Abstract: The disclosure provides compositions, methods, and devices for use in delivering Mitomycin-C(MMC), an antineoplastic chemotherapy drug often used for bladder instillations to treat bladder cancer, which degrades in both acidic and alkaline environments. The disclosure provides a solution of buffered MMC (or a different drug) in 50% propylene glycol that maintains a pH from 7.0 to 8.0 when introduced into acidic solutions (pH of 5.0) and is stable when stored at 2-8° C. for greater than 134 days. This formulation can be produced in an FDA registered 503B Outsourcing facility in a pre-filled, ready-to-administer syringe kit with pre-attached closed system transfer device and accessories required for bladder instillation.

Abstract: Use of a stereoselective transaminase in the asymmetric synthesis of a chiral amine. In particular, provided is use of a polypeptide in the production of a chiral amine or a downstream product using a chiral amine as a precursor. Further provided is a method for producing a chiral amine, comprising culturing a strain expressing the polypeptide so as to obtain a chiral amine. Further provided are a chiral amine production strain and a method for constructing the chiral amine production strain. The stereoselective transaminase has a broad substrate spectrum and thus has a broad application potential in the preparation of a chiral amine.

Abstract: Provided herein are maytansinoid compounds, derivatives thereof, conjugates thereof, and methods of treating or preventing proliferative diseases with the same.

Abstract: This disclosure relates to the isolation and sequencing of nucleic acid molecules that encode cytochrome P450 polypeptides from a Papaver somniferum cultivar; uses in the production of noscapine and identification of poppy cultivars that include genes that comprise said nucleic acid molecules.

Abstract: Synthesis and characterization of novel crystalline mitomycin C forms suitable for pharmaceutical compositions in drug delivery systems to treat human or warm-blooded diseases.

Abstract: The disclosure provides biocatalysts that halogenate complex chemical compounds in specific and predictable ways. Also disclosed are halogenated complex organic compounds. The disclosure further provides methods for the halogenation of complex chemical compounds and methods of inhibiting the contraction of smooth muscle in mammals.

Abstract: The invention relates to a new enantioselective process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a ?-amino-?-biphenyl-?-methylalkanoic acid, or acid ester, backbone.

Abstract: The present invention relates to a method and a device for fermentation based on a microbial asexual reproduction. The method comprises the steps of adding plural silica sands, a medium and a microorganism into a tank; and stirring for separating a cluster of the microorganism by a shear force generated from the plural silica sands and returning the microorganism to a logarithmic growth phase without undergoing a spore phase to increase a fermentation rate of the microorganism. The device comprises a tank, a speed control motor disposed outside the tank, a stirring component connected to the speed control motor, a refluxing mechanism for high pressure air and water connected to the tank, a heating unit disposed in the tank and a pumping motor connected to the tank.

Abstract: The present invention relates to methods of testing medications to evaluate authenticity and identify counterfeits. The testing methods employ a reactive system comprising a solvent and an acid. Optionally, the reactive system can also comprise an organometallic agent. The testing methods can provide rapid results verifying the authenticity of an antimalarial medication. Further the test method can provide clear results that can be implemented and interpreted without special training, anywhere in the world. The test methods can offer quantitative and qualitative results. The test methods are based on reactions that yield different colors where the color can indicate the presence of an active ingredient, and the intensity of the color can indicate the concentration of the active ingredient.

Abstract: Provided are a Streptomyces (Streptomyces hygroscopicus) HS7523 and a method for preparing milbemycin A3 by culturing the Streptomyces. The Streptomyces (Streptomyces hygroscopicus) HS7523 is deposited in “China General Microbiological Culture Collection Center” with an accession number of CGMCC No. 9672 on Sep. 16, 2014.

