- Preparation and characterization of a new open-tubular capillary column for enantioseparation by capillary electrochromatography
-
In order to use the enantioseparation capability of cationic cyclodextrin and to combine the advantages of capillary electrochromatography (CEC) with open-tubular (OT) column, in this study, a new OT-CEC, coated with cationic cyclodextrin (1-allylimidazolium-β-cyclodextrin [AI-β-CD]) as chiral stationary phase (CSP), was prepared and applied for enantioseparation. Synthesized AI-β-CD was characterized by infrared (IR) spectrometry and mass spectrometry (MS). The preparation conditions for the AI-β-CD-coated column were optimized with the orthogonal experiment design L9(34). The column prepared was characterized by scanning electron microscopy (SEM) and elemental analysis (EA). The results showed that the thickness of stationary phase in the inner surface of the AI-β-CD-coated columns was about 0.2 to 0.5?μm. The AI-β-CD content in stationary phase based on the EA was approximately 2.77?mmol·m?2. The AI-β-CD-coated columns could separate all 14 chiral compounds (histidine, lysine, arginine, glutamate, aspartic acid, cysteine, serine, valine, isoleucine, phenylalanine, salbutamol, atenolol, ibuprofen, and napropamide) successfully in the study and exhibit excellent reproducibility and stability. We propose that the column, coated with AI-β-CD, has a great potential for enantioseparation in OT-CEC.
- Li, Yingjie,Tang, Yimin,Qin, Shili,Li, Xue,Dai, Qiang,Gao, Lidi
-
p. 283 - 292
(2019/02/05)
-
- Stereospecific radiosynthesis of 3-fluoro amino acids: Access to enantiomerically pure radioligands for positron emission tomography
-
A variety of substituted non-racemic aziridine-2-carboxylates equivalent to amino acids were prepared and subjected to ring opening reaction by [18F/19F]fluoride. The regio and stereospecific ring opening depends on the substituents on the nitrogen as well as both the carbons of aziridines. The applicability of the methods to afford access to 3-[18F/19F]fluoro amino acids are illustrated.
- Alluri, Santosh R.,Riss, Patrick J.
-
supporting information
p. 2219 - 2224
(2018/04/05)
-
- Chiral Metal–Organic Framework Hollow Nanospheres for High-Efficiency Enantiomer Separation
-
Chiral ZIF-8 hollow nanospheres with d-histidine as part of chiral ligands (denoted as H-d-his-ZIF-8) were prepared for separation of (±)-amine acids. Compared to bulk d-his-ZIF-8 without a hollow cavity, the prepared H-d-his-ZIF-8 showed 15 times higher separation capacity and higher ee values of 90.5 % for alanine, 95.2 % for glutamic acid and 92.6 % for lysine, respectively.
- Wang, Xiaoshi,Zhu, Yanan,Liu, Jian,Liu, Chang,Cao, Changyan,Song, Weiguo
-
p. 1535 - 1538
(2018/06/26)
-
- Covalent Organic Frameworks with Chirality Enriched by Biomolecules for Efficient Chiral Separation
-
The separation of racemic compounds is important in many fields, such as pharmacology and biology. Taking advantage of the intrinsically strong chiral environment and specific interactions featured by biomolecules, here we contribute a general strategy is developed to enrich chirality into covalent organic frameworks (COFs) by covalently immobilizing a series of biomolecules (amino acids, peptides, enzymes) into achiral COFs. Inheriting the strong chirality and specific interactions from the immobilized biomolecules, the afforded biomolecules?COFs serve as versatile and highly efficient chiral stationary phases towards various racemates in both normal and reverse phase of high-performance liquid chromatography (HPLC). The different interactions between enzyme secondary structure and racemates were revealed by surface-enhanced Raman scattering studies, accounting for the observed chiral separation capacity of enzymes?COFs.
- Zhang, Sainan,Zheng, Yunlong,An, Hongde,Aguila, Briana,Yang, Cheng-Xiong,Dong, Yueyue,Xie, Wei,Cheng, Peng,Zhang, Zhenjie,Chen, Yao,Ma, Shengqian
-
supporting information
p. 16754 - 16759
(2018/11/27)
-
- Thalassosamide, a Siderophore Discovered from the Marine-Derived Bacterium Thalassospira profundimaris
-
Here we describe the rapid identification and prioritization of novel active marine natural products using an improved dereplication strategy. During the course of our screening of marine natural product libraries, a new cyclic trihydroxamate compound, thalassosamide, was discovered from the α-proteobacterium Thalassospira profundimaris. Its structure was determined by 2D NMR and MS/MS experiments, and the absolute configuration of the lysine-derived units was established by Marfey's analysis, whereas that of C-9, 9′, and 9″ was determined via the circular dichroism data of the [Rh2(OCOCF3)4] complex and DFT NMR calculations. Thalassosamide showed moderate in vivo efficacy against Pseudomonas aeruginosa.
