Log in

Relevant bibliographies by topics / Allosteric modulators / Dissertations / Theses

To see the other types of publications on this topic, follow the link: Allosteric modulators.

Dissertations / Theses on the topic 'Allosteric modulators'

Author: Grafiati

Published: 4 June 2021

Last updated: 26 July 2025

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles

Select a source type:

Consult the top 50 dissertations / theses for your research on the topic 'Allosteric modulators.'

Next to every source in the list of references, there is an 'Add to bibliography' button. Press on it, and we will generate automatically the bibliographic reference to the chosen work in the citation style you need: APA, MLA, Harvard, Chicago, Vancouver, etc.

You can also download the full text of the academic publication as pdf and read online its abstract whenever available in the metadata.

Browse dissertations / theses on a wide variety of disciplines and organise your bibliography correctly.

1

MACUT, HELENA. "DEVELOPMENT OF ALLOSTERIC PFKFB3 PHOSPHATASE MODULATORS." Doctoral thesis, Università degli Studi di Milano, 2019. http://hdl.handle.net/2434/644064.

Full text

Abstract:

Cardiovascular disease is a severe health problem, especially in the Western world. Its primary cause is atherosclerosis, which is characterized by the arterial wall thickening. Modern therapeutic strategies have restricted efficacy and the mortality still remains high. Current research has supported the idea of targeting dysregulated endothelial cell (EC) metabolism as a novel therapeutic strategy. In the scope of this PhD research work, we aim to further explore the possibilities for an improved treatment of this life threatening disease. EC glycolytic flux is up-regulated during angiogene

APA, Harvard, Vancouver, ISO, and other styles

2

Dhankher, P. "Synthesis of novel allosteric agonists and allosteric modulators for nicotinic acetylcholine receptors." Thesis, University College London (University of London), 2013. http://discovery.ucl.ac.uk/1417083/.

Full text

Abstract:

In healthy individuals, the α7 and α4β2 nAChRs are concentrated in regions of the brain involved with learning, cognition and memory, which are relevant to diseases such as Alzheimer’s disease. Hence, these receptors have become significant from a pharmacological and drug discovery perspective. The tetrahydroquinoline compound 4BP-TQS has been reported to act as a potent allosteric agonist on the α7 nAChR. The natural product desformylflustrabromine is able to act as a positive allosteric modulator (PAM) on the α4β2 nAChR. This thesis describes the development of synthetic routes directed towa

APA, Harvard, Vancouver, ISO, and other styles

3

Alwassil, Osama. "Small Molecules as Negative Allosteric Modulators of Alpha7 nAChRs." VCU Scholars Compass, 2012. http://scholarscompass.vcu.edu/etd/2829.

Full text

Abstract:

Alpha7 Neuronal nicotinic acetylcholine receptors (nAChRs) are involved in essential physiological functions and play a role in disorders such as Alzheimer’s disease. MD-354 (3-chlorophenylguanidine; 21), the first small–molecule negative allosteric modulator (NAM) at alpha7 nAChRs, served as a lead in developing structure–activity relationships for NAMs at a7 nAChRs. MD-354 (21) also binds at 5-HT3 receptors. Analogs of MD-354 with structural features detrimental to 5-HT3 receptor affinity were evaluated in patch-clamp recordings and an aniline N-methyl analog resulted in a more potent and se

APA, Harvard, Vancouver, ISO, and other styles

4

Alwassil, Osama I. "Elaboration and Design of α7 nAChR Negative Allosteric Modulators". VCU Scholars Compass, 2015. http://scholarscompass.vcu.edu/etd/3902.

Full text

Abstract:

α7 Neuronal nicotinic acetylcholine receptors are one of two major classes of receptors responsible for cholinergic neurotransmission in the central nervous system. The existence of α7 neuronal nAChRs in different regions of the nervous system suggests their involvement in certain essential physiological functions as well as in disorders such as Alzheimer’s disease (AD), drug dependence, and depression. This project was aimed toward the discovery and development of small–molecule arylguanidines that modulate α7 nAChR function with improved subtype-selectivity through an allosteric approach. Id

APA, Harvard, Vancouver, ISO, and other styles

5

Myerson, Richard James. "The development of novel allosteric modulators of the 5-HT3 receptor." Thesis, University of Birmingham, 2017. http://etheses.bham.ac.uk//id/eprint/7657/.

