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Protein Engineering with Biosynthesized Libraries from

by Bordetella Bronchiseptica Bacteriophage, Tom Z. Yuan, Cathie M. Overstreet, Issa S. Moody, Gregory A. Weiss , 2013
"... Phage display offers a powerful approach to engineer protein affinity. A naturally occurring analog to phage display, the Bordetella bronchiseptica bacteriophage (BP) employs a highly variable protein termed the major tropism determinant (Mtd) to recognize its dynamic host. Propagation of BP provide ..."
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specific binding to the target T4 lysozyme with dissociation constants in the sub-micromolar range. The results guide future experiments with SMPLs applied to protein engineering.

Differential in vitro activity of the DNA topoisomerase inhibitor idarubicin against Trypanosoma rangeli and Trypanosoma cruzi

by Charles Anwuzia-iwegbu, Ama Banful, Emma Bosier, Mubeen Iqbal, Kelly Jones, Suzanne J Lecutier, Matt Redmond, Andrew Ross-parker, Emily Ward, Paul Wernham, Eleanor M Whidden, Kevin M Tyler, Dietmar Steverding
"... In this study the effect of eight DNA topoisomerase inhibitors on the growth Trypanosoma rangeli epimastigotes in cell culture was investigated. Among the eight compounds tested, idarubicin was the only compound that displayed promising trypanocidal activity with a half-maximal growth inhibition (GI ..."
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(GI 50) value in the sub-micromolar range. Fluorescence-activated cell sorting analysis showed a reduction in DNA content in T. rangeli epimastigotes when treated with idarubicin. In contrast to T. rangeli, against Trypanosoma cruzi epimastigotes idarubicin was much less effective exhibiting a GI 50

In vitro selection of allosteric ribozymes: theory and experimental validation.

by Nicolas Piganeau , Vincent Thuillier , Michael Famulok - J. Mol. Biol. , 2001
"... In vitro selection techniques offer powerful and versatile methods to isolate nucleic acid sequences with speci®c activities from huge libraries. We describe an in vitro selection strategy for the de novo selection of allosteric self-cleaving ribozymes responding to pe¯oxacin and other quinolone de ..."
Abstract - Cited by 5 (2 self) - Add to MetaCart
derivatives. Within 16 selection cycles, highly sensitive clones responding to drug levels in the sub-micromolar range were obtained. The morpholine moiety of the quinolone derivatives was required for inhibition of the self-cleavage of the selected ribozymes: modi®cations of the aromatic system were

Key words: P-type ATPase — Active ion transport

by R. Stimac, F. Kerek, H. -j. Apell, Styryl Dye , 2005
"... Abstract. The previously reported class of potent inorganic inhibitors of Na,K-ATPase, named MCS factors, was shown to inhibit not only Na,K-ATPase but several P-type ATPases with high potency in the sub-micromolar range. These MCS factors were found to bind to the intracellular side of the Na, K-AT ..."
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Abstract. The previously reported class of potent inorganic inhibitors of Na,K-ATPase, named MCS factors, was shown to inhibit not only Na,K-ATPase but several P-type ATPases with high potency in the sub-micromolar range. These MCS factors were found to bind to the intracellular side of the Na, K

Complexes. A Highly Permeable Cationic Platinum(II) Compound with Promising Anticancer Properties

by Malgorzata Frik, Oscar Gonzalo, Víctor Mangas-sanjuan, Alfonso Serrano Del Valle, Chunhua Hu, Marival Bermejo, Isabel Marzo, María Contel
"... ABSTRACT: New organometallic gold(III) and platinum(II) complexes containing iminophosphorane ligands are described. Most of them are more cytotoxic to a number of human cancer cell lines than cisplatin. Cationic Pt(II) derivatives 4 and 5, which differ only in the anion, Hg2Cl6 2 − or PF6 respectiv ..."
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respectively, display almost identical IC50 values in the sub-micromolar range (25−335-fold more active than cisplatin on these cell lines). The gold compounds induced mainly caspase-independent cell death, as previously reported for related cycloaurated compounds containing IM ligands. Cyclo

Detection of noncovalent complexes in biological samples by intensity fading and high-mass detection MALDI–TOF mass spectrometry

by Oscar Yanes, Alexis Nazabal, Ryan Wenzel, Renato Zenobi, Francesc X. Aviles - J. Proteome Res
"... Matrix-assisted laser desorption/ionization (MALDI) mass spectrometry has not yet contributed widely to the study of intact noncovalent biomolecular complexes, because MALDI is known to cause dissociation of the interaction partners and induce formation of nonspecific aggregates. Here, we present a ..."
Abstract - Cited by 2 (0 self) - Add to MetaCart
the overall concentrations of the analytes (nonbinding molecules, protease inhibitor and target enzyme) present in a biological sample of interest are kept at low concentrations, in the sub-micromolar range. Higher concentrations may lead to unspecific interactions and the formation of aggregates both during

An unusual helix turn helix motif in the catalytic core of HIV-1 integrase binds viral DNA and LEDGF

by Hayate Merad, Horea Porumb, Loussiné Zargarian, Brigitte René, Zeina Hobaika, Richard G, Olivier Mauffret, Serge Ferm - PLoS One , 2009
"... Background: Integrase (IN) of the type 1 human immunodeficiency virus (HIV-1) catalyzes the integration of viral DNA into host cellular DNA. We identified a bi-helix motif (residues 149–186) in the crystal structure of the catalytic core (CC) of the IN-Phe185Lys variant that consists of the a 4 and ..."
Abstract - Cited by 5 (2 self) - Add to MetaCart
motif structure thanks to the mutual intramolecular interactions of the a4 and a5 helices that maintain the fold. The main properties are the binding to: 1- the processing-attachment site at the LTR (long terminal repeat) ends of virus DNA with a Kd (dissociation constant) in the sub-micromolar range; 2

MagicWand: A Single, Designed Peptide That Assembles to Stable, Ordered

by unknown authors , 2008
"... ABSTRACT: We describe a straightforward single-peptide design that self-assembles into extended and thickened nano-to-mesoscale fibers of remarkable stability and order. The basic chassis of the design is the well-understood dimeric R-helical coiled-coil motif. As such, the peptide has a heptad sequ ..."
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and the central half anionic with lysine and glutamate, respectively, at core-flanking e and g positions. This +,-,-,+ arrangement gives the peptide its name, MagicWand (MW). As judged by circular dichroism (CD) spectra, MW assembles to R-helical structures in the sub-micromolar range and above. The thermal

Insights into enzyme structur by amide H/D exchange

by Laura S. Busenlehnera
"... in re ne 5 Conformational changes and protein dynamics play an important role in the catalytic efficiency of enzymes. Amide H/D exchange mass spectrometry (H/D exchange MS) is emerging as an efficient technique to study the local and global changes in pro-emerging as an attractive technique that has ..."
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MS) has certain advantages in that there is no practical size limitation to the protein, the working protein concentrations can be in the sub-micromolar range, and the technique can be easily

RIB

by unknown authors
"... A prerequisite of calcium signaling is the maintenance of cytoplasmic free Ca2+ within a narrow, sub-micromolar range, compatible with cell viability. A variety of stress inducing agents and drugs can lead to a disruption of calcium homeostasis with ensuing toxicity. Amiodarone, an anti-arrhythmic d ..."
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A prerequisite of calcium signaling is the maintenance of cytoplasmic free Ca2+ within a narrow, sub-micromolar range, compatible with cell viability. A variety of stress inducing agents and drugs can lead to a disruption of calcium homeostasis with ensuing toxicity. Amiodarone, an anti
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