- Zhang, Fan,Barns, Kenneth,Hoffmann, F. Michael,Braun, Doug R.,Andes, David R.,Bugni, Tim S.
-
p. 2551 - 2555
(2017/09/27)
-
- Chromatographic Resolution of α-Amino Acids by (R)-(3,3'-Halogen Substituted-1,1'-binaphthyl)-20-crown-6 Stationary Phase in HPLC
-
Three new chiral stationary phases (CSPs) for high-performance liquid chromatography were prepared from R-(3,3'-halogen substituted-1,1'-binaphthyl)-20-crown-6 (halogen = Cl, Br and I). The experimental results showed that R-(3,3'-dibromo-1,1'-binaphthyl)-20-crown-6 (CSP-1) possesses more prominent enantioselectivity than the two other halogen-substituted crown ether derivatives. All twenty-one α-amino acids have different degrees of separation on R-(3,3'-dibromo-1,1'-binaphthyl)-20-crown-6-based CSP-1 at room temperature. The enantioselectivity of CSP-1 is also better than those of some commercial R-(1,1'-binaphthyl)-20-crown-6 derivatives. Both the separation factors (α) and the resolution (Rs) are better than those of commercial crown ether-based CSPs [CROWNPAK CR(+) from Daicel] under the same conditions for asparagine, threonine, proline, arginine, serine, histidine and valine, which cannot be separated by commercial CR(+). This study proves the commercial usefulness of the R-(3,3'-dibromo-1,1'-binaphthyl)-20-crown-6 chiral stationary phase.
- Wu, Peng,Wu, Yuping,Zhang, Junhui,Lu, Zhenyu,Zhang, Mei,Chen, Xuexian,Yuan, Liming
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supporting information
p. 1037 - 1042
(2017/07/25)
-
- COMPOSITIONS AND METHODS FOR THE PREPARATION OF KIDNEY PROTECTIVE AGENTS COMPRISING AMIFOSTINE AND AMINO ACIDS
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This invention relates to composition and method of preparation of AminoMedix? comprising of Amifostine, at least one amino acid (Arginine, Lysine, Histidine) with or without other pharmaceutically active compounds. The AminoMedix? composition can be applied for kidney protection during therapy using radiolabeled and non-radiolabeled compounds, contrast agents, chemotherapeutics, antibiotics and drugs showing nephrotoxic effect.
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- A method for preparing DL-lysine
-
The invention provides a method for preparing DL-lysine with chiral lysine salt as a raw material. The method specifically comprises the following steps: dissolving chiral lysine salt in an acetic acid water solution, adding salicylaldehyde or benzaldehyde as a catalyst, carrying out heating and racemization, removing solvents through vacuum distillation after racemization is completed, washing a residual solid with ethanol, obtaining DL-lysine salt, removing salt with an ion exchange column and carrying out concentration and decoloration, thus obtaining a DL-lysine solid. The preparation method has the advantages that the preparation method is lower in production cost and simple in process; pollution is not easily caused in the production process; the racemization rate of L-lysine hydrochloride can be 100%; the purity of the obtained DL-lysine finished product is more than 98%.
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-
Paragraph 0032; 0033
(2017/04/03)
-
- AXIAL-ASYMMETRIC N-(2-ACYLARYL)-2-[5, 7-DIHYDRO-6H-DIBENZO [C, E] AZEPINE-6-YL] ACETAMIDE COMPOUND AND CHIRALITY CONVERSION METHOD FOR A-AMINO ACID USING SAME
-
An object of the present invention is to provide a method for producing an optically active amino acid in high yield and in a highly enantioselective manner, which method has fewer restrictions on the material that can be used as the substrate, and to provide, among others, a compound useful as a chiral auxiliary for the method. The present invention provides an N-(2-acylaryl)-2-[5,7-dihydro-6H-dibenzo[c,e]azepin-6-yl]ac etamide compound represented by Formula (1): or a salt thereof, or a metal complex represented by Formula (3) :
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-
Paragraph 0152; 0153; 0154
(2015/11/27)
-
- SEPARATING AGENT AND MANUFACTURING METHOD THEREOF
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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.