Abstract: The present invention provides methods for catalyzing the conversion of an olefin to any compound containing one or more cyclopropane functional groups using heme enzymes. In certain aspects, the present invention provides a method for producing a cyclopropanation product comprising providing an olefinic substrate, a diazo reagent, and a heme enzyme; and admixing the components in a reaction for a time sufficient to produce a cyclopropanation product. In other aspects, the present invention provides heme enzymes including variants and fragments thereof that are capable of carrying out in vivo and in vitro olefin cyclopropanation reactions. Expression vectors and host cells expressing the heme enzymes are also provided by the present invention.

Abstract: The present invention relates to a composition for, inter alia, preventing or treating a climacteric disease, or preventing or improving a climacteric skin symptom comprising a soybean extract comprising coumestrol as an active ingredient, and more specifically relates to a composition for, inter alia, preventing or treating a climacteric disease, or preventing or improving a climacteric skin symptom comprising a germinated and fermented soybean extract comprising coumestrol as an active ingredient.

Abstract: The present disclosure relates to non-naturally occurring monooxygenase polypeptides useful for preparing prazole compounds, polynucleotides encoding the polypeptides, and methods of using the polypeptides.

Abstract: Synthetic nanostructures, polypeptides that are useful, for example, in making synthetic nanostructures, and methods for using such synthetic nanostructures are disclosed herein.

Abstract: The present disclosure provides engineered transaminase polypeptides useful for the synthesis of chiral amine compounds under industrially relevant conditions. The disclosure also provides polynucleotides encoding the engineered transaminase polypeptides, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases for the production of chiral amine compounds.

Abstract: The invention is directed to immobilized transaminases and methods of making and using them.

Abstract: The disclosure generally relates to the fields of synthetic organic chemistry. In particular, the present disclosure relates to methods and systems for the imidation of sulfides.

Abstract: An isolated novel polynucleotide comprising a nucleotide sequence encoding at least one polypeptide involved in biosynthesis of pyripyropene A, a recombinant vector comprising the polynucleotide and a transformant comprising the polynucleotide are disclosed. By the present invention, a pyripyropene A biosynthetic gene useful for production of a novel pyripyropene analog, improvement of productivity of a pyripyropene A-producing bacterium, production of an insecticidal agent for microorganisms, creation of a plant resistant to insect pests or the like are provided.

Abstract: The present invention has its object to provide a method for producing an L-amino acid comprising reacting a keto acid with an amino acid dehydrogenase and an enzyme having coenzyme regenerating ability to convert to a L-amino acid, wherein a coenzyme is added in two or more portions in the reaction. The method of the present invention enables efficient production of an L-amino acid useful as a synthetic intermediate such as a pharmaceutical intermediate with high optical purity by an enzymatic reductive amination independent of the purity of the keto acid used as a substrate.

Abstract: There is provided a method for culturing a microorganism in which a particular polynucleotide or a recombinant vector comprising it/them is introduced with an intermediate compound necessary for biosynthesis of pyripyropene A. The method of the present invention allows for the production of pyripyropene.

Abstract: The present disclosure provides engineered transaminase polypeptides for the production of amines, polynucleotides encoding the engineered transaminases, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases to prepare compounds useful in the production of active pharmaceutical agents. The present disclosure provides engineered polypeptides having transaminase activity, polynucleotides encoding the polypeptides, methods of the making the polypeptides, and methods of using the polypeptides for the biocatalytic conversion of ketone substrates to amine products. The present enzymes have been engineered to have one or more residue differences as compared to the amino acid sequence of the naturally occurring transaminase of Vibrio fluvialis. In particular, the transaminases of the present disclosure have been engineered for efficient formation of chiral tryptamine derivatives from its corresponding prochiral ketone substrates.

Abstract: A pharmaceutical composition comprising a phenyltetrazole derivative of formula (I) or a pharmaceutical acceptable salt thereof is effective in preventing or treating osteoporosis, obesity, diabetes, or hyperlipidemia, by regulating protein TAZ. wherein, A is ethyl or n-butyl; R1 is methyl, —CH2OH, —CO2CH3, —CH2F, —CH(OCH3)2, —CH2OC(?O)CH3, styryl or —CH2OCH2SCH3; R2 is H, Br, —CO2CH3, phenyl, pyridin-2-yl, pyridin-3-yl, or styryl; R3 is H or methyl; X is CH or N; and P is H or —CH(CH3)OCH2CH3.

