The human aldo-keto reductase AKR1B10, originally identified as an aldose reductase-like protein and small intestine reductase, is a cytosolic NADPH-dependent that metabolizes variety of endogenous compounds, such aromatic aliphatic aldehydes dicarbonyl some drug ketones. enzyme highly expressed in solid tumors several tissues including lung liver, has received considerable interest relevant biomarker for the development those tumors. In addition, AKR1B10 been recently reported to be...

We report a method for the synthesis of N-protected staurosporinones, which are useful indolo[2,3-a]pyrrolo[3,4-c]carbazole alkaloids and related compounds. An interaction gramine methiodide (2) with 3-(N-benzyl)indolylacetonitrile (3) in presence t-BuLi, followed by CF3COOH-catalyzed intramolecular indole−indole coupling dehydrogenation DDQ, produced 5-cyanoindolo[2,3-a]carbazole 6 almost quantitatively. Reduction its cyano group N-benzylation N-benzylaminomethylindolo[2,3-a]carbazole 8b,...

Abstract The synthesis of a 3‐arylisoquinoline alkaloid, decumbenine B, was accomplished in reaction sequence based on the formation an indolizine ring {dibenz[ , f ]indolizin‐5(7 H )‐one} followed by its cleavage at amide bond, starting with interaction 5,6‐(methylenedioxy)isoquinoline 2‐bromo‐5,6‐(methylenedioxy)benzoyl chloride presence Bu 3 SnH.(© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2007)

Evolution is, in a sense, to resolve optimization problems. Our neo-Darwinian algorithm based on the mechanics of inheritance and natural selection uses double-stranded DNA-type genetic information "knap-sack problem." The with asymmetrical mutations due semiconservative replication most effectively resolved problem. results strongly suggest that disparity caused by asymmetric machinery DNA promotes evolution, particular diploid organisms high mutation rate, small population, under strong pressure.

Novel indazole derivatives were prepared and evaluated for their biological activity cardiovascular safety profile as human β3-adrenergic receptor (AR) agonists. Although the initial hit compound 5 exhibited significant β3-AR agonistic (EC50 = 21 nM), it also at α1A-AR 219 nM, selectivity: α1A/β3 10-fold). The major metabolite of 5, which was an oxidative product 3-methyl moiety, gave a clue to strategy improvement selectivity versus activity. Thus, modification 3-substituent moiety...

We previously discovered that indazole derivative 8 was a highly selective β3-adrenergic receptor (β3-AR) agonist, but it appeared to be metabolically unstable. To improve metabolic stability, further optimization of this scaffold carried out. focused on the sulfonamide moiety scaffold, which resulted in discovery compound 15 as potent β3-AR agonist (EC50 = 18 nM) being inactive β1-, β2-, and α1A-AR (β1/β3, β2/β3, α1A/β3 > 556-fold). Compound showed dose-dependent β3-AR-mediated responses...

With a remarkable increase in genomic sequence data of wide range species, novel tools are needed for comprehensive analyses the big data. Self-organizing map (SOM) is powerful tool clustering high-dimensional on one plane. For oligonucleotide compositions handled as data, we have previously modified conventional SOM genome informatics: BLSOM. In present study, constructed BLSOMs fragment sequences (e.g. 100 kb) from vertebrates, including coelacanth, and found that were clustered primarily...

The symmetrical and unsymmetrical title compounds 3 4 were prepared by intermolecular photocycloaddition of 1,3,5‐trivinylbenzene in 1% yield. ratio paddlanes was 24:76, i.e. nearly a statistical one.

Abstract Indolo[2,1‐ a ]isoquinoline alkaloids and related compounds have been known to interesting biological activities, such as antileukemic antitumor activities. We found that 1‐(3,4‐dimethoxyphenethyl)indole gave 2,3‐dimethoxyindolo[2,1‐ 1‐(3,4‐dimethoxyphenylacetyl)indole 2,3‐dimethoxy‐6‐oxoindolo[2,1‐ ]isoquinoline, respectively, by an intramolecular cyclization carried out in boiling trifluoroacetic acid.

A boy developed contractures of the Achilles tendons at 3 years and postcervical muscles 7 years, although neither elbows nor cardiac abnormality were recognized by age 9 years. Muscle computed tomography scanning revealed changes characteristic muscle involvement. Emerin was not detected in biopsied muscle, RT-PCR PCR-based genomic DIMA analyses emerin gene demonstrated no amplification product patient. These results confirmed diagnosis X-linked Emery-Dreifuss muscular dystrophy (EDMD),...

Secretory IgA was isolated from feline bile, using ammonium sulphate precipitation, gel-filtration chromatography and affinity chromatography. It formed a precipitating line between anti-cat whole serum or bile by immunoelectrophoresis double diffusion. consisted of three subunits that molecular weight were 80 kd, 62 kd 27 SDS-PAGE analysis. The protein equivalent to secretory component human other animals. Immunoglobulin levels observed on collected continuously gallbladder cannulation in...

A crude extract from Aureobasidium had β-glucosidase activity, hydrolysing cello-biose, methyl-β-D-glucoside, lactose, carboxymethylcellulose, avicel, o-nitrophenyl-β-D-glucoside and p-nitrophenyl-β-D-glucoside, favourable properties such as high pH thermal stabilities. The optimum temperature of the cello-biase activity were 4 80°C, respectively. cellobiase was stable at 3–7 to 7.8 for least 3 h, retained 34 78% its original 1.5 9, Cellobiase 80°C 15 min, 81% 85°C.

We propose "Evolutionary System Theory" as a unified approach practically applicable for the real world problems such real-time adaptive control and mass genetic information analysis. also "Disparity Hypothesis" on gene replication mechanism of an organism with double stranded DNA that postulates disparity fidelity between error leading strand lagging strand. Our assertion is by taking advantages could evolve rapidly acquire robustness even under fluctuating environmental conditions. To...

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