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Paragraph 0067; 0068; 0069; 0070; 0071; 0072; 0101; 0102
(2015/01/07)
-
- Aplysinellamides A-C, bromotyrosine-derived metabolites from an australian aplysinella sp. marine sponge
-
Mass-directed fractionation of an extract from the Australian marine sponge Aplysinella sp., from the Great Barrier Reef, resulted in the isolation of four new bromotyrosine derivatives, aplysinellamides A-C (1-3) and aplysamine-1-N-oxide (4), along with six known compounds (5-10). The structure elucidation of compounds 1-4 was based on their 1D and 2D NMR and MS spectroscopic data. Aplysamine-1 (6) increased the apolipoprotein E secretion from human CCF-STTG1 astrocytoma cells by 2-fold at the concentration of 30 μM.
- Tian, Li-Wen,Feng, Yunjiang,Shimizu, Yoko,Pfeifer, Tom,Wellington, Cheryl,Hooper, John N. A.,Quinn, Ronald J.
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p. 1210 - 1214
(2014/06/10)
-
- Chemical dynamic kinetic resolution and S/R interconversion of unprotected α-amino acids
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Reported herein is the first purely chemical method for the dynamic kinetic resolution (DKR) of unprotected racemic α-amino acids (α-AAs), a method which can rival the economic efficiency of the enzymatic reactions. The DKR reaction principle can be readily applied for S/R interconversions of α-AAs, the methodological versatility of which is unmatched by biocatalytic approaches. The presented process features a virtually complete stereochemical outcome, fully recyclable source of chirality, and operationally simple and convenient reaction conditions, thus allowing its ready scalability. A quite unique and novel mode of the thermodynamic control over the stereochemical outcome, including an exciting interplay between axial, helical, and central elements of chirality is proposed. A new player for DKR: Dynamic kinetic resolution of α-amino acids has been achieved upon complexation with nickel(II) and a chiral ligand derived from optically active bis(naphthyl)amine under thermodynamic control, thus affording excellent diastereoselectivities and chemical yields. The S to R interconversion of α-amino acids is also described.
- Takeda, Ryosuke,Kawamura, Akie,Kawashima, Aki,Sato, Tatsunori,Moriwaki, Hiroki,Izawa, Kunisuke,Akaji, Kenichi,Wang, Shuni,Liu, Hong,Ace?a, José Luis,Soloshonok, Vadim A.
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supporting information
p. 12214 - 12217
(2016/02/18)
-
- SEPARATING AGENT FOR CHROMATOGRAPHY
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A separating agent for chromatography is provided that is useful for the separation of specific compounds, e.g., for the optical resolution of amino acids. This separating agent for chromatography provides a higher productivity and contains a crown ether-like cyclic structure and optically active binaphthyl. This separating agent for chromatography containing a crown ether-like cyclic structure and optically active binaphthyl is provided by introducing a substitution group for binding to carrier into a specific commercially available 1,1′-binaphthyl derivative that has substituents at the 2, 2′, 3, and 3′ positions, then introducing a crown ether-like cyclic structure, and subsequently chemically bonding the binaphthyl derivative to the carrier through the substitution group for binding to carrier.
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-
Paragraph 0074; 0075
(2013/08/15)
-
- Lysine racemase from a lactic acid bacterium, Oenococcus oeni: Structural basis of substrate specificity
-
Oenococcus oeni, a lactic acid bacterium, possesses a lysine racemase, which has a specific activity towards basic amino acids. A comparison of amino acid residues around the active site suggested that Ile222 and Tyr354 of the Geobacillus stearothermophilus alanine racemase, which shares 60% sequence similarity with lysine racemase, were replaced by Thr224 and Trp355 in the O. oeni lysine racemase. T224I/W355Y double mutations significantly decreased the activity of lysine racemase, whereas I222T/Y354W double mutations endowed alanine racemase with lysine racemization activity. These results suggest that the two residues play an important role in lysine racemization.
