cas 28954-12-3, L(+)-allo-Threonine | Articles data

Articles about 28954-12-3Total 204 be found

Article title
Article abstract
Author
Journal number and time
Download

Noncovalently Functionalized Commodity Polymers as Tailor-Made Additives for Stereoselective Crystallization
Stereoselective inhibition of the nucleation and crystal growth of one enantiomer aided by “tailor-made” polymeric additives is an efficient method to obtain enantiopure compounds. However, the conventional preparation of polymeric additives from chiral monomers are laborious and limited in structures, which impedes their rapid optimization and applicability. Herein, we report a “plug-and-play” strategy to facilitate synthesis by using commercially available achiral polymers as the platform to attach various chiral small molecules as the recognition side-chains through non-covalent interactions. A library of supramolecular polymers made up of two vinyl polymers and six small molecules were applied with seeds in the selective crystallization of seven racemates in different solvents. They showed good to excellent stereoselectivity in yielding crystals with high enantiomeric purities in conglomerates and racemic compound forming systems. This convenient, low-cost modular synthesis strategy of polymeric additives will allow for high-efficient, economical resolution of various racemates on different scales.
Wan, Xinhua,Wang, Zhaoxu,Ye, Xichong,Zhang, Jie
supporting information
p. 20243 - 20248
(2021/08/09)

Mechanism of eukaryotic serine racemase-catalyzed serine dehydration
Eukaryotic serine racemase (SR) is a pyridoxal 5′-phosphate enzyme belonging to the Fold-type II group, which catalyzes serine racemization and is responsible for the synthesis of D-Ser, a co-agonist of the N-methyl-D-aspartate receptor. In addition to racemization, SR catalyzes the dehydration of D- and L-Ser to pyruvate and ammonia. The bifuctionality of SR is thought to be important for D-Ser homeostasis. SR catalyzes the racemization of D- and L-Ser with almost the same efficiency. In contrast, the rate of L-Ser dehydration catalyzed by SR is much higher than that of D-Ser dehydration. This has caused the argument that SR does not catalyze the direct D-Ser dehydration and that D-Ser is first converted to L-Ser, then dehydrated. In this study, we investigated the substrate and solvent isotope effect of dehydration of D- and L-Ser catalyzed by SR from Dictyostelium discoideum (DdSR) and demonstrated that the enzyme catalyzes direct D-Ser dehydration. Kinetic studies of dehydration of four Thr isomers catalyzed by D. discoideum and mouse SRs suggest that SR discriminates the substrate configuration at C3 but not at C2. This is probably the reason for the difference in efficiency between L- and D-Ser dehydration catalyzed by SR.
Goto, Masaru,Hemmi, Hisashi,Ito, Tomokazu,Matsuoka, Mai,Matsushita, Kazuma,Mizobuchi, Taichi,Nasu, Ryoma,Watanabe, Soichiro,Yoshimura, Tohru
(2020/06/08)

A α - amino acid compound synthesis and purification method
The invention relates to a synthesis and purification method for an alpha-amino acid compound. The synthesis and purification method is characterized by comprising the following steps: (1) adding substituted alpha-amino nitrile or a substituted hydantoin-based compound into alkali M(OH)x or metal oxide MxO, adding water or an alcohol and water mixed solvent, and heating for reaction to obtain alpha-amino acid salt; (2) adding ammonium carbonate or ammonium bicarbonate or introducing carbon dioxide into the solution in the step (1), separating to obtain filter liquor and precipitates MxHyCO3, performing reduced pressure concentration on the filter liquor, and recrystallizing in an alcohol solvent to obtain the alpha-amino acid compound (I). The synthesis and purification method for the alpha-amino acid compound is simple, the yield and purity of the obtained alpha-amino acid compound are high; furthermore, recycling utilization and cleaning production of materials can be realized; the synthesis and purification method is especially suitable for synthesis of the alpha-amino acid compound with high water solubility.
-
Paragraph 0069; 0070

(2018/05/16)

Colony-wise Analysis of a Theonella swinhoei Marine Sponge with a Yellow Interior Permitted the Isolation of Theonellamide i
There are several examples of marine organisms whose metabolic profiles differ among conspecifics inhabiting the same region. We have analyzed the metabolic profile of each colony of a Theonella swinhoei marine sponge with a yellow interior and noticed the patchy distribution of one metabolite. This compound was isolated and its structure was studied by a combination of spectrometric analyses and chemical degradation, showing it to be a congener in the theonellamide class of bicyclic peptides. Theonellamides had previously been isolated by us only from T. swinhoei with a white interior and not from those with a yellow interior.
Fukuhara, Kazuya,Takada, Kentaro,Watanabe, Ryuichi,Suzuki, Toshiyuki,Okada, Shigeru,Matsunaga, Shigeki
p. 2595 - 2599
(2018/12/13)