Abstract: The present invention provides a convenient and efficient process for the preparation of enantiomerically enriched, deuterated secondary alcohols without reducing deuterium incorporation.

Abstract: The present invention provides a process for the preparation of enantiomerically enriched, deuterated secondary alcohols of Formula 1-A by employing ketoreductases or carbonyl reductases without reducing deuterium incorporation.

Abstract: The present invention provides a method for producing PQQ using a bacterium belonging to the genera Methylobacterium or Hyphomicrobium, which has been modified to enhance the expression of pqq gene cluster and/or gene(s) encoding a precursor for PQQ biosynthesis.

Abstract: The present disclosure provides engineered proline hydroxylase polypeptides for the production of hydroxylated compounds, polynucleotides encoding the engineered proline hydroxylases, host cells capable of expressing the engineered proline hydroxylases, and methods of using the engineered proline hydroxylases to prepare compounds useful in the production of active pharmaceutical agents. The present disclosure provides engineered proline hydroxylase biocatalysts, polynucleotides encoding the biocatalysts. methods of their preparation, and processes for preparing hydroxylated compounds using these engineered biocatalysts.

Abstract: There is herein described a nanovesicle comprising a bilayer of porphyrin-phospholipid conjugates. Each porphyrin-phospholipid conjugate comprises one porphyrin, porphyrin derivative or porphyrin analog covalently attached to a lipid side chain at one of the sn-1 or the sn-2 positions of one phospholipid. Further, the nanovesicle has a defined regioisomeric ratio of sn-1:sn-2 porphyrin-phospholipid conjugates.

Abstract: Methods for producing phycotoxins from natural sources, wherein the phycotoxins have a definite compositional profile are described herein. In one embodiment, the phycotoxins are produced by cyanobacteria. In one embodiment, the phycotoxins are produced by continuously culturing cyanobacteria under strictly controlled conditions in order to produce a definite compositional profile. In another embodiment, organic nutrients are added to the culture that allows for higher concentrations of neosaxitoxin and saxitoxin or gonyaulatoxins 2 and 3 per weight of the algae. The phycotoxins are isolated primarily from the bacteria but can also be isolated from the culture medium. In one embodiment, the cyanobacteria produce only neosaxitoxin and saxitoxin in a ratio of about 6:1, 5:1, 4:1, or 3:1. In a preferred embodiment, the amount of saxitoxin is less than 20% by weight of the total amount of neosaxitoxin and saxitoxin produced. In another embodiment, the cyanobacteria produce only GTX2 and GTX 3.

Abstract: The present invention provides methods for catalyzing the conversion of an olefin to any compound containing one or more cyclopropane functional groups using heme enzymes. In certain aspects, the present invention provides a method for producing a cyclopropanation product comprising providing an olefinic substrate, a diazo reagent, and a heme enzyme; and admixing the components in a reaction for a time sufficient to produce a cyclopropanation product. In other aspects, the present invention provides heme enzymes including variants and fragments thereof that are capable of carrying out in vivo and in vitro olefin cyclopropanation reactions. Expression vectors and host cells expressing the heme enzymes are also provided by the present invention.

Abstract: The present invention provides a novel method for producing rapamycin by submerged fermentation which comprises cultivating Streptomyces hygroscopicus (CBS 773.72) and mutants thereof. The present invention provides a high yielding mutant culture MTCC5681 from Streptomyces hygroscopicus CBS 773.72. This culture is capable of producing rapamycin more efficiently than the cultures Streptomyces hygroscopicus from sources like ATCC, NRRL etc which have been reported so far.

Abstract: The present disclosure relates to methods of using transaminase polypeptides in the synthesis of chiral amines from prochiral ketones.

Abstract: An object of the present invention is to provide a novel compound useful as an antifungal substance and a method for producing the compound.