- Kato, Shiro,Hemmi, Hisashi,Yoshimura, Tohru
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p. 505 - 508
(2013/02/25)
-
- Analysis of catalytic determinants of diaminopimelate and ornithine decarboxylases using alternate substrates
-
Diaminopimelate decarboxylase (DAPDC) and ornithine decarboxylase (ODC) are pyridoxal 5′-phosphate dependent enzymes that are critical to microbial growth and pathogenicity. The latter is the target of drugs that cure African sleeping sickness, while the former is an attractive target for antibacterials. These two enzymes share the (β/α)8 (i.e., TIM barrel) fold with alanine racemase, another pyridoxal 5′-phosphate dependent enzyme critical to bacterial survival. The active site structural homology between DAPDC and ODC is striking even though DAPDC catalyzes the decarboxylation of a D stereocenter with inversion of configuration and ODC catalyzes the decarboxylation of an L stereocenter with retention of configuration. Here, the structural and mechanistic bases of these interesting properties are explored using reactions of alternate substrates with both enzymes. It is concluded that simple binding determinants do not control the observed stereochemical specificities for decarboxylation, and a concerted decarboxylation/proton transfer at Cα of the D stereocenter of diaminopimelate is a possible mechanism for the observed specificity with DAPDC.
- Fogle, Emily J.,Toney, Michael D.
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experimental part
p. 1113 - 1119
(2012/06/04)
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- Powder storage container
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PROBLEM TO BE SOLVED: To prevent a sealing member from breaking away from a device body even when the sealing member is bent. SOLUTION: A toner replenishing type developing device 4Y, 4M, 4C or 4B comprises a developing device body 4a, and a sealing member 4e. The sealing member 4e comprises an insertion and removal part 41a which a toner replenishing pipe 13Y, 13M, 13C, or 13B is inserted into and removed from, and a bending part 41b which bends by the insertion of the replenishing pipe 13Y, 13M, 13C or 13B into the insertion and removal part 41a, and is restored to its original state by the removal of the toner replenishing pipe 13Y, 13M, 13C or 13B from the insertion and removal part 41a. The bending part 41b of the sealing member 4e is formed in such a manner that the thickness t2 thereof in the insertion direction of the toner replenishing pipe 13Y, 13M, 13C or 13B at the bending part 41b is smaller than the thickness t1 of the insertion and removal part 41a in the insertion direction of the toner replenishing pipe 13Y, 13M, 13C or 13B at the insertion and removal part 41a. COPYRIGHT: (C)2007,JPOandINPIT
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- Kinetics and mechanism of thermal decomposition of kynurenines and biomolecular conjugates: Ramifications for the modification of mammalian eye lens proteins
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Thermal degradation reactions of kynurenine (KN), 3-hydroxykynurenine (3OHKN), and several adducts of KN, to amino acids and reduced glutathione (GSH) have been studied at physiological temperature. These compounds are all implicated in age-related mammalian eye lens cataract formation at the molecular level. The main reaction pathway for both KN and 3OHKN is deamination viaβ-elimination to carboxyketoalkenes CKA and 3OHCKA. These reactions show a weak pH dependence below pH values of ～8, and a strong pH dependence above this value. The 3OHKN structure deaminates at a faster rate than KN. A mechanism for the deamination reaction is proposed, involving an aryl carbonyl enol/enolate ion, that is strongly supported by the structural, kinetic, and pH data. The degradation of Lys, His, Cys and GSH adducts of the CKA moieties was also studied. The Lys adduct was found to be relatively stable over 200 h at 37 °C, while significant degradation was observed for the other adducts. The results are discussed in terms of known post-translational modification reactions of the lens proteins and compared to incubation studies involving KN and related compounds in the presence of proteins.
- Kopylova, Lyudmila V.,Snytnikova, Olga A.,Chernyak, Elena I.,Morozov, Sergey V.,Forbes, Malcolm D. E.,Tsentalovich, Yuri P.
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experimental part
p. 2958 - 2966
(2011/02/25)
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- Compositions, kits, and methods relating to the human FEZ1 gene, a novel tumor suppressor gene
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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.
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-
- Method for the selective and quantitative functionalization of immunoglobulin fab fragments, conjugate compounds obtained with the same and compositions thereof
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The invention provides chemical conjugates between an immunoglobulin Fab fragment and molecular entities imparting diagnostic or therapeutic utility, whereby the only sites of conjugation on the Fab fragment are one or both of the sulfhydryl groups deriving from the selective and quantitative reduction of the inter-chain disulfide bond of said Fab fragment and whereby said molecular entities imparting diagnostic or therapeutic utility have at least one free sulfhydryl-reactive group, characterized in that the conjugation stoichiometric molar ratio molecular entity to Fab fragment is in the range from 0.95 to 1.05 or in the range from 1.95 to 2.05. The invention also provides a process for preparing said conjugates and pharmaceutical compositions thereof.