Full text

Abstract:

This thesis reports the Structure Activity Relationship study that was performed upon the 5-substituted-indole core as a means to identify Negative Allosteric Modulators of the human 5-HT3A receptor for the development of potential drugs for the treatment of IBS-d. Herein is reported the successful identification of a PAM to NAM switch and three novel NAMs which provide the basis for further study into the treatment of IBS-d and insight into the identity of the allosteric site of the human 5-HT3A receptor. The design, synthesis and testing of a novel fluorescent analogue of the orthosteric ant

APA, Harvard, Vancouver, ISO, and other styles

6

Jackson, Doris Clark. "Characterization of Neuronal Nicotinic Acetylcholine Receptors and their Positive Allosteric Modulators." BYU ScholarsArchive, 2017. https://scholarsarchive.byu.edu/etd/6856.

Full text

Abstract:

Neuronal nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels that are necessary in memory and cognition. They are pentameric and consist of Î± and Î² subunits. They are most commonly heteromeric but, can sometimes be homomeric. nAChRs are activated by many ligands including nicotine (exogenous) and acetylcholine (endogenous).nAChRs are located on hippocampal interneurons. The interneurons, although sparse, control the synchronous firing of the pyramidal cells. However, the hippocampal interneuron structure and function is quite diverse and not fully characterized. Therefor

APA, Harvard, Vancouver, ISO, and other styles

7

Abdelrahman, Mostafa Hamed. "Design, synthesis and SAR of novel allosteric modulators of the Cannabinoid CBI receptor." Thesis, University of Aberdeen, 2010. http://digitool.abdn.ac.uk:80/webclient/DeliveryManager?pid=159203.

Full text

Abstract:

We report on the design, synthesis, and structure activity relationship studies of novel Org 27569 analogues as potential allosteric modulators of the CB1 receptors. We also investigated by computer modelling the possible location of the allosteric site on CB1 and the binding confirmation of the allosteric ligands. Docking of the synthesised molecules is also performed and the results are compared to the results of the biological bioassays. The synthesis of non-fused indole analogues of Org 27569 is described. These analogues were systematically varied to study the importance of key functional

APA, Harvard, Vancouver, ISO, and other styles

8

Gómez, Santacana Xavier. "Design, synthesis and characterisation of photoswitchable allosteric modulators of metabotropic glutamate receptors." Doctoral thesis, Universitat de Barcelona, 2016. http://hdl.handle.net/10803/399789.

Full text

Abstract:

Metabotropic glutamate receptors (mGlu receptors) are class C GPCRs widely distributed through the CNS and considered pharmacological targets for neurologic disorders, such as neuropathic pain and Parkinson’s disease, between others. Classical allosteric modulators receptors might be useful to treat these disorders, but they the control over of the compound, once it is administered, is lost. Photoswitchable allosteric modulators have an azo-‐moiety in their chemical scaffold and might offer a powerful alternative to these classical drugs, since their pharmacological activity can be “switched

APA, Harvard, Vancouver, ISO, and other styles

9

Pagare, Piyusha P. "RATIONAL DESIGN OF ALLOSTERIC MODULATORS OF HEMOGLOBIN AS DUAL ACTING ANTISICKLING AGENTS." VCU Scholars Compass, 2018. https://scholarscompass.vcu.edu/etd/5451.

Full text

Abstract:

Intracellular polymerization of deoxygenated sickle hemoglobin (Hb S) remains the principal cause of the pathophysiology associated with sickle cell disease (SCD). Naturally occurring and synthetic allosteric effectors of hemoglobin (AEH) have been investigated as potential therapeutic agents for the treatment of SCD. Several aromatic aldehydes, including vanillin, have been studied previously as AEHs for their antisickling activities. Specifically, these compounds form Schiff- base adduct with Hb to stabilize the oxygenated (R) state, increase Hb affinity for O2 and concomitantly prevent the

APA, Harvard, Vancouver, ISO, and other styles

10

Young, G. T. "Molecular characterisation of nicotinic acetylcholine receptor subtypes : interactions with agonists and allosteric modulators." Thesis, University College London (University of London), 2009. http://discovery.ucl.ac.uk/17315/.

Full text

Abstract:

Nicotinic acetylcholine receptors (nAChRs) are members of the ligand-gated ion channel family. They are also members of the sub-family of Cys-loop ligandgated ion channels, which includes closely related receptors for the neurotransmitters γ-aminobutyric acid (GABA), glycine, and 5- hydroxytryptamine (serotonin). There is a wealth of evidence demonstrating that nAChRs are involved in mediating fast excitatory transmission, and also that they modulate the release of other neurotransmitters. They have been implicated in several neurological disorders such as Alzheimer’s disease, Parkinson’s dise

APA, Harvard, Vancouver, ISO, and other styles

11

Jain, Atul. "Positive Allosteric Modulators of Alpha4Beta2 Neuronal Nicotinic Receptors: Synthesis and In vitro Studies." VCU Scholars Compass, 2013. http://scholarscompass.vcu.edu/etd/2953.

