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Thèses sur le sujet « NMR ligand-receptor interaction studies »

Auteur : Grafiati

Publié le 9 mars 2023

Mis à jour le 31 juillet 2025

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1

Guzzetti, I. "INTEGRIN AND CADHERIN LIGANDS: INTERACTION STUDIES BY COMPUTATIONAL METHODS AND BIOAFFINITY NMR ON INTACT CELLS." Doctoral thesis, Università degli Studi di Milano, 2014. http://hdl.handle.net/2434/243616.

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On a molecular level protein – ligand interactions are central to a number of biological processes, but their investigation is inherently difficult due to several problems, especially for membrane proteins. The study of this type of interactions poses a whole set of challenges, including the characterization of the dynamic behaviour and of the conformational properties of the ligands in complex with the target macromolecules. A variety of biophysical methods have been developed to study protein – ligand interactions and several NMR spectroscopic techniques have emerged as powerful methods to i

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2

Tengel, Tobias. "Studies of protein structure, dynamics and protein-ligand interactions using NMR spectroscopy." Doctoral thesis, Umeå : Univ, 2007. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-1472.

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AIROLDI, CRISTINA. "Development of new potential antitumor drugs based on Ras protein inhibition." Doctoral thesis, Università degli Studi di Milano-Bicocca, 2007. http://hdl.handle.net/10281/116562.

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Because of their role in oncogenesis, inhibition of Ras proteins, particularly of their tumorigenic variants, represents today one of the principal strategies finalized to the obtainment of new antitumoral therapies. Among the different possible approaches, one of the most innovative and less explored is represented by the inhibition of this protein activation, key event for the explication of their biological activity, but also for the Ras-induced tumoral cell transformation. Objective of this thesis has been the development of new small molecules able to inhibit, at least partially (total i

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MERLO, SILVIA. "Characterization of biomedical relevant ligand-protein interactions using Nuclear Magnetic Resonance (NMR) Spectroscopy." Doctoral thesis, Università degli Studi di Milano-Bicocca, 2013. http://hdl.handle.net/10281/40953.

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NMR techniques allow to obtain structural information useful for the comprehension of biological processes. The aim of this work is to investigate interactions between biological macromolecules and binding partners, including other macromolecules, small ligands and therapeutically relevant compounds. These results will be exploited for the design and development of new potential drugs and medical devices.

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5

Edwards, Rachel. "Ligand interactions of glutamate receptor 2 studied by NMR." Thesis, University of Manchester, 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.495042.

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Neurotransmission is the action of communication between neurons; the most common neurotransmitter in the mammalian CNS is glutamate. Excessive activation of glutamate receptors have been implicated in a number of neurodegenerative diseases; they are therefore of great interest for investigation as drug targets. The ionotropic glutamate receptor GluR2 has previously been expressed as a soluble construct representing the ligand binding domain known as S1S2J. GluR2 S1S2J contains two separate binding sites for different types of ligands; the glutamate binding site and the allosteric modulator bi

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6

Curtis, Nicola. "Tritium NMR studies of protein-ligand interactions." Thesis, University of Surrey, 1994. http://epubs.surrey.ac.uk/842983/.

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Tritium NMR studies provide a convenient way of obtaining detailed information about conformational equilibria, dynamic processes and specific interactions in protein-ligand complexes provided that suitably 3H-labelled molecules are available. In this study [7,9-3H]- and [3',5',7-3H]folic acid, and [3',5',7-3H]methotrexate were synthesised and the NMR spectra of their complexes with Lactobacillus casei dihydrofolate reductase (DHFR) were assigned and analysed as a function of pH (DHFR-folate complexes) and temperature (DHFR-methotrexate complexes). From these data it was possible to obtain fur

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7

Miyoshi, Emi. "Platinum(II) complexes : studied by diffusion NMR." Thesis, View thesis, 2008. http://handle.uws.edu.au:8081/1959.7/33587.

