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 36 for “"active conformation"”.
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The role of the CCR5 co-receptor conformation in HIV fusion
… thesis aimed to better define the co-receptor conformation by determining whether mutants of the CCR5 receptor stabilized in the active conformation were less able to mediate HIV fussion. Eight mutant receptors were generated by site-directed mutagenesis and screened for constitutive activity …
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Syntheses and Bioactivities of Targeted and Conformationally Restrained Paclitaxel and Discodermolide Analogs
… Studies aimed at understanding the biologically active conformation of paclitaxel bound on β–tubulin are described. In this work, the synthesis of isotopically labeled taxol analogs is described and the REDOR studies of this compound complexed to tubulin agrees with the hypothesis that palictaxel …
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Structural investigations of adenosylcobalamin-dependent enzyme maturation
… from M. extorquens. This structure trapped an active conformation of the G-protein chaperone, revealing the first snapshots of the 180° rotation of one protomer needed to complete the nucleotide binding site and perform GTP hydrolysis. We also present mutagenesis and solution state data for …
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Regulatory domains of the Arf GEF Sec7 scaffold autoinhibited and active conformations
… DCB/HUS domain, and we demonstrate this is the active conformation. In this conformation the GEF domain displaces a loop in the DCB/HUS domain we refer to as the “D-loop”. Removal of the D-loop results in a modest increase in GEF activity in vitro, and when combined with HDS2 mutations …
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Methods and Applications of Computational Design in Multiple States
… energy landscape that determines the available conformational states of a protein. Over the past two decades, our ability to design proteins has advanced significantly, however, our understanding of and ability to design multistate proteins remains an area of significant challenge. The …
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The Mechanism of N10-Formyltetrahydrofolate Synthetase. Use of Human Thymidylate Synthase Variants to Characterize Asymmetric Ligand Binding and to Identify Novel Allosteric Inhibitors.
… ZD9331, occupies the same space within the active site as the nucleosides. The presence and position of substrate, substrate analog, and intermediate within the active site supports the catalytic mechanism hypothesis that FTHFS works via a random bi uni uni bi ping-pong ter ter mechanism. …
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Lariat peptide inhibitors of Abl kinase
… and instead bind preferentially to the kinase active conformation. Selectivity analysis indicated that the lariats do not recognize Src family kinases, which share a high structural similarity with Abl kinase in their active conformation. These findings, coupled with preliminary results from …
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Synthesis of Taxol™ Analogs as Conformational Probes
… Studies aimed at understanding the biologically active conformation of taxol and its binding environment on β-tubulin are described. This knowledge is important because it could lead to the design of structurally less complicated drugs with better efficacy and better bioavailability. Moreover, …
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Innovative Purification Protocol for Heparin Binding Proteins: Relevance in Biopharmaceutical and Biomedical Applications
… FGF-1 and the D2 are in a native biologically active conformation. The findings of this study will not only aid an in-depth investigation of this class of proteins but will also provide avenues for inexpensive and efficient purification of other important biological macromolecules.</p>
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Dynamics of Hairpin Ribozyme
… understanding how RNA organizes itself into an active conformation that performs its catalytic function. As a small nucleolytic ribozyme, the hairpin ribozyme provides an excellent opportunity to dissect the enzymatic origin of RNA systems. In our experiments we use RNA molecules that have been …
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Insights Into the Dynamic Structure and Inhibitory Mechanism of Plasminogen Activator Inhibitor Type 1
… of the stable variant as a starting point. Using conformationally-sensitive ligands, we found that the RCL of PAI-1 exhibited more partial insertion into the beta-sheet A and that beta-sheet A was more accessible to the mobile RCL than was evident from the crystal structure of 14-1B. These …
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Cip4 and Src In Promoting The Migration and Invasion of Breast Cancers
… promotes actin polymerization by stabilizing the active conformation of N-WASp. CIP4 and N-WASp are both phosphorylated by Src, implicating this pathway in Src-dependent cytoskeletal rearragement. This represents a novel role for F-BAR proteins in migration and invasion.
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Structure of the LKB1-STRAD-MO25 tumour suppressor complex
… can exert their functions through their conformation rather than phosphorylation. STRAD adopts a closed conformation typical of active protein kinases, and binds LKB1 as a pseudosubstrate. STRAD binding promotes the active conformation of LKB1, which is further stabilised by MO25 …
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Design and stereoselective synthesis of novel bicyclicbeta-turn dipeptide mimetics and cis-4-substitutedproline analogues for peptides and peptidomimetics
… function. However, to establish the biologically active conformation is challenging because most small linear peptides are inherently flexible, and at present, our knowledge of 3D structural information of ligand-receptor complexes is very limited. Hence, some strategies have been developed to …
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Biochemical and molecular characterization of methyl-accepting chemotaxis proteins from Bacillus subtilis
… purified and reconstituted in a functionally active conformation from the gram positive bacterium, Bacillus subtilis. This forms the foundation for the establishment of an in vitro system using other purified chemotactic components. Four transducer genes were subsequently cloned and sequenced …
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Nonlinear optical properties of chiral media.
… of molecular chirality is examined. An optically active conformation for water in a static electric field parallel to the surface is proposed.
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Discovery of novel highly selective Rho kinase (ROCK) inhibitory peptides and evaluation of their biological activities
… 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 inhibition of other kinases such as PKA and PKC. In order to overcome this …
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Pressure Dissociation and Temperature Stability of Lactate Dehydrogenase (Oligomeric, Proteins, Conformational, Drift, Activity)
… monomers undergo a progressive change in conformation with time, i.e., a "conformational drift", the extent of which depends upon the pressure applied and the duration of high-pressure incubation. The drifted monomer is proven to reassociate into tetramers immediately after release of …
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Structural studies of Butirosin D and FrbG
… presented here represents a catalytically active conformation, with the C4 of the NADP(H) nicotinamide situated near the N5 of the FAD isoalloxazine, poised for hydride transfer. A comparison with previously determined structures of FMOs in the post-hydride transfer conformation highlights …
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Structural studies of metalloenzyme complexes in acetogenic carbon fixation
… with in crystallo activity data, illustrates how conformational movements, which can occur within protein crystals, enable the B12 cofactor to alternate between a sequestered conformation for cofactor protection and an active conformation for catalysis. Small-angle X-ray scattering (SAXS) …
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