Full text

Abstract:

des-Formylflustrabromine (dFBr), isolated from the marine organism Flustra foliacea, is the first selective, positive allosteric modulator (PAM) of α4β2 nicotinic acetylcholine receptors that potentiates the action of the neurotransmitter acetylcholine (ACh). Most agonists for this receptor population are not selective and can activate other nACh receptors. A selective PAM, which activates α4β2 nACh receptors only in the presence of ACh, might find application in the treatment of of various neurological diseases such as Alzheimer’s disease or autism. dFBr was examined and found to produce a bi

APA, Harvard, Vancouver, ISO, and other styles

12

Blgacim, Nuria. "Molecular Control of the δ-opioid Receptor Signaling and Functional Selectivity by Sodium". Thesis, Université d'Ottawa / University of Ottawa, 2018. http://hdl.handle.net/10393/37806.

Full text

Abstract:

Accumulating evidence suggests a prominent role of the arrestin-dependent signaling pathway in triggering most of the deleterious side effects observed using δ-OR targeting drugs. Numerous small molecules targeting the δ-OR receptors have been developed but their pharmacological properties, including their functional selectivity, have been poorly characterized. The absence of functionally selective opioid drugs, and the lack of knowledge of the pharmacological profile and signaling properties of the δ-OR receptor, limits its therapeutic exploitation. The development of functionally selective m

APA, Harvard, Vancouver, ISO, and other styles

13

Fish, Eric W. "GABAA positive modulators, corticosterone, and schedule heightened aggression in mice /." Thesis, Connect to Dissertations & Theses @ Tufts University, 2003.

Find full text

Abstract:

Thesis (Ph. D.)--Tufts University, 2003.<br>Advisers: Klaus Miczek; Joe DeBold. Submitted to the Dept. of Psychology. In title, GABAA is spelled GABA with a subscript A. Includes bibliographical references (leaves 146-183). Access restricted to members of the Tufts University community. Also available via the World Wide Web;

APA, Harvard, Vancouver, ISO, and other styles

14

Henderson, Brandon J. "Discovery and Characterization of Selective Negative Allosteric Modulators of Human α4β2 Neuronal Nicotinic Receptors". The Ohio State University, 2011. http://rave.ohiolink.edu/etdc/view?acc_num=osu1307647472.

Full text

APA, Harvard, Vancouver, ISO, and other styles

15

Orfali, Razan. "SK Channel Modulators as Drug Candidates and Pharmacological Tools." Chapman University Digital Commons, 2018. https://digitalcommons.chapman.edu/pharmaceutical_sciences_theses/1.

Full text

Abstract:

The small- and intermediate-conductance Ca2+ activated K + (SK/IK) channels play a fundamental role in the regulation of neurons in the central nervous system. In animal models, SK/IK channel positive modulators have been shown to be effective in reducing the symptoms of neurological diseases such as ataxia. Ataxia is a lethal neurological rare disease characterized by lack of balance and incoordination of muscle movements, often as a result of cerebellar or spinocerebellar neurodegeneration. SK/IK channel modulators have been developed over the past few decades. Currently available modulators

APA, Harvard, Vancouver, ISO, and other styles

16

Ring, Joshua Roderick. "SYNTHETIC AROMATIC AGMATINE ANALOGS AS ALLOSTERIC MODULATORS OF THE N-METHYL-D-ASPARTATE (NMDA) RECEPTOR CHANNEL." UKnowledge, 2006. http://uknowledge.uky.edu/gradschool_diss/413.

Full text

Abstract:

The N-methyl-D-aspartate (NMDA) receptors are highly regulated ligand-gated ion channels, which are affected by many substrates. Overactivation of the NMDA receptor can lead to hyperexcitability and a number of neurotoxic effects and neurological diseases. Agmatine has been demonstrated to act allosterically as an inhibitory modulator at the polyamine recognition sites of the NMDA receptor complex. The present study synthesized and evaluated a library of agmatine analogs for their ability to displace tritiated MK-801 from NMDARs in P2 membrane preparations from rat brains at ligand concentrati

APA, Harvard, Vancouver, ISO, and other styles

17

D'Oyley, J. M. "Synthesis of five-membered heterocycles : novel allosteric modulators for nicotinic receptors and new gold-catalysed reactions." Thesis, University College London (University of London), 2014. http://discovery.ucl.ac.uk/1455536/.

Full text

Abstract:

The Drug Discovery project is centred on the design, synthesis and characterisation of novel positive allosteric modulators (PAMs) for α7 nicotinic receptors (nAChR). These receptors are widely found in the central and peripheral nervous systems and are involved in a range of physiological processes. They are active targets for the treatment of pain as well as psychiatric and neurodegenerative disorders. Nicotinic receptors are ion channels which open and allow ions to flow in or out of the neuron upon binding of an agonist. Positive allosteric modulators (PAM) enhance the receptor’s response

APA, Harvard, Vancouver, ISO, and other styles

18

Freitas, Kelen. "THE ANTINOCICEPTIVE EFFECTS OF ALPHA 7 NICOTINIC ACETYLCHOLINE RECEPTOR POSITIVE ALLOSTERIC MODULATORS IN DIFFERENT ANIMAL PAIN MODELS." VCU Scholars Compass, 2012. http://scholarscompass.vcu.edu/etd/2827.