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- T-CELL SELECTIVE INTERLEUKIN-4 AGONISTS
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The invention is directed to human IL-4 muteins numbered in accordance with wild-type IL-4 having T-cell activating activity, but having reduced endothelial cell activating activity. In particular, the invention is related to human IL-4 muteins wherein the surface-exposed residues of the D helix of the wild-type IL-4 are mutated whereby the resulting mutein causes T-cell proliferation, and causes reduced IL-6 secretion from HUVECs, relative to wild-type IL-4. This invention realizes a less toxic IL-4 mutant that allows greater therapeutic use of this interleukin. Further, the invention is directed to IL-4 muteins having single, double and triple mutations represented by the designators R121A, R121D, R121E, R121F, R121H, R121I, R121K, R121N, R121P, R121T, R121W; Y124A, Y124Q, Y124R, Y124S, Y124T; Y124A/S125A, T13D/R121E; and R121T/E122F/Y124Q, when numbered in accordance with wild-type IL-4 (His=1). The invention also includes polynucleotides coding for the muteins of the invention, vectors containing the polynucleotides, transformed host cells, pharmaceutical compositions comprising the muteins, and therapeutic methods of treatment.
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-
- Analysis of underivatized amino acids and their D/L-enantiomers by sheathless capillary electrophoresis/electrospray ionization-mass spectrometry
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Capillary electrophoresis/electrospray ionization-mass spectrometry (CE/ESI-MS) was applied to the analysis of underivatized amino acids and the separation of their D/L-enantiomers. Under full-scan mode, all standard protein amino acids were separated and detected at low-femtomole levels using a 130-cm-long, 20-μm-i.d., 150-μm-o.d. underivatized fused-silica capillary with 1 M formic acid as the background electrolyte. The CE/ESI-MS technique was also applied to the separation of L-arginine from L-canavanine (a close analogue of arginine where the terminal methylene linked to the guanidine group of arginine is replaced by an oxygen atom) in a complex mixture containing all standard protein amino acids. The utility of CE/ESI-MS in the analysis of real-world samples was demonstrated by the identification of two metabolic diseases (PKU and tyrosinemia) through blood analysis with minimal sample preparation. In addition, the on-line separation of 11 underivatized L-amino acids from their D-enantiomers was achieved by using a 30 mM solution of (+)-(18-crown-6)-2,3,11,12-tetracarboxylic acid as the background electrolyte.
- Schultz, Casey L.,Moini, Mehdi
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p. 1508 - 1513
(2007/10/03)
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- (1 -> 3, 1 -> 4)-beta-glucanase of enhanced stability
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A modified cereal (1→3,1→4)-β-glucanase is produced by the method of single point substitution in a native cereal (1→3,1→4)-β-glucanase enzyme, whereby the substitution: a) maintains enzyme specificity by conserving the active site groove of the native cereal (1→3,1→4)-β-glucanase enzyme; and b) effects increased thermostability over the native cereal (1→3,1→4)-β-glucanase enzyme by: i) replacing glycine by proline or alanine in helices of the cereal (1→3,1→4)-β-glucanase enzyme, in order to stiffen the enzyme amino acid chain and reduce entropy of the unfolded enzyme; ii) attaching negatively charged residues to N-termini of helices in the native cereal (1→3,1→4)-β-glucanase enzyme; iii) introducing ion pairs into the native cereal (1→3,1→4)-β-glucanase enzyme, to increase binding energy in the folded enzyme; iv) replacing lysine by arginine in the cereal (1→3,1→4)-β-glucanase enzyme, and thereby preventing lysine glycation and increasing hydrogen bonding with other parts of the enzyme; v) replacing, by glycine, an amino acid in the native cereal (1→3,1→4)-β-glucanase enzyme in which the main chain torsion angle about the N and Cα atoms is greater than 0°; or vi) creating cysteine pairs in the native cereal (1→3,1→4)-β-glucanase enzyme which can form disulphide bonds across the C and N terminals.
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- 3-deoxyglucosone and skin
-
The invention relates to a method of removing 3-deoxyglucosone and other alpha-dicarbonyl sugars from skin. The invention further relates to methods of inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin. The invention also relates to methods of treating 3-deoxyglucosone and other alpha-dicarbonyl sugars associated diseases and disorders of skin.