Abstract: The present disclosure provides engineered transaminase polypeptides for the production of amines, polynucleotides encoding the engineered transaminases, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases to prepare compounds useful in the production of active pharmaceutical agents. The present disclosure provides engineered polypeptides having transaminase activity, polynucleotides encoding the polypeptides, methods of the making the polypeptides, and methods of using the polypeptides for the biocatalytic conversion of ketone substrates to amine products. The present enzymes have been engineered to have one or more residue differences as compared to the amino acid sequence of the naturally occurring transaminase of Vibrio fluvialis. In particular, the transaminases of the present disclosure have been engineered for efficient formation of chiral tryptamine derivatives from its corresponding prochiral ketone substrates.

Abstract: The present invention is directed to the biosynthetic pathway for a nonribosomal peptide synthetase (NRPS) derived drug and analogs thereof. The invention also discloses polynucleotide sequences useful for heterologous expression in a convenient microbial host for the synthesis of the NRPS derived drug.

Abstract: Methods for producing phycotoxins from natural sources, wherein the phycotoxins have a definite compositional profile are described herein. In one embodiment, the phycotoxins are produced by cyanobacteria. In one embodiment, the phycotoxins are produced by continuously culturing cyanobacteria under strictly controlled conditions in order to produce a definite compositional profile. In another embodiment, organic nutrients are added to the culture that allows for higher concentrations of neosaxitoxin and saxitoxin or gonyaulatoxins 2 and 3 per weight of the algae. The phycotoxins are isolated primarily from the bacteria but can also be isolated from the culture medium. In one embodiment, the cyanobacteria produce only neosaxitoxin and saxitoxin in a ratio of about 6:1, 5:1, 4:1, or 3:1. In a preferred embodiment, the amount of saxitoxin is less than 20% by weight of the total amount of neosaxitoxin and saxitoxin produced. In another embodiment, the cyanobacteria produce only GTX2 and GTX 3.

Abstract: The biosynthesis of fungal bicyclo[2.2.2]diazaoctane indole alkaloids with a wide spectrum of biological activities have attracted increasing interest. Their intriguing mode of assembly has long been proposed to feature a non-ribosomal peptide synthetase, a presumed intramolecular Diels-Alderase, a variant number of prenyltransferases, and a series of oxidases responsible for the diverse tailoring modifications of their cyclodipeptide-based structural core. Until recently, the details of these biosynthetic pathways have remained largely unknown due to lack of information on the fungal derived biosynthetic gene clusters. Herein, we report a comparative analysis of four natural product metabolic systems of a select group of bicyclo[2.2.2]diazaoctane indole alkaloids including (+)/(?)-notoamide, paraherquamide and malbrancheamide, in which we propose an enzyme for each step in the biosynthetic pathway based on deep annotation and on-going biochemical studies.

Abstract: Provided is a novel strain permitting genetic engineering of green sulfur bacteria that synthesize bacteriochlorophyll e. Isolated green sulfur bacterium Chlorobaculum limnaeum strain RK-j-1 with accession number NITE BP-1202; isolated transformed Chlorobaculum limnaeum strain obtained by transformation of strain RK-j-1, preferably Chlorobaculum limnaeum dbchU strain with accession number NITE BP-1203 wherein bchU gene is disrupted; a production method of bacteriochlorophyll f containing a step of cultivating Chlorobaculum limnaeum strain dbchU; and bacteriochlorophyll f obtained by the aforementioned production method.

Abstract: The disclosure relates to a nucleic acid molecule isolated from a Papaver somniferum cultivar that produces the opiate alkaloid noscapine which comprises 10 genes involved in the biosynthesis of opiate alkaloids.

Abstract: The invention provides a microbial eukaryotic cell capable of utilizing C5 sugars, in particular xylose. Another objective of the invention is to provide an improved protein sequence to enable eukaryotic cells to degrade C5 sugars. The present invention thus provides protein comprising an amino acid sequence having at least 75% identity, preferably 80% identity, most preferably 90% identity, most highly preferably 95% identity to SEQ ID NO. 2 or SEQ ID NO. 8 and having xylose-isomerase activity in a eukaryotic cell.