Full text

Abstract:

The α7 nicotinic acetylcholine receptor (nAChR) subtype is abundantly expressed in the central nervous system (CNS) and in the periphery. Positive allosteric modulators (PAMs) of the α7 increase the response to an agonist and are divided into two types depending on whether they also decrease desensitization of the receptor (type II) or not (type I). Therefore, this study aims to investigate whether the enhancement of endogenous α7 nAChR function will result in a beneficial effect in nociceptive, inflammatory and chronic neuropathic pain models. While NS1738 and PNU-120596 were not active to re

APA, Harvard, Vancouver, ISO, and other styles

19

Luo, Yujia. "Analgesic Effect of Nicotine and Exploration of Binding Sites for α4β2 Nicotinic Acetylcholine Receptor Positive Allosteric Modulators". Thesis, The University of Sydney, 2023. https://hdl.handle.net/2123/30000.

Full text

Abstract:

Pain is a leading cause of the global burden of disease and disability. Nicotinic acetylcholine receptors (nAChRs), especially the α4β2 subtype, are widely expressed throughout the central nervous system (CNS) and peripheral nervous system (PNS), making them critical analgesic targets for the development of novel drugs. In the early part of this thesis, the analgesic effects of nicotine were quantified through meta-analysis. Sixteen eligible articles, including five studies on pain tolerance (n = 210), five studies on pain threshold (n = 210), and 11 studies on pain scores (n = 1,148) were inc

APA, Harvard, Vancouver, ISO, and other styles

20

Carper, Daniel Jay. "Total Synthesis of Ceratamine A & B and Synthesis of Negative Allosteric Modulators of Neuronal Nicotinic Acetylcholine Receptors." The Ohio State University, 2010. http://rave.ohiolink.edu/etdc/view?acc_num=osu1282788134.

Full text

APA, Harvard, Vancouver, ISO, and other styles

21

Taylor, Lee. "Positive allosteric modulators of the strychnine sensitive glycine receptor : a new concept in the treatment of chronic pain." Thesis, University of Liverpool, 2014. http://livrepository.liverpool.ac.uk/2011359/.

Full text

Abstract:

Chronic pain is a global medical-health problem. It is estimated that approximately 20% of the adult population suffer from some form of chronic pain. Along with the physical and emotional burden that living with chronic pain brings to the individual, there is also a huge socio-economic cost implication currently estimated at more than €200 million per annum in Europe and at over $150 million in the USA. Unfortunately, because of a lack of efficacious treatments, chronic pain is poorly managed. Current therapies for chronic pain act upon well-established targets and have been shown not only to

APA, Harvard, Vancouver, ISO, and other styles

22

Bortz, David Michael. "Positive Allosteric Modulators of the Alpha7 Nicotinic Acetylcholine Receptor Potentiate Glutamate in Prefrontal Cortex: In Vivo Evidence for a Novel Class of Schizophrenia Treatments." The Ohio State University, 2015. http://rave.ohiolink.edu/etdc/view?acc_num=osu1429111729.

Full text

APA, Harvard, Vancouver, ISO, and other styles

23

Wylde, Elinor. "Drug metabolism and pharmacokinetics in the lead optimisation of novel positive allosteric modulators of α1 strychnine sensitive glycine receptors". Thesis, University of Liverpool, 2015. http://livrepository.liverpool.ac.uk/2048099/.

Full text

Abstract:

Chronic pain is a condition that is thought to affect roughly 8 million people in the UK. It is classified as pain that persists for more than 6 months. Chronic pain is commonly associated with depression, insomnia, anxiety and poor quality of life. Many treatments for chronic pain are accompanied by numerous debilitating side-effects, this in combination with insufficient pain relief means that approximately 50% of patients will discontinue their treatment. Most sufferers choose to live with the pain rather than deal with numerous adverse-effects. There is a great need for new therapeutics th

APA, Harvard, Vancouver, ISO, and other styles

24

IOVINELLI, DANIELE. "Structure-based approaches for the rapid identification of tumor microenvironment nutrients, inhibitors and allosteric modulators against soluble and membrane proteins." Doctoral thesis, Università di Siena, 2022. http://hdl.handle.net/11365/1203165.