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- Inhibition of BEHAB cleavage and primary central nervous system (CNS) tumors
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The present invention relates to primary CNS tumors and provides useful compositions and methods for reducing tumor volume and increasing the length of survival in mammals with primary CNS tumors, thereby providing a treatment for primary CNS tumors. The invention also relates to methods of identifying compounds for reducing tumor volume and increasing animal survival, which therefore relate to treating primary CNS tumors.
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- Compositions, methods, and kits relating to resistin-like molecules
-
The invention relates to novel nucleic acids encoding a mammalian resistin-like molecule (RELM), and proteins encoded thereby, whose expression is increased in certain diseases, disorders, or conditions, including, but not limited to, intestinal (e.g., colonic) tumors. The invention further relates to methods of treating and detecting irritable bowel disease, inflammatory bowel disease, familial adenomatous polyposis, diabetes, insulin resistance, obesity, Syndrome X, and glucose metabolism disorders, colon cancer, breast cancer, and tongue cancer, comprising modulating or detecting RELM expression and/or production and activity of RELM polypeptide, wherein RELM encompasses resistin-like molecule α and resistin-like molecule β.
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- Mammalian prestin polynucleotides
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The invention relates to mammalian prestin protein, which has been discovered to be the mammalian cochlear outer hair cell motor, and to polynucleotides encoding prestin. Full length gerbil prestin and its cDNA are described, full length murine prestin and its cDNA are described, and a partial sequence of human prestin and its chromosomal location are described.
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- 20(S) camptothecin glycoconjugates
-
The present invention relates to glycoconjugates of 20(S)-camptothecin, in which a 3-O-methylated β-L-fucose unit is linked to the 20-hydroxyl group of a camptothecin derivative via a thiourea-modified peptide spacer. The invention furthermore relates to processes for the preparation of the compounds according to the invention and to their use as medicaments, in particular in connection with oncoses.
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- Bix-azo naphthylene compounds and their use in compositions and inks for ink-jet printing
-
Compounds of the Formula (1) and salts thereof: wherein: each A independently is N, C—Cl, C—CN or C—NO2; each Ar independently is a substituted aryl group carrying a —COOH group ortho to the azo (—N═N—) group; L is an aliphatic group carrying a —COOH, —SO3H or —PO3H2group; each Z independently is —SR2, —OR3, —NR4R5or a labile atom or group; each X independently is —S—, —O— or —NR1—; each R1independently is H or optionally substituted alkyl; and R2, R3, R4and R5are independently H, optionally substituted alkyl, optionally substituted aryl or optionally substituted aralkyl; or R4and R5together with the nitrogen to which they are attached form an optionally substituted five or six membered ring, and their use in compositions and inks for ink jet printing processes and ink jet printer cartridges.
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- Monoclonal antibody against human telomerase catalytic subunit
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The present invention provides a monoclonal antibody which can specifically and efficiently recognize hTERT protein; which is the catalytic subunit of telomerase, and provides a human chimeric antibody, a CDR grafted antibody, a single chain antibody, and a disulfide stabilized antibody each containing the monoclonal antibody. In addition, the present invention provides a method for detecting/quantitating hTERT protein using these antibodies, and provides diagnosis method, diagnosis agent, and therapeutic agent, for diseases, such as cancer, in which telomerase is involved using these bodies.
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- Thermochemical data on adducts of copper chloride with the amino acids lysine and glycine
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Adducts of the general formula CuCl2·nlys (n = 1,2,4;lys = lysine) and CuCl2·ngly (n = 2,4;gly = glycine) were prepared by reacting the ligands with CuCl2 in solid state. The adducts were characterized by elemental analysi
- Martínez, Leandro,De Farias, Robson F.,Airoldi, Claudio
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-
- 9-BBN: An amino acid protecting group for functionalization of amino acid side chains in organic solvents.
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9-Borabicyclononane (9-BBN) has been utilized to protect functionalized amino acids for potential chemoselective side chain manipulation. The 9-BBN group imparts organic solubility to otherwise hydrophilic molecules and is tolerant of a wide range of reaction conditions. The high degree of solubility of these molecules in THF is particularly noteworthy. It is cleaved with either aqueous HCl or by exchange with ethylenediamine in methanol. [reaction: see text]
- Dent 3rd., William H,Erickson, W Randal,Fields, Stephen C,Parker, Marshall H,Tromiczak, Eric G
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p. 1249 - 1251
(2007/10/03)
-
- Gene recombinant antibody and antibody fragment thereof
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A recombinant antibody or the antibody fragment thereof which specifically reacts with an extracellular domain of human CCR4; a DNA which encodes the recombinant antibody or the antibody fragment thereof; a method for producing the recombinant antibody or the antibody fragment thereof; a method for immunologically detecting CCR4, a method for immunologically detecting a cell which expressed CCR4 on the cell surface, a method for depleting a cell which expresses CCR4 on the cell surface, and a method for inhibiting production of Th2 cytokine, which comprise using the recombinant antibody according or antibody fragment thereof; a therapeutic or diagnostic agent for Th2-mediated immune diseases; and a therapeutic or diagnostic agent for a blood cancer.