Preparation and purification method of amino acid compound
The invention relates to the field of industrial organic synthesis, in particular to a preparation and purification method of an amino acid compound. The method comprises the following steps that (1)alpha-amino nitrile compounds or hydantoin compounds or mixtures thereof are heated to react to obtain alpha-amino acid salt under the condition that volatile alkali and a suitable solvent exist; (2)after the alpha-amino acid salt obtained in step (1) is distilled, the alpha-amino acid salt is recrystallized in an organic solvent to obtain the alpha-amino acid compound. According to the method, reaction conditions are mild, materials can be recycled, and introduction of metal ions and use of ammonium carbonate salt are avoided, so that post-treatment is simple and no waste salt is generated.
-
Paragraph 0066; 0067

(2018/06/21)

Trading N and O. Part 2: Exploiting aziridinium intermediates for the synthesis of β-hydroxy-α-amino acids
The β-hydroxy-α-amino acids (S,S)-allo-threonine, (S,S)-β-hydroxyleucine and a range of aryl substituted (S,S)-β-hydroxyphenylalanines were prepared from the corresponding enantiopure anti-α-hydroxy-β-amino esters via a rearrangement protocol, which proceeds via the intermediacy of the corresponding aziridinium ions. The starting anti-α-hydroxy-β-amino esters were prepared in >99:1 dr using our diastereoselective aminohydroxylation procedure, whereby conjugate addition of lithium (R)-N-benzyl-N-(α-methylbenzyl)amide to an α,β-unsaturated ester is followed by oxidation of the resultant enolate with (-)-camphorsulfonyloxaziridine. Subsequent activation of the hydroxyl group within the anti-α-hydroxy-β-amino esters promoted aziridinium ion formation [which proceeds with inversion of configuration at C(2)], and regioselective ring-opening of the intermediate aziridinium ions with H2O [which proceeds with inversion of configuration at C(3)] gave the corresponding anti-β-hydroxy-α-amino esters as single diastereoisomers (>99:1 dr). Deprotection of these substrates via sequential hydrogenolysis and ester hydrolysis gave the corresponding β-hydroxy-α-amino acids in good yield and high diastereoisomeric and enantiomeric purity.
Davies, Stephen G.,Fletcher, Ai M.,Frost, Aileen B.,Roberts, Paul M.,Thomson, James E.
p. 5849 - 5862
(2015/03/30)

COMPOUND EXHIBITING REGULATORY ACTIVITY ON LYSOPHOSPHATIDYLSERINE RECEPTOR FUNCTION
The object of the present invention is to provide a compound having a lysophosphatidylserine receptor function modulation activity or a salt thereof. A compound having a lysophosphatidylserine receptor function modulation activity or a salt thereof, or a pharmaceutical composition or a lysophosphatidylserine receptor function moderator containing such compound or salt is provided by the present invention.
-
Paragraph 0217

(2015/12/19)

Stellettapeptins A and B, HIV-inhibitory cyclic depsipeptides from the marine sponge Stelletta sp.
Two new HIV-inhibitory depsipeptides, stellettapeptins A (1) and B (2), were isolated from an extract of the marine sponge Stelletta sp., collected from northwestern Australia. Structures of these cyclic nonribosomal peptides were elucidated on the basis of extensive NMR data analysis, and chemical degradation and derivatization studies. Stellettapeptins contain numerous nonproteinogenic amino acid residues and they are the first peptides reported to contain a 3-hydroxy-6,8-dimethylnon-4-(Z)-enoic acid moiety. Compounds 1 and 2 potently inhibit infection of human T-lymphoblastoid cells by HIV-1RF with EC50 values of 23 and 27 nM, respectively.
Shin, Hee Jae,Rashid, Mohammad A.,Cartner, Laura K.,Bokesch, Heidi R.,Wilson, Jennifer A.,McMahon, James B.,Gustafson, Kirk R.
supporting information
p. 4215 - 4219
(2015/06/22)

SEPARATING AGENT AND MANUFACTURING METHOD THEREOF
An embodiment of the present invention is a separating agent wherein a group represented by a chemical formula of: or a group represented by a chemical formula of: is introduced on a surface thereof.
-
Paragraph 0067; 0068; 0069; 0070; 0071; 0072; 0093; 0094

(2015/01/07)

