76 results about "Chemo enzymatic" patented technology

The invention provides synthetic chemical and chemoenzymatic methods of producing simvastatin and various intermediates. In one aspect, enzymes such as hydrolases, e.g., esterases, are used in the methods of the invention.

This invention provides a direct method for monitoring bacterial transglycosylase activity using labeled substrates produced by chemo-enzymatic synthesis wherein the labels are selected to permit the detection of both polymeric and non-polymeric products simultaneously, either directly or following the separation of product from starting material. The invention promotes the discovery of new antibiotics with activity against bacterial transglycosylases by a) laying the groundwork for structural analysis of purified, active transglycosylase (which permits structure-based design); and b) providing an assay that can be used to screen for inhibitors.

Methods of producing peptide beta-lactones and beta-hydroxy acids are disclosed that include contacting a beta-hydroxy-alpha-amino acid, an aryl carrier protein (ObiD), and ATP with a non-ribosomal protein synthetase. A continuous flow reactor is disclosed that includes an elongate conduit with at least one region that includes a first region with a non-ribosomal protein synthetase immobilized to a substrate. The non-ribosomal protein synthetase of the continuous flow reactor is configured to contact a flow of a reaction mixture that includes a beta-hydroxy-alpha-amino acid and an aryl carrier protein. The non-ribosomal protein synthetase is further configured to release a peptide beta-lactone into the flow of the reaction mixture.

The present invention generally relates to materials and methods for exploiting glycosyltransferase reversibility for nucleotide diphosphate (NDP) sugar synthesis. The present invention provides engineered glycosyltransferase enzymes characterized by improved reaction reversibility and expanded sugar donor specificity as compared to corresponding non-mutated glycosyltransferase enzymes. Such reagents provide advantageous routes to NDP sugars for subsequent use in a variety of biomedical applications, including enzymatic and chemo-enzymatic glycorandomization.

This invention provides a direct method for monitoring bacterial transglycosylase activity using labeled substrates produced by chemo-enzymatic synthesis wherein the labels are selected to permit the detection of both polymeric and non-polymeric products simultaneously, either directly or following the separation of product from starting material. The invention promotes the discovery of new antibiotics with activity against bacterial transglycosylases by a) laying the groundwork for structural analysis of purified, active transglycosylase (which permits structure-based design); and b) providing an assay that can be used to screen for inhibitors.

The present invention relates to a novel process for the preparation of optically enriched substituted R(+)beta-benzyl-gamma-butyrolactones of the general formula 1, wherein, R1 and R2 independently represent the following groups, R1=R2=H, OH, -OCnH2n+1 (n=1 to 8), NH2, and / or CF3, R1 and R2 together represents -O(CH2)mO- where m=2 to 4.

A new class of paromomycin-derived aminoglycosides, which exhibit efficient stop-codon mutation suppression activity, low toxicity and high selectivity towards eukaryotic cells are provided. Also provided are chemical and chemo-enzymatic processes of preparing these paromomycin-derived aminoglycosides and intermediates thereof, as well as pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders.

The invention provides a chemical-enzyme method for preparing D-basic amino acid hydrochloride. The method comprises the following steps of: derivatizing DL-basic amino acid serving as a raw material to obtain DL-N-diphenyl acetyl basic amino acid by utilizing an acylating agent, hydrolyzing the DL-N-diphenyl acetyl basic amino acid by using immobilized penicillin acylase as a biocatalyst through non-stereo selectivity and enantioselectivity to obtain L-basic amino acid, phenylacetic acid and D-alpha-N-phenylacetyl basic amino acid; and performing acidolysis on the D-alpha-N-phenylacetyl basic amino acid to obtain phenylacetic acid and D-basic amino acid dihydrochloride, and performing treatment of epoxypropane to obtain the D-basic amino acid hydrochloride. The D-lysine hydrochloride and D-ornithine hydrochloride which are prepared by the method have the yield of more than 40 percent, and ee is more than 99 percent. The method has the characteristics of high yield and optical purity, simple process and the like, and is suitable for the large-scale production of the D-basic amino acid hydrochloride.