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- Method for the preparation of 1-benzotriazolylcarbonate esters of poly(ethylene glycol)
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The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non-peptidic polymer with di(1-benzotriazolyl) carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcarbonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid, such as lysine, to form an amino acid derivative.
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- Antiviral composition derived from allium CEPA and therapeutic use thereof
-
Novel medicinal extracts derived from Allium species, preferablyAllium cepaare provided. These extracts have broad medicinal properties, especially for treatment of AIDS and other viral infections.
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- NON-NATURALLY OCCURRING LIPOPROTEIN PARTICLE
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Non-naturally occurring receptor competent LDL particle comprising at least one peptide component wherein the said peptide component comprises at least a binding site for an Apo B protein receptor and at least one lipophilic substituent.
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- Simultaneous imaging of cardiac perfusion and a vitronectin receptor targeted imaging agent
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The present invention describes a method of concurrent imaging in a mammal comprising: a) administering to said mammal a vitronectin receptor targeted imaging agent and a perfusion imaging agent; and b) concurrently detecting the vitronectin target imagin
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- T-cell selective interleukin-4 agonists
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This invention realizes a less toxic IL-4 mutant that allows greater therapeutic use of interleukin 4. Further, the invention is directed to IL-4 muteins having single and double mutations represented by the designators R121E and T13D/R121E, numbered in accordance with wild type IL-4 (His=1). The invention also includes polynucleotides coding for the muteins of the invention, vectors containing the polynucleotides, transformed host cells, pharmaceutical compositions comprising the muteins, and therapeutic methods of treatment.
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- Method of using PON-1 to decrease atheroma formation
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The invention is directed to a method of decreasing atheroma formation in a mammal comprising administering a pharmaceutically effective amount of PON-1 or its functional equivalent to a patient in need thereof. Also included herein are pharmaceutical compositions, and a method for diagnosing predisposition to hypercholesterolemia by assessing the level of native circulating PON-1.
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- ASSAYS FOR HOMOCYSTEINE AND HOMOCYSTEINE DESULPHURASE FROM PROTOZOAN TRICHOMONASVAGINALIS
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The present invention relates to an assay for determining homocysteine, cysteine, O-acetyl-L-serine and/or methionine levels in a biological sample using an enzyme that catalyzes the degradation of homocysteine, cysteine, O-acetyl-L-serine and methionine. The enzyme being more particularly homocysteine desulphurase, a polynucleotide fragment encoding protozoan homocysteine desulphurase, a recombinant vector comprising a polynucleotide fragment, transformed cells, the protozoan homocysteine desulphurase polypeptide, and pharmaceutical compositions comprising recombinant homocysteine desulphurase for use in medicine or veterinary medicine.
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- CELL DELIVERY COMPOSITIONS
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The present invention provides improved cell delivery compositions. In particular, the invention provides biocompatible endosomolytic agents. In a preferred embodiment, the endosomolytic agents are also biodegradable and can be broken down within cells into components that the cells can either reuse or dispose of. Preferred endosomolytic agents include cationic polymers, particularly those comprised of biomolecules, such as histidine, polyhistidine, polylysine or any combination thereof. Other exemplary endosomolytic agents include, but are not limited to, other imidazole containing compounds such as vinylimidazole and histamine. More particularly preferred are those agents having multiple proton acceptor sites and acting as a “proton sponge”, disrupting the endosome by osmolytic action. In preferred embodiments, the endosomolytic agent comprises a plurality of proton acceptor sites having pKas within the range of 4 to 7, which endosomal lysing component is polycationic at pH 4. The present invention also contemplates the use of these endosomolytic agents as delivery agents by complexation with the desired compound to be delivered. Thus, the present invention also acts as a cell delivery system comprising an endosomolytic agent, a delivery agent, and a compound to be delivered.
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- Composition of matter having bioactive properties
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Particles of coordinated complex comprising a basic, hydrous polymer and a capacitance adding compound, as well as methods for their production, are described. These complexes exhibit a high degree of bioactivity making them suitable for a broad range of applications through their incorporation into conventional vehicles benefiting from antimicrobial and similar properties.