Ohmyungsamycins A and B: Cytotoxic and antimicrobial cyclic peptides produced by Streptomyces sp. from a volcanic island
Ohmyungsamycins A and B (1 and 2), which are new cyclic peptides, were isolated from a marine bacterial strain belonging to the Streptomyces genus collected from a sand beach on Jeju, a volcanic island in the Republic of Korea. Based on the interpretation of the NMR, UV, and IR spectroscopic and MS data, the planar structures of 1 and 2 were elucidated as cyclic depsipeptides bearing unusual amino acid units, including N-methyl-4-methoxytrytophan, β-hydroxyphenylalanine, and N,N-dimethylvaline. The absolute configurations of the α-carbons of the amino acid residues were determined using the advanced Marfey's method. The configurations of the additional stereogenic centers at the β-carbons of the threonine, N-methylthreonine, and β-hydroxyphenylalanine units were assigned by GITC (2,3,4,6-tetra-O-acetyl- β-d-glucopyranosyl isothiocyanate) derivatization and the modified Mosher's method. We have developed a new method utilizing PGME (phenylglycine methyl ester) derivatization coupled with chromatographic analysis to determine the absolute configuration of N,N-dimethylvaline. Our first successful establishment of the absolute configuration of N,N-dimethylvaline using PGME will provide a general and convenient analytical method for determining the absolute configurations of amino acids with fully substituted amine groups. Ohmyungsamycins A and B showed significant inhibitory activities against diverse cancer cells as well as antibacterial effects.
Um, Soohyun,Choi, Tae Joon,Kim, Heegyu,Kim, Byung Yong,Kim, Seong-Hwan,Lee, Sang Kook,Oh, Ki-Bong,Shin, Jongheon,Oh, Dong-Chan
p. 12321 - 12329
(2014/01/17)

Identification of four new agr quorum sensing-interfering cyclodepsipeptides from a marine Photobacterium
During our search for new natural products from the marine environment, we discovered a wide range of cyclic peptides from a marine Photobacterium, closely related to P. halotolerans. The chemical fingerprint of the bacterium showed primarily non-ribosomal peptide synthetase (NRPS)-like compounds, including the known pyrrothine antibiotic holomycin and a wide range of peptides, from diketopiperazines to cyclodepsipeptides of 500-900 Da. Purification of components from the pellet fraction led to the isolation and structure elucidation of four new cyclodepsipeptides, ngercheumicin F, G, H, and I. The ngercheumicins interfered with expression of virulence genes known to be controlled by the agr quorum sensing system of Staphylococcus aureus, although to a lesser extent than the previously described solonamides from the same strain of Photobacterium.
Kjaerulff, Louise,Nielsen, Anita,Mansson, Maria,Gram, Lone,Larsen, Thomas O.,Ingmer, Hanne,Gotfredsen, Charlotte H.
p. 5051 - 5062
(2014/02/14)

Trading N and O: Asymmetric syntheses of β-hydroxy-α-amino acids via α-hydroxy-β-amino esters
Both diastereoisomers of 2-amino-3-hydroxybutanoic acid and 2-amino-3-hydroxy-3-phenylpropanoic acid have been prepared from enantiopure α-hydroxy-β-amino esters via the intermediacy of the corresponding cis- and trans-aziridines. Aminohydroxylation of two α,β-unsaturated esters produced enantiopure 2,3-anti-α-hydroxy-β-amino esters in >99:1 dr. Subsequent epimerisation at the C(2)-position via a sequential oxidation/diastereoselective reduction protocol gave the corresponding enantiopure 2,3-syn-α-hydroxy-β-amino esters in >99:1 dr. These syn- and anti-substrates were then converted into the corresponding N-Boc protected cis- and trans-aziridines, respectively, via a three step reaction sequence: (i) hydrogenolysis and in situ N-Boc protection; (ii) OH-activation; and (iii) aziridine formation. Subsequent regioselective ring-opening of the C(3)-methyl-aziridines with Cl3CCO2H proceeded with inversion of configuration to give the corresponding 2-amino-3-trichloroacetate esters, whereas the analogous reaction with the C(3)-phenyl-aziridines resulted in rearrangement to the corresponding oxazolidin-2-ones with retention of configuration. In each case, hydrolysis of the products from these ring-opening reactions produced the corresponding enantiopure β-hydroxy-α-amino acids as single diastereoisomers.
Davies, Stephen G.,Fletcher, Ai M.,Frost, Aileen B.,Lee, James A.,Roberts, Paul M.,Thomson, James E.
p. 8885 - 8898
(2013/09/23)

Tataricins A and B, two novel cyclotetrapeptides from Aster tataricus, and their absolute configuration assignment
Two novel cyclotetrapeptides, tataricins A and B, with a unique cyclopeptide backbone and aδ 2,4Pro side chain, were isolated from the traditional Chinese medicine Aster tataricus. Their structures and absolute configurations were determined using a combination of spectroscopic data, the advanced Marfey's method, and a total synthesis. Copyright
Xu, Hui-Min,Yi, Hua,Zhou, Wen-Bing,He, Wen-Jun,Zeng, Gang-Zhi,Xu, Wen-Yan,Tan, Ning-Hua
supporting information
p. 1380 - 1383
(2013/04/23)