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Six novel platinum(II) intercalators of the form [Pt(AL)(IL)]Cl2, where AL = ethylenediamine (en), 1R,2R-diaminocyclohexane (R,R-dach), or 1S,2S-diaminocyclohexane (S,S-dach) and IL = 4,7-dihydroxy-1,10-phenanthroline (4,7-dhp) or 4,7-dicarboxy-1,10-phenanthroline (4,7-dcp), were synthesised. All complexes were prepared by the addition of the intercalating ligand followed by the addition of the diamine ancillary ligand. The complexes with 4,7-dhp were soluble in DMSO and were characterised by 1H, 13C, and 195Pt NMR, elemental analysis, UV-vis, ESI-MS, and CD. The complexes with 4,7-dcp were on

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8

Miyoshi, Emi. "Platinum(II) complexes studied by diffusion NMR /." View thesis, 2008. http://handle.uws.edu.au:8081/1959.7/33587.

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Thesis (M.Sc.) (Hons)--University of Western Sydney, 2008.<br>A thesis presented to the University of Western Sydney, College of Health and Science, School of Biomedical and Health Sciences, in fulfilment of the requirements for the degree of Master of Science (Honours). Includes bibliographies.

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Åkerberg, Helena. "Functional Studies of the Neuropeptide Y System : Receptor-Ligand Interaction and Regulation of Food Intake." Doctoral thesis, Uppsala universitet, Institutionen för neurovetenskap, 2009. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-9533.

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The members of the mammalian neuropeptide Y family, i.e. the peptides neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP), are all involved in regulation of food intake. In human and most other mammals they act via receptors Y1, Y2, Y4 and Y5. NPY is released in the hypothalamus and is one of the strongest appetite-stimulating neurotransmitters whereas PP and PYY are secreted from gut endocrine cells after meals and function as appetite-reducing hormones. This thesis describes studies of the NPY system at both the molecular and the physiological level. The first part describ

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10

Björnerås, Johannes. "The opioid peptide dynorphin A : Biophysical studies of peptide–receptor and peptide–membrane interactions." Doctoral thesis, Stockholms universitet, Institutionen för biokemi och biofysik, 2014. http://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-107766.

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The work presented in this thesis concerns the opioid peptide dynorphin A (DynA). DynA functions primarily as a neurotransmitter and belongs to the family of typical opioid peptides. These peptides are a part of the opioid system, together with the opioid receptors, a family of GPCR membrane proteins. The opioid system system is involved or implicated in several physiological processes such as analgesia, addiction, depression and other types of neurological disorders. In this thesis, two biologically relevant aspects of DynA have been investigated with biophysical methods. First, interactions

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11

Rigau, Roca Laura. "Identification of protein-ligand interactions by mass spectrometry and NMR, case studies: LFA-1, Bcl-xl and Bcl-2." Thesis, University of Bristol, 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.492546.

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Current genomic and proteomic research is generating a considerable number of potential new therapeutic targets. To tackle all these pharmacological targets, the development of rapid and reliable screening methods, which give information on protein-ligand interactions, are of great importance. New advances in these technologies are often emerging and more will surely follow.

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12

Wang, Ying-Hui. "Molecular interaction of zinc finger domain : study of androgen receptor DNA binding domain and SCA7 domain of Ataxin7 by NMR." Strasbourg, 2010. http://www.theses.fr/2010STRA6018.

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La voie de signalisation du récepteur des androgènes (AR) est impliquée dans la progression du cancer de la prostate, et il a été montré que des mutations dans ce domaine étaient responsables de l'activation constitutive des gènes placés sous le contrôle des hormones androgènes. Une de ces mutations transforme un résidu thréonine du DBD en alanine (T575A). Des expériences permettant de mesurer l'activité de transcription ont permis à l'équipe du Dr. Ceraline à l'IRCAD de montrer que la mutation T575A induit un changement de spécificité du récepteur. Alors que l'activité de promoteurs placés so

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13

Liao, Subo 1963. "Design and synthesis of topographically constrained amino acids, and bioactive peptides for studies of ligand-receptor interaction, and for de novo design of delta-opioid selective non-peptide mimetics as potential therapeutics." Diss., The University of Arizona, 1997. http://hdl.handle.net/10150/282418.