Full text

Abstract:

Bioinformatics is an interdisciplinary field that develops methods and software tools for understanding biological data, in particular when the data sets are large and complex. As an interdisciplinary field of science, bioinformatics combines biology, computer science, information engineering, mathematics and statistics to analyze and interpret the biological data. Bioinformatics has been used for in silico analyzes of biological queries using mathematical and statistical techniques. During the three years of doctorate we focused about Structural Bioinformatics and in particular in stud

APA, Harvard, Vancouver, ISO, and other styles

25

Jaeger, Alexander M. "Discovery of novel negative allosteric modulators of neuronal nicotinic acetylcholine receptors implications in the treatment of addiction and other neurological disorders /." Connect to resource, 2010. http://hdl.handle.net/1811/45419.

Full text

APA, Harvard, Vancouver, ISO, and other styles

26

Earl, Damien E. "Regulation of Neuronal L-type Voltage-Gated Calcium Channels by Flurazepam and Other Positive Allosteric GABA_A Receptor Modulators." University of Toledo Health Science Campus / OhioLINK, 2011. http://rave.ohiolink.edu/etdc/view?acc_num=mco1307379688.

Full text

APA, Harvard, Vancouver, ISO, and other styles

27

Bernat, Viachaslau [Verfasser], Peter [Akademischer Betreuer] Gmeiner, and Markus [Akademischer Betreuer] Heinrich. "Structure-based design and synthesis of allosteric modulators and chemical tools for the human chemokine receptor CXCR3 / Viachaslau Bernat. Gutachter: Peter Gmeiner ; Markus Heinrich." Erlangen : Friedrich-Alexander-Universität Erlangen-Nürnberg (FAU), 2014. http://d-nb.info/1075475856/34.

Full text

APA, Harvard, Vancouver, ISO, and other styles

28

Wilhelm, Adriana [Verfasser], and Rolf W. [Akademischer Betreuer] Hartmann. "Allosteric modulators directed to the PIF pockets of phosphoinositide-dependent protein kinase 1 (PDK1) and protein kinase C zeta (PKCz) / Adriana Wilhelm. Betreuer: Rolf W. Hartmann." Saarbrücken : Saarländische Universitäts- und Landesbibliothek, 2012. http://d-nb.info/1052781209/34.

Full text

APA, Harvard, Vancouver, ISO, and other styles

29

Bennouar, Khaled-Ezaheir. "Le récepteur métabotropique du glutamate de type 4 comme cible thérapeutique pour la maladie de Parkinson." Thesis, Aix-Marseille, 2012. http://www.theses.fr/2012AIXM4022.

Full text

Abstract:

La maladie de Parkinson (MP) est une maladie neurodégénérative chronique qui apparait en moyenne à partir 55 ans. Sa cause reste inconnue mais son apparition et son développement sont corrélés avec la perte progressive des neurones dopaminergique de la substance noire qui innervent les ganglions de la base (GB). Jusqu'à ce jour le traitement le plus efficace est basé sur la compensation du déficit en dopamine (DA) par l'administration de son précurseur, la L-DOPA, qui est métabolisé en DA. Ce traitement améliore les symptômes moteurs de la maladie et donc la qualité de vie des patients. Néanmo

APA, Harvard, Vancouver, ISO, and other styles

30

Shah, Urjita H. "A Roadmap for Development of Novel Antipsychotic Agents Based on a Risperidone Scaffold." VCU Scholars Compass, 2017. http://scholarscompass.vcu.edu/etd/4804.

Full text

Abstract:

Schizophrenia is a chronic psychotic illness affecting ~21 million people globally. Currently available antipsychotic agents act through a dopamine D2 receptor mechanism, and produce extrapyramidal or metabolic side effects. Hence, there is a need for novel targets and agents. The mGlu2/5-HT2A receptor heteromer has been implicated in the action of antipsychotic agents, and represents a novel and attractive therapeutic target for the treatment of schizophrenia. A long-term goal of this project is to synthesize bivalent ligands where a 5-HT2A receptor antagonist is tethered to an mGlu2 PAM via

APA, Harvard, Vancouver, ISO, and other styles

31

Contó, Marcos Brandão [UNIFESP]. "Estudo farmacológico e auto-radiográfico do complexo GABAA/Sítio benzodiazepínico, e ensaios bioquímicos da enzima Na+/K+- Atpase e de receptores glutamatérgicos em regiões encefálicas de ratos susceptíveis e não-susceptíveis às convulsões clônicas induzidas pelo DMCM, um agonista inverso benzodiazepínico." Universidade Federal de São Paulo (UNIFESP), 2008. http://repositorio.unifesp.br/handle/11600/9586.