Imaging mass spectrometry and genome mining reveal highly antifungal virulence factor of mushroom soft rot pathogen
Soft rot diseases caused by a variety of bacteria account for severe losses in agriculture, devastating fruits, vegetables, and cultivated mushrooms. After bacterial infection, often owing to direct contact or transmission by insects, virulence factors and lytic enzymes cause degradation of plant and mushroom tissues, thereby turning crop into mush. In many cases, the chemical mediators of soft rot diseases have remained elusive, as in the long-known mushroom pathogen Janthinobacterium agaricidamnosum. This motile Gram-negative bacterium has been found to be the causative agent of soft rot disease of the cultured button mushroom, Agaricus bisporus. Typical symptoms of the infection are lesions turning into sticky blotches on the cap surface and a complete dissolution of the mushroom within only a few days (Figure 1A, B). We reasoned that knowledge on the causative agent of the soft rot would have a double benefit. Foremost, it could aid in understanding the pathobiology of the mushroom pathogen, which may be a starting point for protective measures. Second, there is an increasing need for novel antifungals, since the incidents of severe and even lethal fungal infections and resistance towards antifungals are on the rise. We hypothesized that mushroom soft rot bacteria could excrete antifungal agents as virulence factors, which might also be active against human pathogens. Herein we report the discovery and full characterization of a highly antifungal virulence factor from the soft rot pathogen Janthinobacterium agaricidamnosum guided by imaging mass spectrometry and genome mining.
Graupner, Katharina,Scherlach, Kirstin,Bretschneider, Tom,Lackner, Gerald,Roth, Martin,Gross, Harald,Hertweck, Christian
supporting information
p. 13173 - 13177
(2013/03/14)

ETHYNYLBENZENE DERIVATIVES
Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.
-
Page/Page column 100

(2012/03/26)

An efficient route to both enantiomers of allo-threonine by simultaneous amino acid racemase-catalyzed isomerization of threonine and crystallization
We present an efficient method for the production of D- and L-allo-threonine (allo-Thr) with very high purity by enzymatic isomerization of L- or D-threonine (Thr) and simultaneous crystallization. Isomerization of Thr to allo-Thr is catalyzed by a purified amino acid racemase (AArac12996) from Pseudomonas putida NBRC12996, which can easily be obtained from a recombinant E. coli strain by secretion into the medium and subsequent anion exchange chromatography. Crystallization of D- and L-allo-Thr was performed in a repetitive batch mode over a period of up to 55 days at 30 °C. Total amounts of 30.8 g D-allo-Thr and 32.4 g L-allo-Thr were obtained with a very good diastereomeric excess of deD-allo>99.2% and de L-allo>98.4%, respectively, and in good yields (D-allo-Thr: 83%, L-allo-Thr: 79%). The enzyme's remarkable high stability under process conditions resulted in enzyme specific yields of 2.56 g D-allo-Thr per mg AArac12996 and 1.62 g L-allo-Thr per mg AArac12996. In contrast to chemical multi-step syntheses of allo-Thr, our process consists of only one enzyme-catalyzed reaction step with simultaneous product crystallization. The process is performed under low energy consumption (30 °C, atmospheric pressure) in water and avoids the use and production of any toxic or harmful compounds. Recovery of the enantiomerically pure products is performed by simple filtration which reduces downstream processing significantly compared to chromatographic methods which are usually applied. Copyright
Wuerges, Kerstin,MacKfeld, Ursula,Pohl, Martina,Luetz, Stephan,Wilhelm, Susanne,Wiechert, Wolfgang,Kubitzki, Tina
experimental part
p. 2431 - 2438
(2011/11/06)

Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold
Compounds inhibiting LpxC in the lipid A biosynthetic pathway are promising leads for novel antibiotics against multidrug-resistant Gram-negative pathogens. We report the syntheses and structural and biochemical characterizations of LpxC inhibitors based on a diphenyl-diacetylene (1,4-diphenyl-1,3-butadiyne) threonyl-hydroxamate scaffold. These studies provide a molecular interpretation for the differential antibiotic activities of compounds with a substituted distal phenyl ring as well as the absolute stereochemical requirement at the C2, but not C3, position of the threonyl group.
Liang, Xiaofei,Lee, Chul-Jin,Chen, Xin,Chung, Hak Suk,Zeng, Daina,Raetz, Christian R.H.,Li, Yaoxian,Zhou, Pei,Toone, Eric J.
supporting information; experimental part
p. 852 - 860
(2011/03/19)

Preparation of optically active allothreonine by separating from a diastereoisomeric mixture with threonine
A simple procedure is described to obtain D-and L-allothreonine (D-and L-aThr). A mixture of N-acetyl-D-allothreonine (Ac-D-aThr) and N-acetyl-L-threonine (Ac-L-Thr) was converted to a mixture of their ammonium salts and then treated with ethanol to precipitate ammonium N-acetyl-L- threoninate (Ac-L-Thr.NH3) as the less-soluble diastereoisomeric salt. After separating Ac-L-Thr.NH3 by filtration, Ac-D-aThr obtained from the filtrate was hydrolyzed in hydrochloric acid to give D-aThr of 80% de, recrystallized from water to give D-aThr of >99% de. L-aThr was obtained from a mixture of the ammonium salts of Ac-L-aThr and Ac-D-Thr in a similar manner.
Yajima, Tatsuo,Ichimura, Serina,Horii, Shirabe,Shiraiwa, Tadashi
experimental part
p. 2106 - 2109
(2011/06/25)