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- Methods of enhancing functioning of the large intestine
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The invention relates to glucagon-related peptides and their use for the prevention or treatment of disorders involving the large intestine. In particular, it has now been demonstrated that GLP-2 and peptidic agonists of GLP-2 can cause proliferation of the tissue of large intestine. Thus, the invention provides methods of proliferating the large intestine in a subject in need thereof. Further, the methods of the invention are useful to treat or prevent inflammatory conditions of the large intestine, including inflammatory bowel diseases.
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- TUMOR ANTIGEN PEPTIDE ORIGINATING IN SART-1
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To provide a tumor antigen peptide derived from SART-1 and a derivative thereof, possessing functionally equivalent characteristics thereto; or a therapeutic agent, prophylactic agent or the like for a tumor, each utilizing the tumor antigen peptide.
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- Bacillus thuringiensis Cry1Ia-Cry1Ba hybrid toxins
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Bacillus thuringiensishybrid toxin fragment comprising structural domains I, II and III in this order starting from the N-terminal, wherein the domains are derived from at least two different Cry proteins, domain I is domain I of any Bacillus thuringiensisCry protein or a part of said domain or a peptide substantially similar to said domain, domain II is domain II of Cry1la or a part of said domain or a peptide substantially similar to said domain, and domain III is domain III of Cry1Ba or a part of said domain or a peptide substantially similar domain.
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- THYMIDINE KINASE MUTANTS
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The present invention provides isolated nucleic acid molecules encoding a Herpesviridae thymidine kinase enzyme comprising one or more mutations, at least one of the mutations encoding an amino acid substitution upstream from a DRH nucleoside binding site which increases a biological activity of the thymidine kinase, as compared to unmutated thymidine kinase. Within another aspect, one of the mutations is an amino acid substitution within a DRH nucleoside binding site which increases a biological activity of the thymidine kinase, as compared to unmutated thymidine kinase. Also provided are vectors suitable for expressing such DNA molecules, as well as methods for utilizing such vectors.
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- NOVEL G PROTEIN-COUPLED RECEPTOR PROTEIN AND DNA THEREOF
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The present invention relates to a rat cerebellum-derived G-protein-coupled receptor protein, its partial peptides, and salts thereof, and a nucleic acid and its derivatives that encodes the receptor protein. The rat cerebellum-derived G-protein-coupled receptor protein of this invention and the nucleic acid and its derivatives encoding the said protein can be used for determination of ligands (agonists) for the G-protein-coupled receptor protein of this invention, prophylactic and/or therapeutic drugs for diseases related to dysfunction of the G-protein-coupled receptor protein of this invention, gene diagnostic drugs, and methods for screening compounds that change the expression level of the receptor protein of this invention and its partial peptides.
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- Human betacellulin-specific antibodies and uses thereof
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Disclosed are an antibody which have a binding activity to human betacellulin protein or a mutein thereof with specificity; especially a monoclonal antibody which does not have cross reactitivity with human epidermal growth factor (EGF) and human transforming growth factor a (TGF-α), belongs to the immunoglobulin class of IgG, and,specifically binds to human betacellulin protein to neutralize biological activity thereof; a hybridoma for producing the monoclonal antibody; and a method for producing the monoclonal antibody. Said monoclonal antibody neutralizes biological activity of a human BTC protein, and bind to the protein with high sensitivity and specificity, so that they can be used as a therapeutic agent for diseases such as arterial sclerosis and cancers, and also used as a reagent for assaying the human BTC protein or a mutein thereof and as a diagnostic agent for diabetes or complications thereof.
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- Prolonged delivery of peptides
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There are disclosed methods for the treatment of non-insulin dependent diabetes mellitus in a mammal comprising the prolonged administration of GLP-1 (7-37), and related peptides. Also disclosed are compositions to prolong the administration of the peptides.
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- Compositions, kits, and methods for effecting adenine nucleotide modulation of DNA mismatch recognition proteins
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Compositions, and products comprising a MutS homolog which binds to a mismatched region of a duplex DNA molecule in the presence of ADP are provided, as are methods of binding MutS homologs to mismatched DNA in the presence of ADP. The use of MutL homolog derivatives in combination with MutS homologs is also included. Nonhuman mammals which are nullizygous for both Msh2 and p53 are also provided, as are methods of making and using the same.
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