Full text

Abstract:

Made available in DSpace on 2015-07-22T20:50:10Z (GMT). No. of bitstreams: 0 Previous issue date: 2008-12-26. Added 1 bitstream(s) on 2015-08-11T03:25:54Z : No. of bitstreams: 1 Publico-11764a.pdf: 1760987 bytes, checksum: 26371946d909a5525c0bd6c7cc6d7c33 (MD5). Added 1 bitstream(s) on 2015-08-11T03:25:55Z : No. of bitstreams: 2 Publico-11764a.pdf: 1760987 bytes, checksum: 26371946d909a5525c0bd6c7cc6d7c33 (MD5) Publico-11764b.pdf: 969495 bytes, checksum: d87ae7194b036aaff67581e32d434f64 (MD5)<br>Objetivo: Verificar se indivíduos susceptíveis e não-susceptíveis às convulsões clônicas indu

APA, Harvard, Vancouver, ISO, and other styles

32

Li, Victor. "Functional characterization of a novel NMDA receptor positive allosteric modulator." Thesis, University of British Columbia, 2017. http://hdl.handle.net/2429/62144.

Full text

Abstract:

The NMDA receptor is a glutamatergic ionotropic receptor key in mediating neuronal plasticity across virtually all synaptic circuits in the brain. An increasing list of neurological disorders have implicated NMDA receptor hypofunction as an integral part of pathogenesis, necessitating the production of NMDA receptor potentiators as therapeutics. To date, most of these attempts have used increased co-agonism at the glycine binding site of NMDA receptors, but this strategy has been plagued by low specificity and efficacy. Specific allosteric modulation of NMDA receptors is an ideal solutio

APA, Harvard, Vancouver, ISO, and other styles

33

Horswill, James G. "Pharmacological characterisation of a novel cannabinoid CB1 receptor allosteric modulator." Thesis, University of Reading, 2011. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.541953.

Full text

APA, Harvard, Vancouver, ISO, and other styles

34

Kwapisz, Lina. "Pharmacology of a novel biased allosteric modulator for NMDA receptors." Thesis, Virginia Tech, 2021. http://hdl.handle.net/10919/103690.

Full text

Abstract:

NMDA glutamate receptor is a ligand-gated ion channel that mediates a major component of excitatory neurotransmission in the central nervous system (CNS). NMDA receptors are activated by simultaneous binding of two different agonists, glutamate and glycine/ D-serine1. With aging, glutamate concentration gets altered, giving rise to glutamate toxicity that contributes to age-related pathologies like Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, and dementia88,95. Some treatments for these conditions include NMDA receptor blockers like memantine130. However, when compl

APA, Harvard, Vancouver, ISO, and other styles

35

Batis, Nikolaos. "Investigation of the allosteric pharmacology of the 5-HT₃ receptor identifying the potent allosteric modulator 5-chloroindole." Thesis, University of Birmingham, 2015. http://etheses.bham.ac.uk//id/eprint/5747/.

Full text

Abstract:

The 5-HT₃ receptor is a ligand-gated ion channel that mediates for example fast synaptic neurotransmission in the CNS and PNS. 5-HT₃ receptor antagonists are established anti-emetics in the clinic, they also offer symptomatic relief for patients with irritable bowel syndrome, yet, sometimes serious side-effects limits their use in this indication. The 5-HT₃ receptor is modulated allosterically by various compounds including colchicine, alcohols and volatile anaesthetics but as yet, these modulators either lack potency or selectivity, which hinders investigation. The present study reports a nov

APA, Harvard, Vancouver, ISO, and other styles

36

Yi, Bitna. "Allosteric Approaches to the Targeting of Neuronal Nicotinic Receptor for Drug Discovery." The Ohio State University, 2013. http://rave.ohiolink.edu/etdc/view?acc_num=osu1371550355.

Full text

APA, Harvard, Vancouver, ISO, and other styles

37

Gade, Aravind. "Hydrogen Sulfide as an allosteric modulator of ATP sensitive potassium channels in colonic inflammation." VCU Scholars Compass, 2012. http://scholarscompass.vcu.edu/etd/2711.

Full text

Abstract:

The ATP sensitive potassium channel (KATP) in mouse colonic smooth muscle cell is a complex containing a pore forming subunit (Kir6.1) and a sulfonyl urea receptor subunit (SUR2B). These channels are responsible for maintaining the cellular excitability of the smooth muscle cell which in turn regulates the motility patterns in the colon. We used whole-cell voltage-clamp techniques to study the alterations in these channels in smooth muscle cells in experimental model of colitis (colonic inflammation). Colitis was induced in BALB/C mice following an intracolonic administration of trinitrobenzen

APA, Harvard, Vancouver, ISO, and other styles

38

Schmitz, Jens. "Synthese von Liganden muscarinerger Rezeptoren : Allostere Modulatoren, bivalente Agonisten und Antagonisten." Doctoral thesis, kostenfrei, 2008. http://www.opus-bayern.de/uni-wuerzburg/volltexte/2008/2839/.