New polypeptides inducing apoptosis and uses thereof
The present invention concerns a polypeptide comprising the sequence X1WX2X3X4RX5X6X7 X8 X9, and derivatives thereof, wherein X1 is an amino acid selected in the group consisting in histidinc (H), tyrosinc (Y), aspartic acid (D), glutamine (Q), and leucine (L), preferably histidine (H) or tyrosine (Y); X2 is a polar amino acid, charged or not, and selected in the group consisting in serine (S) threonine (T), lysine (K), arginine (R), asparagine (N), aspartic acid (D), cysteine (C), glycine (G), glutamine (Q), histidine (H), and glutamic acid (E); X3 is a polar amino acid, charged or not, and selected in the group consisting in serine (S), threonine (T), asparagine (N), cysteine (C), histidine (H), leucine (L), tyrosine (Y), alanine (A), and isoleucine (1); X4 is an amino acid selected in the group consisting in threonine (T), arginine (R), asparagine (N), alanine (A), isoleucine (I), leucine (L), methionine (M), phenylalanine (F), tryptophane (W), valine (V) and tyrosine; X5 is an amino acid selected in the group consisting in leucine (L), methionine (M), isoleucine (I), tryptophane (W), tyrosine (Y), histidine (H), glutamine (Q), lysine (K), and arginine (R); X6 is an amino acid selected in the group consisting in leucine (L), and glutamic acid (E); X7 is an amino acid selected in the group consisting in cysteine (C), asparagine (N), alanine (A), tyrosine (Y), serine (S), glutamine (Q), and proline (P); X8 is a hydrophobic amino acid selected in the group consisting in alanine (A), isoleucine (I), leucine (L), methionine (M), phenylalanine (F), tryptophane (W), valine (V) and tyrosine; and X9 is a threonine or an hydrophobic amino acid selected in the group consisting in alanine (A), isoleucine (I), leucine (L), methionine (M), phenylalanine (F), tryptophane (W), valine (V) and tyrosine.
-
(2009/02/10)

Compositions and Methods for Binding Lysophosphatidic Acid
Compositions and methods for making and using anti-LPA agents, for example, monoclonal antibodies, are described.
-
(2009/06/27)

Modulating neuronal outgrowth via the major histocompatibility complex class I (MHC I) molecule
The invention relates to methods and compositions for treating neural damage caused by injury or disease, by enhancing neural outgrowth and/or repair responses in the nervous system. Preferably, the methods and compositions utilize agents which interfere with the ability of the major histocompatibility complex (MHC) Class I molecule (MHC I) to inhibit neurite outgrowth. Such agents include antibodies directed to MHC I, MHC I fragments and/or analogs, and agents which interfere with MHC I interaction with its neuronal receptor and the receptor's signaling pathway.
-
(2009/07/10)

METHOD AND COMPOSITIONS FOR TREATING SKIN
A skin care composition comprising at least one keratinocyte CLOCK or PER1 gene activator and at least one DNA repair enzyme; a method for inhibiting damage to human keratinocytes due to environmental aggressors by applying a composition comprising at least one keratinocyte CLOCK or PER1 gene activator and at least one DNA repair enzyme; and a method for repairing DNA damage in human keratinocytes.
-
(2009/09/08)

GEP, a novel chondrogenic growth factor and target in cartilage disorders
The present invention relates to the expression and regulating growth factors in chrondrocytes and developing cartilage, particularly granulin-epithelin precursor (GEP). The invention relates to the modulation and manipulation of these growth factors, GEP, and/or the molecules they interact with, for instance COMP, in cartilage disorders, including arthritis. Assays and screening methods for the determination of the expression and activity of GEP, or of GEP-COMP, are provided, including for screening for the presence or extent of cartilage or arthritic disease and for identifying modulators or compounds/agents for treatment or prevention of cartilage or arthritic diseases.
-
(2009/09/25)

NOVEL ATTENUATED POLIOVIRUS
A novel and stable attenuated poliovirus, which replicates in neuroblastoma cells, is produced by engineering an indigenous replication element (cre), into the 5′ non-translated genomic region and inactivating the native cre element located in the coding region of 2C (mono-crePV). The stably attenuated poliovirus replicates in a neuroblastoma model (Neuro-2aCD155 tumors) expressing CD155, the poliovirus receptor, and is effective for oncolytic treatment and cure of solid tumors, such as neuroblastoma.
-
(2009/10/06)

Cell Model for Alzheimer's Disease Pathology
The present invention encompasses compositions and methods for studying in cell culture the pathologic changes associated with Alzheimer's disease. The present invention further relates to methods for studying and detecting early events in the conversion of healthy neurons to Alzheimer's disease neurons.
-
(2009/12/04)

