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Showing 1 to 20 of 61 for “"amphipathic"”.
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Amphipathic Hybrid Cyclic-Linear Peptides as a Drug Delivery System
<p>Amphipathic Hybrid Cyclic-Linear Peptides as a Drug Delivery System by Jonathan A. Moreno Peptides</p> <p>[RW]<sub>4</sub> and [R<sub>5</sub>W<sub>4</sub>] have been previously identified as molecular transporter Cell Penetrating Peptide (CPP) and antimicrobial agents, respectively. These …
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Modulation of Antibacterial Activity and Cytotoxicity in Amphipathic Cyclic Peptide [R4W4] Using Histidine Substitution
<p>Antibiotics have been the gold standard frontline defense against bacterial infections for decades. At the same time, these infecting bacteria have continued to evolve to resist developed antibiotics in an almost endless cycle. As such, we aim to take an alternative approach utilizing …
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Conformational ensembles and dynamics of amphipathic aggregates and proteins examined by synergy of NMR experiments and MD simulation
The structure-function paradigm, postulating that protein structures regulate their biological functions, is based on structural biology techniques that enable protein structure determination. However, a large fraction of biomolecular systems, such as disordered proteins, cellular membranes and …
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Characterization of an Amphipathic Alpha-Helix in the Membrane Targeting and Viral Genome Replication of Brome Mosaic Virus
… This study examined the possible role of an amphipathic α-helix, helix B, in BMV 1a's membrane association. Deletion or single substitution of multiple amino acids of helix B abolished BMV 1a's localization to nuclear ER membranes. Additional reporter-based, gain-of-function assays showed …
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Overcoming the plasma membrane barrier: uptake of amphipathic cell-penetrating peptides induces influx of calcium ions and downstream responses
Mitmed potentsiaalsed ravimid ning bioaktiivsed ühendid, mis on lahuses efektiivsed, ei ole kahjuks võimelised läbima rakumembraani ja ei ole seetõttu kasutatavad elusrakkude korral, kus need peaksid oma toimet avaldama. Samas on rakumembraani barjääri ületamiseks välja töötatud mitmeid meetoteid. …
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Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors
… onto a variety of core scaffolds including amphipathic benzene, bicyclo[2.2.2]octane, and urea, resulting in three different series of compounds that could be utilized as coactivator binding inhibitors (CBIs). A fluorescence-based assay was used to evaluate the ability of the CBIs to …
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HAMP Domain and Signaling Mechanism of the Aer Protein
… The Aer HAMP domain is proposed to contain three amphipathic helices. The first amphipathic sequence (residues 207-233) was required for proper folding of the N terminus of Aer. Mutations that abolished FAD binding were clustered in the second putative amphipathic helix (residues 234-251), whereas …
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Deterministic design of peptide-membrane interactions
… their fundamental structural motif: they are amphipathic and cationic. Generic electrostatic and hydrophobic interactions between a cationic, amphipathic AMP and a cell membrane lead to strong binding between the peptide and membrane and subsequent partial insertion of the peptide into the …
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Synthesis and Polymerization of Substituted Stilbenes with Maleic Anhydride for Membrane Solubilization and Protein Extraction
… isolation has been alleviated by use of amphipathic polymers that stabilize proteins by maintaining the native protein environment. Of these amphipathic copolymers, SMA2000—a commercially available styrene-maleic anhydride copolymer with a 2:1 styrene to maleic anhydride ratio—has …
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Mutagenic effects on protein folding and stability
… 5-sheet and have the binary pattern of an amphipathic -sheet. Switching two residues in this region (NL11, LN12) results in the formation of two right-handed 310-helices and changes the binary pattern to that of an amphipathic helix. Arc NL11 has an ambiguous binary pattern and is in …
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Structure and activity of human clusterin.
… non specific affinity for markedly hydrophobic/amphipathic ligands including terminal complement components, Alzheimer's disease amyloid beta (Abeta) peptides, and apo AI-HDL in addition to immunoglobulins, TGFbeta receptors, heparin and the endocytic receptor LRP2. Little is known of clusterin …
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Biophysical characterization of the Escherichia coli RNA degradosome
… of the RNA degradosome, RNase E, contains an amphipathic alpha helix that recruits the degradosome to the cytoplasmic membrane. Investigations on the membrane binding properties of the RNase E as well as the RNA unwinding properties of RhlB were performed in this study. Total internal …
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Biochemical and structural studies of the FtsZ:FtsA complex and polymerising abilities of the FtsA protein
… C-terminal motif, which is predicted to form an amphipathic helix and has been shown to localise FtsA (and with it FtsZ) to the membrane. FtsA belongs to the actin/HSP70 family of proteins, although its fold was shown to deviate by a subdomain deletion and addition. Many members of this family …
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Functional characterisation of the human mitochondrial ATP-Mg/Pi carriers and their disease-causing variants
… responsive to extra-mitochondrial calcium, an amphipathic helix, and a mitochondrial carrier domain, which catalyses substrate transport. In the proposed “locking-pin” mechanism, the amphipathic helix is bound to the regulatory domain in the presence of calcium, whereas it is bound to the …
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Incorporation and analysis of bilayer constituents in nanodiscs
… composed of a lipid bilayer and two surrounding amphipathic proteins, have been utilized to house and solubilize integral membrane proteins and other molecules with large hydrophobic groups which limit their aqueous solubility. In the experiments described herein, lipids from the Nanodiscs’ …
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Holin-dependent secretion of a large clostridial cytotoxin by C. perfringens
… cell-surface biotinylation to determine if the amphipathic helix of TpeE changes its orientation in the presence of TpeL. Using FAST fluorescence, the mean pixel intensity for each frame did not change between TpeE-FAST and TpeE-FAST TpeL cultures, using a membrane impermeable dye. This …
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Synthesis and solid state F-NMR studies on fluorine-labeled antimicrobial peptide RK-21
… peptide LL-37, which is α-helical, cationic and amphipathic in nature. RK-21 displays similar antimicrobial activity to LL- 37. In order to understand the mechanism of lipid bilayer disruption, fluorine-labeled antimicrobial peptide RK-21 was chemically synthesized and 19F-NMR studies were done. …
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The Role of DNA Binding in Transcription Activation by Estrogen Receptor
… of a well defined, synthetic 18 amino acid amphipathic helix into the hinge region of the Xenopus estrogen receptor (XER). The resulting mutant, XER/2AH, provides us with a useful tool to study the mechanisms of gene activation by estrogen. XER/2AH exhibited 2-3 fold increased …
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Design, Synthesis, and Characterization of Glycodendrons Through Small Molecule and Linear Polymer Models
… that would lead to success of more complicated amphipathic polymer-polymer coupling reactions. The first chapter provides an introductory overview of the importance and applications of glycopolymers, bioimaging, and Janus dendrimersomes. The second chapter presents the synthetic methods for …
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Engineering membrane-selective antibiotic peptides to combat multidrug resistance
… networks, in the context of alpha-helical amphipathic cationic peptides, dictates both the selectivity and mechanism of membrane lysis. We further harnessed our results to develop an algorithm for the design of a new generation of non-toxic, bacterial-selective StAMPs for clinical …
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