Full text

APA, Harvard, Vancouver, ISO, and other styles

39

Verespy, Stephen S. III. "Probing Allosteric, Partial Inhibition of Thrombin Using Novel Anticoagulants." VCU Scholars Compass, 2016. http://scholarscompass.vcu.edu/etd/4431.

Full text

Abstract:

Thrombin is the key protease that regulates hemostasis; the delicate balance between procoagulation and anticoagulation of blood. In clotting disorders, like deep vein thrombosis or pulmonary embolism, procoagulation is up-regulated, but propagation of clotting can be inhibited with drugs targeting the proteases involved, like thrombin. Such drugs however, have serious side effects (e.g., excessive bleeding) and some require monitoring during the course of treatment. The reason for these side effects is the mechanism by which the drugs’ act. The two major mechanisms are direct orthosteric and

APA, Harvard, Vancouver, ISO, and other styles

40

BERARDO, CLARISSA ANGELA IRIS. "MPEP, a metabotropic Glutamate Receptor 5 (mGluR5) negative allosteric modulator, protects from hepatic ischemic injury both in vitro and ex vivo." Doctoral thesis, Università degli studi di Pavia, 2018. http://hdl.handle.net/11571/1214799.

Full text

APA, Harvard, Vancouver, ISO, and other styles

41

Shimizu, Yuji. "Studies on the binding kinetics and signaling biases of drugs targeting seven-transmembrane receptors." Kyoto University, 2018. http://hdl.handle.net/2433/230981.

Full text

APA, Harvard, Vancouver, ISO, and other styles

42

Planelles, Herrero Vicente José. "Bases mécanistiques et structurales de la régulation de l'activité des myosines." Thesis, Paris 6, 2017. http://www.theses.fr/2017PA066465.

Full text

Abstract:

Les moteurs moléculaires sont des protéines capables de produire une force : elles transforment l'énergie chimique de l'hydrolyse de l'ATP en énergie mécanique. Cette thèse se focalise sur l'étude d'une famille de moteurs moléculaires, les myosines, qui se déplacent le long des filaments d'actine et assurent d'importantes fonctions cellulaires.La myosine VI est une myosine très particulière car elle est la seule à se déplacer vers l'extrémité négative des filaments d'actine. Elle est produite dans la cellule sous forme auto-inhibée, inactive. Dans la cellule, son activité est également régulée

APA, Harvard, Vancouver, ISO, and other styles

43

Scholl, Daniel. "Exchange between ordered and disordered segments in CFTR modulates function at the expense of stability: A molecular pathway for misfolding of CFTR." Doctoral thesis, Universite Libre de Bruxelles, 2020. http://hdl.handle.net/2013/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/313253.

Full text

Abstract:

The genetic disease cystic fibrosis is the most common lethal genetic disease in Western countries. People born with cystic fibrosis suffer from many health issues including severe respiratory problems, inflammation and recurrent lung infections that can become fatal. The disease is caused by the loss of function of a protein called the cystic fibrosis transmembrane conductance regulator (CFTR). CFTR is an chloride ion channel and, in healthy people, its activity assures correct water and salt transport across the cell membrane. Most cases of cystic fibrosis are caused by a genetic defect that

APA, Harvard, Vancouver, ISO, and other styles

44

Tora, Amélie. "Modulation endogène des récepteurs métabotropiques du glutamate : bases moléculaires et implications fonctionnelles de la sensibilité au chlore extracellulaire." Thesis, Montpellier, 2015. http://www.theses.fr/2015MONTT032.

Full text

Abstract:

Les récepteurs métabotropiques du glutamate (mGluRs) sont des récepteurs couplés aux protéines G (RCPGs) modulant la transmission synaptique au sein du système nerveux central. D'un point de vue structural, ils ont la particularité de posséder un large domaine extracellulaire, le Venus Flytrap (VFT), où se lie leur ligand endogène, le glutamate. Leur domaine transmembranaire à 7 hélices, commun à tous les RCPGs, est connu pour être la cible d'une nouvelle classe de molécules à visée thérapeutique, les modulateurs allostériques. Au contraire, le VFT est le siège du développement de ligands comp

APA, Harvard, Vancouver, ISO, and other styles

45

Langer, Kai [Verfasser], Bodo [Akademischer Betreuer] Laube, and Gerhard [Akademischer Betreuer] Thiel. "Analysis of M4 transmembrane domains in NMDA receptor function: a negative allosteric modulator site at the GluN1-M4 is determining the efficiency of neurosteroid modulation / Kai Langer ; Bodo Laube, Gerhard Thiel." Darmstadt : Universitäts- und Landesbibliothek, 2021. http://d-nb.info/1234657767/34.