EPSPS Mutants
The present invention relates to the production of a non-transgenic plant resistant or tolerant to a herbicide of the phosphonomethylglycine family, e.g., glyphosate. The present invention also relates to the use of a recombinagenic oligonucleobase to make a desired mutation in the chromosomal or episomal sequences of a plant in the gene encoding for 5-enol pyruvylshikimate-3-phosphate synthase (EPSPS). The mutated protein, which substantially maintains the catalytic activity of the wild-type protein, allows for increased resistance or tolerance of the plant to a herbicide of the phosphonomethylglycine family, and allows for the substantially normal growth or development of the plant, its organs, tissues or cells as compared to the wild-type plant irrespective of the presence or absence of the herbicide. Additionally the present invention relates to mutant E. coli cells that contain mutated EPSPS genes.
-
(2009/12/24)

Diastereo- And enantioselective synthesis of β-Hydroxy-α-amino acids: Application to the synthesis of a key intermediate for lactacystin
The development of a highly efficient and stereoselective methodology for the preparation of β-hydroxy-α- amino acids is described. Nucleophilic addition of enolates of tricyclic iminolactones 1a and 1b to aldehydes in the presence of 6 equiv of lithium chloride in THF at -78 °C leads to aldol adducts in good yield (63-86%) and high diastereoselectivity (up to >25:1 dr). Subsequently, hydrolysis of the aldol adducts under acidic conditions leads to the corresponding β-hydroxy-a-amino acids in good yields (up to 83%) and excellent enantiomeric excesses (99% ee) with good recovery yields of the chiral auxiliaries 6 and 7. This methodology was applied to the facile synthesis of the key intermediate for lactacystin along with several isomers.
Li, Qiong,Yang, Shao-Bo,Zhang, Zhihui,Li, Lei,Xu, Peng-Fei
supporting information; experimental part
p. 1627 - 1631
(2009/09/24)

Method for the production of high-level soluble human recombinant interferon alpha in e. coli and vectors useful for such a production
Method for the production of high-level soluble human recombinant interferon alpha protein (rhuIFNα) in E. coli and vectors useful for such a production. Said method comprises the steps of: (1) Transforming an E. coli selected in the group consisting of E. coli protease deficient host strains, and E. coli reductase deficient host strains, with a recombinant expression vector comprising the sequence encoding the glutathione-S-transferase (GST), a junction sequence including a recognition site for a specific protease and a sequence able to encode an interferon alpha (IFN alpha) protein under the control of an inducible promoter, said vector encoding a GST-IFN alpha fusion protein (2) Expressing said interferon alpha protein in conditions comprising the induction of the expression with 0.1 mM-0.5 mM IPTG and a growth temperature of 25° and/or 37°C, depending on said E. coli strain and (3) Isolating the expressed IFN alpha protein.
-
(2009/01/20)

Growth Hormone Secretagogue Receptor 1A Ligands
The present invention relates to new growth hormone secretagogue receptor 1A (GHS-R 1A) ligands, and pharmaceutical compositions comprising any of the new GHS-R1 A ligands. The ligands are suitable for a wide range of applications, and thus the present invention also relates to use of the GHS-R1 A ligands according to the present invention in the manufacture of a medicament for the treatment of an individual in need thereof. In another aspect, the present invention relates to a method of treatment of an individual in need thereof, comprising administering to said individual one or more of the GHS-R1A ligands disclosed herein, such as e.g. for treatment of cancer cachexia.
-
(2009/01/20)

Cell-proliferation inhibiting VPg proteins, fragments or analogs thereof and their applications
Use of VPg proteins, fragments or analogs thereof having the ability to bind an eukaryotic initiation factor eIF4E, for inhibiting cell-proliferation.
-
(2009/01/24)

Compositions, kits, and methods relating to the human FEZ1 gene, a novel tumor suppressor gene
The invention relates to isolated polynucleotides homologous with a portion of one strand of the human tumor suppressor gene, FEZ1, and to the tumor suppressor protein encoded thereby, Fez1. The polynucleotides are useful, for example, as probes, primers, portions of expression vectors, and the like. The invention also includes diagnostic, therapeutic, cell proliferation enhancement, and screening methods which involve these polynucleotides and protein. The invention further includes kits useful for performing the methods of the invention.
-
(2008/06/13)

Cell adhesion and extracellular matrix proteins
Various embodiments of the invention provide human cell adhesion and extracellular matrix proteins (CADECM) and polynucleotides which identify and encode CADECM. Embodiments of the invention also provide expression vectors, host cells, antibodies, agonists, and antagonists. Other embodiments provide methods for diagnosing, treating, or preventing disorders associated with aberrant expression of CADECM.
-
(2008/06/13)

