Abstract Glycosylation patterns in antibodies critically determine biological and physical properties but their precise control is a significant challenge biology biotechnology. We describe herein the optimization of an endoglycosidase‐catalyzed glycosylation best‐selling biotherapeutic Herceptin, anti‐HER2 antibody. Precise MS analysis intact four‐chain Ab heteromultimer reveals nonspecific, non‐enzymatic reactions (glycation), which are not detected under standard denaturing conditions....

Protein endoglycosidases are useful for biocatalytic alteration of glycans on protein surfaces, but the currently limited selectivity has prevented effective manipulation certain N-linked widely found in nature. Here we reveal that a bacterial endoglycosidase from Streptococcus pyogenes , EndoS, is complementary to other known (EndoA, EndoH) used current remodeling. It allows processing complex-type +/- core fucosylation does not process oligomannose- or hybrid-type glycans. This activity...

Febrifugine (1), a quinazoline alkaloid, isolated from Dichroa febrifuga roots, shows powerful antimalarial activity against Plasmodium falciparum. The use of 1 as an drug has been precluded because side effects, such diarrhea, vomiting, and liver toxicity. However, the potent stimulated medicinal chemists to pursue compounds derived 1, which may be valuable leads for novel drugs. In this study, we synthesized new series febrifugine derivatives formed by structural modifications at (i) ring,...

Red yeast, Xanthophyllomyces dendrorhous is the only yeast known to produce astaxanthin, an anti-oxidant isoprenoid (carotenoid) widely used in aquaculture, food, pharmaceutical and cosmetic industries. The potential of this microorganism as a platform cell factory for production has been recognized because high flux through its native terpene pathway. Recently, we developed multiple gene expression system X. enhanced mevalonate synthetic pathway increase astaxanthin production. In contrast,...

Abstract We quantified the level of backscatter radiation generated from physicians’ heads using a phantom. also evaluated shielding rate protective eyewear and optimal placement eye-dedicated dosimeter (skin surface or behind Pb-eyewear). performed diagnostic X-rays two head phantoms: Styrofoam (negligible radiation) anthropomorphic (included radiation). Radiophotoluminescence glass dosimeters were used to measure eye-lens dose, with without 0.07-mm Pb-equivalent eyewear. tube voltages 50,...

Quinazolinone type alkaloids, febrifugine (1) and isofebrifugine (2), isolated from Dichroa febrifuga roots, show powerful antimalarial activity against Plasmodium falciparum. Unfortunately, their emetic effect other undesirable side effects have precluded clinical use for malaria. Because of potency, analogues were searched for, with the goal preserving strong activity, while dramatically reducing effects. We expected that compounds useful in drug development would exist metabolites derived...

Red yeast, Xanthophyllomyces dendrorhous (Phaffia rhodozyma) is the only yeast known to produce astaxanthin, an anti-oxidant isoprenoid (carotenoid) that widely used in aquaculture, food, pharmaceutical and cosmetic industries. Recently, potential of this microorganism as a platform cell factory for production has been recognized because high flux through its native terpene pathway. Addition mevalonate, common precursor biosynthesis, shown be critical enhance astaxanthin content X....

Abstract Glycosylation patterns in antibodies critically determine biological and physical properties but their precise control is a significant challenge biology biotechnology. We describe herein the optimization of an endoglycosidase‐catalyzed glycosylation best‐selling biotherapeutic Herceptin, anti‐HER2 antibody. Precise MS analysis intact four‐chain Ab heteromultimer reveals nonspecific, non‐enzymatic reactions (glycation), which are not detected under standard denaturing conditions....

α-Mannosides made easy: Mutation of a family-GH31 α-glucosidase that displays plasticity to alterations at the 2-OH position donor substrates created an efficient α-mannoside-synthesizing biocatalyst. A simple fluoride reagent was used for synthesis range mono-α-mannosylated conjugates using α-mannosynthase displaying low (unwanted) oligomerization activity.

A novel class of PPARγ ligand 1 (EC50 = 197 nM) with a dibenzoazepin scaffold was identified through high-throughput screening campaign. To avoid the synthetically troublesome chiral center 1, its conformational analysis using MacroModel conducted, focusing on flip tricyclic ring and restriction by methyl group at center. On basis this analysis, hopping dibenzoazepine into dibenzo[ b, e]oxepine replacing structures corresponding olefinic E/ Z isomers performed. Consequently, 9 developed...

This study presents a simple, accurate, and selective bioanalytical method of bevacizumab detection from plasma samples based on aptamer affinity purification⁻high-temperature reversed-phased liquid chromatography (HT-RPLC) with fluorescence detection. Bevacizumab in was purified using magnetic beads immobilized an anti-idiotype DNA for bevacizumab. The separated HT-RPLC detected its native fluorescence. Using beads, selectively as single peak the chromatogram. achieved good separation sharp...

The structure of zeolite UTM-1 has been determined from synchrotron X-ray powder diffraction pattern by direct methods and Rietveld refinement. framework consists pocket-like cages connected sharing eight-membered rings forming one-dimensional channels. can be completely described the assembly chains 58 cages. Identical are found in MFI topology; zeolites ZSM-5 distinguished each another way assembled.

α-Mannoside synthetisierende Biokatalysatoren wurden durch Mutation einer α-Glucosidase der GH31-Familie erhalten. Diese zeigt Plastizität gegenüber Veränderungen an 2-OH-Position von Donorsubstraten. Ein Fluorid-Donorreagens ergab mithilfe dieser α-Mannosynthase, die eine niedrige (unerwünschte) Oligomerisierungsaktivität aufweist, mehrere mono-α-mannosylierte Konjugate.

To investigate the structural dynamics of homology pairing polymers, we modeled scenario homologous chromosome pairings during meiosis in Schizosaccharomyces pombe, one simplest model organisms eukaryotes. We consider a simple consisting pairs polymers with same structures that are confined cylindrical container, which represents local parts chromosomes contained an elongated nucleus S. pombe. Brownian simulations this showed excluded volume effects among non-homological and transitional...

Red yeast, Xanthophyllomyces dendrorhous (Phaffia rhodozyma) is the only yeast known to produce astaxanthin, an anti-oxidant isoprenoid (carotenoid) that widely used in aquaculture, food, pharmaceutical and cosmetic industries. Recently, potential of this microorganism as a platform cell factory for production has been recognized because high flux through its native terpene pathway. Addition mevalonate, common precursor biosynthesis, shown be critical enhance astaxanthin content X....

After the Fukushima nuclear power plant accident in 2011, many types of survey meters were used, including Geiger-Müller (GM) meters, which have long been used to measure β-rays. Recently, however, a novel radiation meter that uses plastic-scintillation sensor has developed. Although manufacturers' catalog data are available for these there no user reports on performance. In addition, performance commercial not evaluated. this study, we experimentally compared with GM meter. The results show...

A simple and readily avalable DNA cleaving agent, 2, 2'-bis(aminomethyl)-4, 4'-bithiazole at 50 μM concentration showed a significant activity for plasmid only in the presence of Cu(II) under physiological conditions without any reducing agents.

To investigate the structural dynamics of homology pairing polymers, we mod- eled scenario homologous chromosome pairings during meiosis in Schizosaccharomyces pombe, one simplest model organisms eukaryotes. We consider a simple consist- ing pairs polymers with same structures that are confined cylindrical container, which represents local parts chromosomes contained an elongated nucleus S. pombe. Brownian simulations this showed excluded volume effects among non-homological and transitional...