Full text

APA, Harvard, Vancouver, ISO, and other styles

46

Planelles, Herrero Vicente José. "Bases mécanistiques et structurales de la régulation de l'activité des myosines." Electronic Thesis or Diss., Paris 6, 2017. https://accesdistant.sorbonne-universite.fr/login?url=https://theses-intra.sorbonne-universite.fr/2017PA066465.pdf.

Full text

Abstract:

Les moteurs moléculaires sont des protéines capables de produire une force : elles transforment l'énergie chimique de l'hydrolyse de l'ATP en énergie mécanique. Cette thèse se focalise sur l'étude d'une famille de moteurs moléculaires, les myosines, qui se déplacent le long des filaments d'actine et assurent d'importantes fonctions cellulaires.La myosine VI est une myosine très particulière car elle est la seule à se déplacer vers l'extrémité négative des filaments d'actine. Elle est produite dans la cellule sous forme auto-inhibée, inactive. Dans la cellule, son activité est également régulée

APA, Harvard, Vancouver, ISO, and other styles

47

Soualmia, Feryel. "Modulateurs synthétiques de la kallikréine 6, protéase à sérine impliquée dans les maladies neurodégénératives : identification, mécanisme d’action et validation de concept." Electronic Thesis or Diss., Paris 6, 2016. http://www.theses.fr/2016PA066755.

Full text

Abstract:

La kallikréine humaine 6 (hK6) ou neurosine est la protéase à sérine la plus abondante du système nerveux central (SNC). Sa dualité de fonction dans les processus neurodégénératifs font d’elle une cible privilégiée pour la conception de modulateurs pharmacologiques de son activité. Cependant, il existe aujourd’hui très peu de composés répondant à cette attente. Aussi, le principal objectif de ces travaux de thèse a consisté à identifier des inhibiteurs et activateurs organiques de faible poids moléculaire (<500 Da) de la hK6, compatibles avec un développement clinique. L’étude de la hK6 sou

APA, Harvard, Vancouver, ISO, and other styles

48

Mazzolari, A. "IN SILICO APPROACHES IN DRUG DESIGN AND DEVELOPMENT: APPLICATIONS TO RATIONAL LIGAND DESIGN AND METABOLISM PREDICTION." Doctoral thesis, Università degli Studi di Milano, 2015. http://hdl.handle.net/2434/347523.

Full text

Abstract:

In the last decades, the applications of computational methods in medicinal chemistry have experienced significant changes which have incredibly expanded their approaches, and more importantly their objectives. The overall aim of the present research project is to explore the different fields of the modelling studies by using well-known computational methods as well as different and innovative techniques. Indeed, computational methods traditionally consisted in ligand-based and the structure-based approaches substantially aimed at optimizing the ligand structure in terms of affinity, potenc

APA, Harvard, Vancouver, ISO, and other styles

49

Mebarki, Lamia. "Recherche ou développement, et caractérisation fonctionnelle et structurale d'effecteurs peptidiques de deux récepteurs membranaires à incidences physiopathologiques." Thesis, Aix-Marseille, 2017. http://www.theses.fr/2017AIXM0217.

Full text

Abstract:

Les récepteurs à la vasopressine V1bR et à la sérotonine 5HT3R jouent des rôles physiologiques importants dans la détection des signaux extracellulaires, les mécanismes de transmission nerveuse et diverses pathologies dont le cancer, le diabète et des maladies des SNC et SNP. Mes études avaient pour but de générer ou trouver des modulateurs peptidiques de ces deux récepteurs. Pour le V1bR, j’ai développé plusieurs anticorps de type VHH et les ai caractérisés aux plans biochimique et fonctionnel. L’un de ces VHHs agit comme un agoniste allostérique complet et spécifique du V1bR humain (hV1bR).

APA, Harvard, Vancouver, ISO, and other styles

50

Cornelison, Garrett Lee. "Zinc interactions with allosteric modulators at the glycine receptor." Thesis, 2014. http://hdl.handle.net/2152/25830.

Full text

Abstract:

The glycine receptor (GlyR) is a ligand-gated ion channel member of the Cys-loop receptor superfamily, responsible for inhibitory neurotransmission in the brain and spinal cord. Zinc is a potent allosteric modulator of GlyR function, enhancing GlyR activity at low nM to 10[mu]M concentrations while inhibiting GlyR activity at higher concentrations. We investigated sources of contaminating zinc, identifying low nM levels of zinc in ultrapure H₂O, powdered reagents used in the preparation of common electrophysiological buffers, and in polystyrene pipets. These low levels of zinc were capable of

APA, Harvard, Vancouver, ISO, and other styles

We offer discounts on all premium plans for authors whose works are included in thematic literature selections. Contact us to get a unique promo code!