Abstract: The invention relates to a new method for preparing (R)-praziquantel. In the invention, by taking advantage of the high stereo selectivity, site selectivity and region selectivity of an enzyme, an intermediate of a pure optical and chiral (R)-praziquantel are obtained by means of the dynamic kinetic resolution of an enantiomer from the synthesized racemate or derivatives thereof, and the (R)-praziquantel is obtained by using various conventional and mature organic chemical reactions with higher yield. The method of the invention has the potential advantages of easily available raw materials, low cost, environmentally safer process and convenience for large-scale production. Also, the purity of the end product can be more than 98%. By adopting the invention, the quality of the product is improved and a basis for developing high quality of active pharmaceutical ingredients and formulations is established, and thus the pending industrial problem of purifying praziquantel over 30 years becomes solvable.

Abstract: The invention relates to a new method for preparing (R)-praziquantel. In the invention, by taking advantage of the high stereo selectivity, site selectivity and region selectivity of an enzyme, an intermediate of a pure optical and chiral (R)-praziquantel are obtained by means of the dynamic kinetic resolution of an enantiomer from the synthesized racemate or derivatives thereof, and the (R)-praziquantel is obtained by using various conventional and mature organic chemical reactions with higher yield. The method of the invention has the potential advantages of easily available raw materials, low cost, environmentally safer process and convenience for large-scale production. Also, the purity of the end product can be more than 98%. By adopting the invention, the quality of the product is improved and a basis for developing high quality of active pharmaceutical ingredients and formulations is established, and thus the pending industrial problem of purifying praziquantel over 30 years becomes solvable.

Abstract: Provided are processes for the synthesis of amino analogues from ketone starting materials.

Abstract: A process for efficiently producing optically active succinimide derivatives as key intermediates of (3R)-2?-(4-bromo-2-fluorobenzyl)spiro{pyrrolidine-3,4?(1?H)-pyrrolo[1,2-a]pyrazine}-1?,2,3?,5(2?H)-tetraone, which comprises the following reaction steps, and the step 2 is performed by using a non-animal-derived enzyme.

Abstract: The present disclosure relates to non-naturally occurring monooxygenase polypeptides useful for preparing prazole compounds, polynucleotides encoding the polypeptides, and methods of using the polypeptides.

Abstract: The present disclosure relates to polypeptides having transaminase activity, polynucleotides encoding the polypeptides, and methods of using the polypeptides.

Abstract: A triprenyl phenol compound represented by the following formula (II) and (III) and having a thrombolysis-enhancing activity, and an efficient method for producing the triprenyl phenol compound. In formula (II) and (III), R1 represents an aromatic group having as a substituent or as a part of a substituent at least one member selected from the group consisting of a carboxyl group, a hydroxyl group, a sulfonic acid group and a secondary amino group, or an aromatic group which comprises a secondary amino group and may comprise nitrogen; R4 in the general formula (III) represents an aromatic amino acid residue represented by the general formula (III-1) below; X represents —CHY—(CH3)2Z; and Y and Z are respectively —H or —OH or together form a single bond: (III-1) wherein R5 represents a hydroxyl group which may be present or absent; and n represents an integer of 0 or 1.

Abstract: The present invention relates to the production of alkaloids from Liliaceae cell culture.

Abstract: This invention relates to the field of biologically active compounds and specifically to phaeofungins, of the general formula (I) or a pharmacologically acceptable salt, solvate, hydrate or a pharmacologically acceptable formulation thereof, pharmaceutical compositions comprising these compounds, methods for the production of the phaeofungins and their use as fungicide, antibiotic as well as antitumor agent.

Abstract: An object of the present invention is to provide a novel compound useful as an antifungal substance and a method for producing the compound.

Abstract: The invention relates to a method for the amination of at least one keto group in a multicyclic ring system comprising at least one keto group into an amino group, using at least one enzyme E having transaminase activity.