Synthesis of γ-halogenated and long-chain β-hydroxy-α-amino acids and 2-amino-1,3-diols using threonine aldolases
The l- and d-threonine aldolase catalyzed formation of γ-halogenated and long-chain l- and d-3-alkylserine-derivatives 1-12, respectively, was shown starting from glycine and halogenated C2- or C4-C12 aldehydes. lTA from Pseudomonas putida accepted all tested aldehydes with strongly varying diastereoselectivity (de up to 93%). Only aldehydes smaller than decanal were converted by dTA from Alcaligenes xylosoxidans with good selectivities (de up to 73%). Utilizing isobutanal enantio- and diastereopure d-syn-2-amino-3-hydroxy-4-methylpentanoic acid was obtained (ee>99%, de>95%), which was converted to the corresponding 2-amino-1,3-diol.
Steinreiber, Johannes,Fesko, Kateryna,Mayer, Clemens,Reisinger, Christoph,Schürmann, Martin,Griengl, Herfried
p. 8088 - 8093
(2008/02/08)

Plant peptide with antimicrobial activity
The invention concerns novel peptides, in particular plant peptides, having an antimicrobial activity and a cytotoxic activity, in particular for plant cells. The invention also concerns polynucleotides coding for said peptides, vectors comprising said polynucleotides, micro-organisms and cells transformed with said vectors, transgenic organisms whereof all of part of the cells contain and/or express said vectors, uses of said peptides and said polynucleotides, in particular as plant-specific antimicrobial agents. The invention further concerns an antimicrobial and/or cytotoxic method for treating plants.
-
(2008/06/13)

Determination of the complete absolute configuration of petriellin A
We report the full structural determination of the depsipeptide petriellin A. The absolute configuration of the amino acid residues, N-methyl isoleucine and N-methyl threonine, have been determined by a combination of HPLC and TLC comparison of synthetic Marfey's derivatives and Marfey's derivatives of the natural product hydrolysate. The configuration of the chiral centres in these two N-methylated residues was found to be the same as those of the common unmethylated l-amino acids. CSIRO 2006.
Aurelio, Luigi,Brownlee, Robert T. C.,Dang, Jason,Hughes, Andrew B.,Polya, Gideon M.
p. 407 - 414
(2008/02/04)

Interleukin-2:remodeling and glycoconjugation of interleukin-2
The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide.
-
(2008/06/13)

Novel protein and use thereof
A novel gene likely inhibiting the onset and progress of cancer. A protein having an amino acid sequence which is the same or substantially the same as the amino acid sequence represented by SEQ ID NO:4 or its salt; a polynucleotide encoding the same; and medicinal use, etc. thereof are provided.
-
(2008/06/13)

Process for producing alpha 2,3/ alpha 2,8-sialyltransferase and sialic acid-containing complex sugar
The present invention can provide a process for producing a protein having α2,3/α2,8-sialyltransferase activity using a transformant comprising a DNA encoding a protein having α2,3/α2,8-sialyltransferase activity derived from a microorganism belonging to the genus Pasteurella and a process for producing a sialic acid-containing complex carbohydrate using a transformant capable of producing a protein having α2,3/α2,8-sialyltransferase activity derived from a microorganism.
-
(2008/06/13)

CIS-ELEMENT REGULATING TRANSCRIPTION, TRANSCRIPTIONAL REGULATORY FACTOR BINDING SPECIFICALLY THERETO AND USE OF THE SAME
The present invention provides a novel fructose responsive transcription control cis-element and a transcriptional regulatory factor that interacts therewith, a non-human animal having them transferred or inactivated, a diagnostic method for genetic susceptibility to a metabolic disorder using them, and a screening method for a prophylactic or therapeutic drug for a metabolic disorder using them.
-
(2008/06/13)

Small peptides having apoptotic activities and their applications
The present invention relates to nine residue peptides (M32-40) from flavivirus M ectodomain able to modulate specifically the apoptotic activity of diverse flavivirus, to pharmaceutical composition comprising the same and their use for the treatment and/or the prevention of flavivirus-linked infections and cancers.
-
(2008/06/13)

Novel enoyl reductases and methods of use thereof
The present provides structurally related enzymes that act as enoyl reductases. These enoyl reductases share a common amino acid consensus sequence, and bind a flavin cofactor. One particular enoyl reductase provided, FabK, catalyzes the identical reaction as the NADH-dependent enoyl-ACP reductase, FabI. Nucleic acids encoding the enoyl reductases, the enoyl reductases, and anitbodies for the enoyl reductases are also included. Methods are also provides for identifying agents that can act to prevent and/or treat bacterial infections.
-
(2008/06/13)