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Topographical constraint is the most powerful approach for the design of bioactive peptides to explore the bioactive conformation of crucial side-chain pharmacophores of amino acid residues in peptide-receptor recognition and signal transduction. Novel topographically constrained amino acids β-isopropylphenylalanine and 2',6'-dimethyl-2,3-methanophenylalanine have been designed and synthesized. Incorporation of the four optically pure β-isopropylphenylalanine stereoisomers into deltorphin I produced four peptide analogues of [β-iPrPhe]Deltorphin I with differentiated bioactivities. The most po

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14

Miyoshi, Emi, University of Western Sydney, College of Health and Science, and School of Biomedical and Health Sciences. "Platinum(II) complexes : studied by diffusion NMR." 2008. http://handle.uws.edu.au:8081/1959.7/33587.

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Six novel platinum(II) intercalators of the form [Pt(AL)(IL)]Cl2, where AL = ethylenediamine (en), 1R,2R-diaminocyclohexane (R,R-dach), or 1S,2S-diaminocyclohexane (S,S-dach) and IL = 4,7-dihydroxy-1,10-phenanthroline (4,7-dhp) or 4,7-dicarboxy-1,10-phenanthroline (4,7-dcp), were synthesised. All complexes were prepared by the addition of the intercalating ligand followed by the addition of the diamine ancillary ligand. The complexes with 4,7-dhp were soluble in DMSO and were characterised by 1H, 13C, and 195Pt NMR, elemental analysis, UV-vis, ESI-MS, and CD. The complexes with 4,7-dcp were on

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15

Chitayat, Seth. "NMR and Biophysical Studies of Modular Protein Structure and Function." Thesis, 2007. http://hdl.handle.net/1974/727.

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Proteins modularity enhances the multi-functionality and versatility of proteins by providing such properties as multiple and various ligand-binding sites, increased ligand affinity through the avidity effect, and the juxtaposition of ligand-binding modules near catalytic domains. An NMR-based "dissect-and-build" approach to studying modular protein structure and function has proven very successful, whereby modules are initially characterized individually and then correlated with the overall function of a protein. We have used the dissect-and-build approach and NMR to study two modular protein

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16

Karanth, N. Megha. "Protein NMR Studies of E. Coli IlvN and the Protease-VPg Polyprotein from Sesbania Mosaic Virus." Thesis, 2013. http://etd.iisc.ac.in/handle/2005/3334.

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Acetohydroxyacid synthase is a multisubunit enzyme that catalyses the first committed step in the biosynthesis of the branched chain amino acids viz., valine, leucine and isoleucine. In order to understand the structural basis for the observed allosteric feedback inhibition in AHAS, the regulatory subunit of AHAS isozymes I from E. coli was cloned, expressed, purified and the conditions were optimized for solution NMR spectroscopy. IlvN was found to exist as a dimer both in the presence and absence of the feedback inhibitor. Using high-resolution multidimensional, multinuclear NMR experiments,

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17

Karanth, N. Megha. "Protein NMR Studies of E. Coli IlvN and the Protease-VPg Polyprotein from Sesbania Mosaic Virus." Thesis, 2013. http://etd.iisc.ernet.in/2005/3334.

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Acetohydroxyacid synthase is a multisubunit enzyme that catalyses the first committed step in the biosynthesis of the branched chain amino acids viz., valine, leucine and isoleucine. In order to understand the structural basis for the observed allosteric feedback inhibition in AHAS, the regulatory subunit of AHAS isozymes I from E. coli was cloned, expressed, purified and the conditions were optimized for solution NMR spectroscopy. IlvN was found to exist as a dimer both in the presence and absence of the feedback inhibitor. Using high-resolution multidimensional, multinuclear NMR experiments,

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