The invention discloses a method for synthesizing pseudouridine by a chemical enzyme method, which comprises the following steps: synthesizing pseudouridine monophosphate from ribose-5-phosphoric acid and a pseudouridine-5-phosphosidase mutant, and carrying out dephosphorylation and separation to obtain pseudouridine. The amino acid sequence of the pseudouridine-5-phosphosidase mutant is as shown in SEQ ID NO: 1. According to the method, the pseudouridine is synthesized through chemical-enzymatic reaction, mass production of the pseudouridine is realized through simple reaction and low cost, and the application of industrial synthesis of the pseudouridine is promoted.

The invention provides a chemical-enzyme method for preparing D-tyrosine. The method comprises the following steps: based on DL-tyrosine as a raw material, deriving DL-tyrosine into DL-N-phenylacetyltyrosine in an acidic medium by using an acylating agent; based on immobilized penicillin acylase as a biocatalyst, carrying out enantiomorphous selective hydrolysis so as to form L-tyrosine, phenylacetic acid and D-N-phenylacetyltyrosine; and carrying out acidolysis on D-N-phenylacetyltyrosine so as to obtain phenylacetic acid and D-tyrosine. According to the chemical-enzyme method, the yield of D-tyrosine is 40%, and enantiomeric excess is larger than 99%. The method provided by the invention has the characteristics of high yield and optical purity of product, simple process and the like, and is suitable for large-scale production of D-tyrosine.

The invention discloses a preparation method and application of an anti-tumor immune cell based on a ligand-targeted cell conjugate (LTCC)technology. The preparation method comprises the following steps: adding non-natural sugar modified with a biological orthogonal reaction group into a culture medium of immune cells, such as NK cells, so as to obtain immune cells modified with the biological orthogonal reaction group; then, modifying a targeting ligand, such as a nano antibody, of which one end is a biological orthogonal reaction pairing group capable of being matched with the biological orthogonal reaction group to generate a connection reaction to the surface of the immune cell through biological orthogonal reaction under physiological conditions, wherein the linking mode is a transpeptidase SrtA mediated chemical enzyme method, and ligand targeting has the characteristics of high-specificity recognition and high-expression receptor binding to the surface of the tumor cell. The ligand-targeted modified immune cell can specifically bind to cancer cells in a targeting manner, so that the modified immune cell generates an effect of secreting a large number of cytokines to enable the surfaces of the cancer cells to generate transmembrane pores or phagocytic cleavage of the cancer cells, and the immune cell has the effect of specifically killing the cancer cells.

The invention relates to methods and compositions for causing the selective targeting and killing of tumor cells. The present invention describes prophylactic or therapeutic cancer vaccines based on purified TAA proteins or TAA-derived synthetic peptides altered by chemical, enzymatic or chemo-enzymatic methods to introduce αGal epitopes or αGal glycomimetic epitopes, in order to allow for enhanced opsonization of the antigen by natural anti-αGal antibodies to stimulate TAA capture and presentation, thereby inducing a humoral and cellular immune response to the TAA expressed by a tumor. The animal's immune system thus is stimulated to produce tumor specific cytotoxic cells and antibodies which will attack and kill tumor cells present in the animal.

The present invention relates to a novel synthetic process for the enriched preparation of substituted R(+)β-benzyl-γ-butyrolactone (1) as shown in the drawing wherein R1 and R2 independently or in combination represent the following groups: i.e. R1═R2═H, —OCnH2n+1 (where n=1 to 8); R1, and R2 together represents —O(CH2)mO— (where m=2 to 4)

The present invention provides protected tetrasaccharides, their process of preparation and their use in the synthesis of oligosaccharides, in particular fragments of O-antigens from Shigella flexneri, for example of serotype la, lb, 2a, 2b, 3a, X, 4a, 4b, 5a, 5b, 7a or 7b.