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 25 for “"ATP binding site"”.
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Site-directed mutagenesis of the ATP-binding site in spinach rubisco activase
… A significant difference in the kinetics of the ATP response between the two cloned isoforms was observed. The 45 kD polypeptide exhibited sigmoidal kinetics for both rubisco activase and ATPase activities, while the activities of the 41 kD isoform appeared to follow standard Michaelis-Menten …
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Regulation of Rubisco in Arabidopsis Thaliana Rca(-) Complemented With Arabidopsis Rubisco Activase Engineered at an ATP Binding Site
… greater than 42kD wild type and Q111S at ADP/ATP ratios known to exist in planta. Q111D showed a Rubisco activation rate at night time ADP/ATP greater than the 42kD wild type rate at zero ADP/ATP suggesting an altered response. Measurements of K$\rm\sb{d}$ ADP and K$\rm\sb{d}$ ATP with a …
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A Fragment-Based Drug Discovery Approach for the Development of Selective Inhibitors of Protein Kinase CK2
… successfully led to the identification of novel binding sites and highly efficient chemical ligands. This demonstrates the utility of the FBDD strategy against well-established kinase targets, where selectivity is otherwise challenging due to significant conservation of the ATP-binding site. …
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Discovery of novel highly selective Rho kinase (ROCK) inhibitory peptides and evaluation of their biological activities
… inhibitors of ROCK are type I which compete with ATP to bind to the ATP binding site on catalytic domain of ROCK in its active conformation and since the ATP binding site is highly conserved in kinases, these inhibitors can cause many side effects associated with their nonspecific binding and …
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Functionalization and Modification of Naphthaquinone Analogs as HER2 Kinase Inhibitors
… small molecule inhibitors that bind to the ATP binding site of the tyrosine kinase domain in order to inhibit tyrosine auto-phosphorylation. This process controls biological pathways that mediate the cell growth. In normal cells this process is highly controlled. We are targeting the …
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Synthesis and evaluation of novel kinase inhibitors as anti-cancer agents
… and apoptosis. ROCK is inhibited bythe ATP mimic Y27632, which competitively binds the ATP binding site. All protein kinasespossess an ATP binding pocket and subtle differences in these pockets can allow thedevelopment of highly selective ATP mimicking inhibitors.The major part of my …
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Expression of the P-glycoprotein Homologue1 on food vacuoles isolated from Chloroquine-sensitive and resistant Plasmodium falciparum strains
… multidrug resistance protein of the malaria parasite Plasmodium falciparum, the P-glycoprotein homologue1 (Pgh1), was quantified on food vacuoles, the site of action of chloroquine. Chloroquine susceptibility was determined in 8 different P. falciparum strains. Food vacuoles were isolated from …
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Novel Design Strategy for Potent and Selective CDPK1 Inhibitors for Cryptosporidiosis
… Among those, small molecules targeting the ATP-binding site of CDPK1 have held promise; however, none of the original series of CDPK1 inhibitors has successfully been used in humans due to various toxicities. Recently, UH15-16 that contains a pyridopyrimidinone scaffold, was reported as a …
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Novel Structures of RAD51 Reveal Mechanisms in DNA Damage Repair and Genomic Stability
… the presence of a second metal cation at the ATP-binding site, which forms the basis for a mechanism of ATP-hydrolysis dependent filament disassembly, confirmed by the structure of a RAD51 filament in the presence of ADP. Here I also describe two structures of RAD51 bound to the C-terminus of …
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G-Triple Chemiluminescent DNAZyme Based Biosensor for the Detection of Calcium(II) Ions in Solution and the Biological Functionality of Kinase Enzymes and the Rationale for their Employment as Promising Drug Targets, Substrate Specific Inhibition of P38alpha
… which provide a suitable hydrophobic hemin binding pocket that contributes to oxidation enhancement. G-triplex DNA structures are characterized by G:G:G triads and are stabilized by Hoogsteen hydrogen bonding. Originally identified as folding intermediates for G-quadruplexes, certain …
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Protein-Protein Interaction and Structure-Function Studies of XcpR, a Protein Involved in Extracellular Protein Secretion of Pseudomonas Aeruginosa
… secretion apparatus which contains a consensus ATP-binding site and is thought to energize the secretion process. These mutations result in a deficiency of exoprotein secretion at a non-permissible temperature, and therefore, these conditional xcpR mutations were used to isolate suppressor …
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Gene cloning, adjustable expression and site-directed mutagenesis of Escherichia coli adenylate kinase
… effect on the adenine nucleotide concentrations. Site-directed mutagenesis was used to investigate the location of the ATP and AMP binding sites on adenylate kinase and the mechanism of substrate inhibition. Two amino acids, phe86 and tyr133, which were found to be in close contact with the …
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Uncovering Reversible AMPylation of BiP Mediated by dFic During ER Homeostasis
… a covalent attachment of an AMP moiety from ATP to hydroxyl side chains of target substrates. Fic domain which mediates AMPylation is highly conserved across species, including higher eukaryotes, implicating an essential role of this modification in cellular function. Despite the recent …
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Uncovering Reversible AMPylation of BiP Mediated by dFic During ER Homeostasis
… a covalent attachment of an AMP moiety from ATP to hydroxyl side chains of target substrates. Fic domain which mediates AMPylation is highly conserved across species, including higher eukaryotes, implicating an essential role of this modification in cellular function. Despite the recent …
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Targeting protein kinases to manage or prevent Alzheimer’s disease
… used to define the amino acid residues in the ATP binding site as well as other important sites and motifs. We searched for the comstructural motifs and domains of GSK-3β, CDK5 and PERK. Further, we identified the conserved water molecules in GSK-3β, CDK5 and PERK through calculation of the …
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Approaches Towards the Inhibition of Anti-Apoptotic Proteins
… targeting pockets outside the well-conserved ATP-binding site: -Using a Fragment-Based-Drug-Discovery (FBDD) approach twelve small molecule inhibitors of CK2 were developed. The lead molecule, 3l, inhibited the catalytic activity of CK2α by binding in the cryptic αD pocket with a Kd of 4 μM. …
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Response to treatment with chemical and biological inhibitors of c-met mutated form
c-MET is a receptor tyrosine kinase that, after binding with its ligand, hepatocyte growth factor (HGF), activates many signaling pathways, driving proliferation, motility, migration and invasion. Although c-MET is important in the control of tissue homeostasis under normal physiological …
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A Chemical-Genetic Map of Drug Resistance in Mycobacterium Tuberculosis
… screens was ettA, a ribosome-associated ATPase that regulates translation initiation. CRISPRi mutants for ettA were resistant to a diverse set of drugs including streptomycin, levofloxacin, and ethambutol. Mining a whole genome sequence database of over 40,000 clinical Mtb isolates we …
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Characterisation of the reaction of 1,4-phenylenebismaleimide with Ca²⁺-ATPase and elucidation of the intramolecular crosslink site
The SR Ca²⁺-ATPase is an ATP driven pump that removes calcium from the sarcoplasm and myofibrils to allow muscle relaxation. The sulfhydryl crosslinker, 1,4- phenylenebismaleimide, reacts with Ca²⁺-ATPase (110 kD) to form a species with an apparent molecular weight of 125 kD, as well as dimers and …
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On the origins of enzyme inhibitor selectivity and promiscuity: a case study of protein kinase binding to staurosporine
… to find the relationship between the shapes of ATP binding sites and their affinities for inhibitors. My shape-based dendrogram shows clustering of the kinases based on similarity in shape. I investigate the pocket in terms of conservation of surrounding amino acids and atoms in order to …
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