Enzymes derived from thermophilic organisms that function as a chromosomal replicase, preparation and use thereof
The present invention relates to an isolated DNA molecule from a thermophilic bacterium which encodes a DNA polymerase III-type enzyme subunit. Also encompassed by the present invention are host cells and expression system including the heterologous DNA molecule of the present invention, as well as isolated replication enzyme subunits encoded by such DNA molecules. Also disclosed is a method of producing a recombinant thermostable DNA polymerase III-type enzyme, or subunit thereof, from a thermophilic bacterium, which is carried out by transforming a host cell with at least one heterologous DNA molecule of the present invention under conditions suitable for expression of the DNA polymerase III-type enzyme, or subunit thereof, and then isolating the DNA polymerase III-type enzyme, or subunit thereof.
-
(2008/06/13)

ENZYME FOR CLEAVAGE OF THE ANCHOR REGION OF SURFACE PROTEINS FROM GRAM POSITIVE BACTERIA
The invention relates to an enzyme which cleaves surface proteins of gram-positive bacteria, to methods of detecting the enzyme, and methods of isolating the enzyme. In particular, the enzyme is isolated from a group A Streptococcus, and cleaves at the sequence LPXTGX (SEQ ID NO:1). A method for screening putative inhibitors of the enzyme which cleaves the anchor region of surface proteins from gram positive bacteria is also disclosed.
-
(2008/06/13)

Assays for screening compounds which interact with cation channel proteins, mutant prokaryotic cation channel proteins, and uses thereof
Assays for screeing potential drugs or agents that can interact and potentially bind to cation channel proteins, and potentially have uses in treating conditions related to the function of cation channel proteins is provided, along with prokaryotic cation channel proteins mutated to mimic eukaryotic cation channels, which can then be used in assays of the present invention.
-
(2008/06/13)

Peptides of IL-2 and derivatives thereof
The present invention relates to new peptides of IL-2, and derivatives thereof and their use as therapeutic agents.
-
(2008/06/13)

EGF receptor epitope peptides and uses thereof
The present invention relates generally to growth factor receptor epitope peptides, particularly EGF family receptor epitope peptides. The invention also relates to the use of the receptor peptides in generating antibodies which have anti-tumor or anti-cancer activity or in stimulating an immunological response. The invention further relates to antibodies specifically directed against the receptor peptides. Methods for generating an immune response and for treatment of tumors and cancer are also provided.
-
(2008/06/13)

Multi-functional chimeric hematopoietic receptor agonists
Disclosed are novel multi-functional chimeric hematopoietic receptor agonist proteins, DNAs which encode the multi-functional chimeric hematopoietic receptor agonist proteins, methods of making the multi-functional chimeric hematopoietic receptor agonist proetiens and methods of using the multi-functional chimeric hematopoietic receptor agonist proteins.
-
(2008/06/13)

Asymmetric hydrogenation of alpha-amino carbonyl compounds
A process for preparing a non-racemic aminoalcohol is provided. The process includes the step of contacting a chiral alpha-amino carbonyl compound and hydrogen, in the presence of a non-racemic hydrogenation catalyst, at a temperature, pressure and for a length of time sufficient to produce the non-racemic aminoalcohol. In a preferred embodiment, the process can be described by the reaction scheme: where R is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl or hetereoaryl group; and E can be hydrogen, COOR, CONHR, CONR2, COOH, COR, CN, NO2, alkyl, substituted alkyl, aryl, substituted aryl or hetereoaryl group.
-
Page/Page column 12

(2008/06/13)

Stereoselective β-hydroxy-α-amino acid synthesis via an ether-directed, palladium-catalysed aza-Claisen rearrangement
A highly diastereoselective synthesis of (2S,3S)-β-hydroxy-α- amino acids has been developed from enantiopure α-hydroxy acids using a MOM-ether-directed, palladium(II)-catalysed, aza-Claisen rearrangement of allylic acetimidates to effect the key step. This highly stereoselective process gave allylic amides in diastereomeric ratios of up to 14 : 1. Problems associated with the isolation of 1,3-products (anti-Claisen) from sterically demanding substrates via an in situ palladium(0)-catalysed rearrangement process were overcome by the addition of a re-oxidant, p-benzoquinone, leading to cleaner reactions and improved yields of the 3,3-products (Claisen). The target β-hydroxy-α-amino acids are an important class of natural products that are also components of more complex organic compounds with significant biological properties. The Royal Society of Chemistry 2005.
Fanning, Kate N.,Jamieson, Andrew G.,Sutherland, Andrew
p. 3749 - 3756
(2007/10/03)

CONJUGATES OF TRANSPORTER PEPTIDES AND NUCLEIC ACID ANALOGS, AND THEIR USE
Constructs of peptides and nucleic acid analogs conjugated together for transport across a lipid membrane and for delivery into interactive contact with intracellular polynucleotides are disclosed. Transport is effected through at least the exterior membrane of a cell, and most likely also through the walls of subcellular structures separated from the cytosol by lipid membranes, including the nucleus, mitochondria, ribosomes, etc. Peptide nucleic acid (PNA) analog sequences conjugated through a labile disulfide bond to transporting peptides, are intracellulary cleaved, and target mRNA (antigene) or dsDNA (antisense).
-
(2008/06/13)