and ligand recognition
The 5-HT3 receptors are members of the cys-loop family of ligand-gated ion channels. Two functional subtypes are known, the homomeric 5HT3A and the heteromeric 5HT3A/B receptors, which exhibit distinct biophysical characteristics but are difficult to differentiate pharmacologically. Atomic force …
-
Isolation and partial characterization of three members of the GGR-1 family in the parasitic nematode Haemonchus contortus
… an urgent need for novel anti-parasitic drugs. Cys-loop ligand gated ion channels have been recognized as important invertebrate specific drug targets. However, specific targets must be identified and characterized prior to drug development. This thesis describes the identification and partial …
-
Structure-function studies of agonist binding to the muscle-type nicotinic acetylcholine receptor and the development of a trifunctional non-competitive antagonist suitable for activity-dependent profiling
… junction. It is the archetype of the Cys-Loop superfamily of receptors and a prototypic allosteric protein. The muscle-type AChR has two distinct transmitter binding sites found in the extracellular ligand-binding domain. When acetylcholine binds these sites, a series of still …
-
The Role of Transmembrane Domain Helix-Helix Interactions in the Function of Pentameric Ligand-Gated Ion Channels
… interactions between the M4 C-terminus and the Cys-loop of the agonist-binding domain, with such interactions promoting coupling between the agonist site and channel gate. The first part of my thesis indirectly tests this hypothesis by exploring the effects of membrane hydrophobic thickness on …
-
Structural and molecular determinants of the sensitivity of alpha4beta2 nicotinic acetylcholine receptors to the allosteric ligand desformylflustrabromine
… The post-M4 region (C-terminal) and the Cys loop residues F167 and F170 of the α4 subunit play central roles in transducing dFBr binding to potentiation of the ACh responses of the α4β2 nAChR. Whilst the residues that contribute to the dFBr binding site in the α4 are conserved across all …
-
Structural and molecular determinants of the sensitivity of alpha4beta2 nicotinic acetylcholine receptors to the allosteric ligand desformylflustrabromine
… The post-M4 region (C-termina1) and the Cys loop residues FI 67 and F170 of the a4 subunit play central roles in transducing dFBr binding to potentiation of the ACh responses of the a4P2 nAChR. Whilst the residues that contribute to the dFBr binding site in the a4 are conserved across all …
-
Charakterisierung des 5-HT<sub>3B</sub>-Promotors der Ratte vor dem Hintergrund eines mit Chemotherapie-induziertem Erbrechen assoziierten Polymorphismus
… Typ 3 (5-HT3), einem Ionenkanal aus der Cys-loop-Rezeptorfamilie. Das Gen HTR3B kodiert für 5-HT3B. Der -100_-102delAAG-Polymorphismus im HTR3B-Promotor kann die HTR3B-Promotoraktivität beeinflussen und wurde mit Häufigkeit und Schweregrad von Chemotherapie-induzierter Übelkeit und …
-
An examination of interacting residues in the GABA-gated ion channel UNC-49 within the parasitic nematode Haemonchus contortus
Haemonchus contortus is a blood-feeding parasitic nematode that infects ruminant animals around the world, including those with significant economic importance such as cattle, sheep, and goats. UNC-49 is a GABA-gated chloride channel found to be exclusive to nematodes which could be a viable future …
-
A molecular characterization of agonists that bind to Hco-UNC-49, a GABA-gated chloride channel from Haemonchus contortus
Haemonchus contortus is a blood feeding parasitic nematode infecting ruminants causing anemia and poor health at great economic cost. The ability to pharmaceutically control infection has been challenged by the rapid development and spread of drug resistance. The discovery of new targets is …
-
The Lipid-Facing M4 Helix of α4β2 nACh and 5-HT3A Receptors
Pentameric ligand-gated ion channels (pLGICs) are expressed throughout the human nervous system, and contribute to a range of muscle, gut, and neurological functions. Elucidating their mechanism of action and how it might be modulated would improve our understanding of the nervous system, and …
-
Development and application of quantitative ligand-binding studies to elucidate mechanistic aspects of pentameric ligand-gated ion channels
Submission published under a 24 month embargo labeled 'Closed Access', the embargo will last until 2025-12-01
-
Modulación molecular de la función del receptor neuronal α7
… postsinápticos. Los receptores de la familia cys-loop, que incluye al receptor nicotínico de acetilcolina (nAChR, nicotinic acetylcholine receptor), son miembros de la superfamilia de los canales pentaméricos activados por ligando (pLGICs, pentameric ligand-gated ion channels). Están formados …
Page 1 of 2