摘要:
Methods and compositions for making glycoproteins, both in vitro and in vivo, are provided. One method involves incorporating an unnatural amino acid having a N-acetylgalactosamine moiety into a protein; optionally, the N-acetylgalactosamine-containing unnatural amino acid can be further modified with additional sugars.
摘要:
The present invention provides medicinally active extracts and fractions, and a method for preparing the same by extracting and fractioning constituents from the tissue of components of Ganoderma lucidum. These active extracts and fractions are useful for inhibiting tumor growth, modulating immune response, and increasing hematopoietic activity.
摘要:
The invention provides arrays of molecules where the molecules (e.g., glycans) are attached to the arrays by cleavable linkers. The invention also provides methods for using these arrays, methods for identifying the structural elements of molecules bound to these arrays by using the cleavable linkers, especially the structural elements that are important for binding to test samples. The invention further provides methods for evaluating whether test samples and test molecules can bind to distinct glycans on the arrays and useful glycans identified using the methods and arrays provided herein.
摘要:
The present invention is based on the discovery that 2-deoxyribose-5-phosphate aldolase (DERA, EC 4.1.2.4) and variants thereof can be used to catalyze sequential asymmetric aldol reactions between a wide variety of donor and acceptor aldehydes. The reaction products typically contain at least two new stereogenic centers and can be produced in enantiomerically pure form. As such, DERA catalyzed asymmetric aldol chemistry can be exploited to produce synthons for the synthesis of a variety of bioactive molecules.
摘要:
A one-pot glycosylation reaction is disclosed in which a mannosyl (Man) group is enzymatically transferred to an acceptor molecule. The starting glycoside is a mannosyl 1-phosphate that is enzymatically converted to its GDP derivative via UTP and a pyrophorylase. The formed GDP derivative is used in the enzyme-catalyzed glycosyl transfer. That enzyme-catalyzed glycosyl transfer to an acceptor releases GDP that is enzymatically converted to GTP for further conversion of mannosyl 1-phosphate into its GDP derivative. Also disclosed are a recombinant α1,2-mannosyltransferase that is enzymatically active, is dispersible in an aqueous reaction medium, and free of the transmembrane portion of the native enzyme, as well as DNA encoding that transferase, an expression vector containing exogenous DNA that encodes that enzyme and E. coli cells containing that vector.
摘要:
Combinatorial libraries of HIV and FIV protease inhibitors are characterized by α-keto amide or hydroxyethylamine core structures flanked by on one side by substituted pyrrolidines, piperidines, or azasugars and on the other side by phenylalanine, tyrosine, or substituted tyrosines. The libraries are synthesized via a one step coupling reaction. Highly efficacious drug candidates are identified by screening the libraries for binding and inhibitory activity against both HIV and FIV protease. Drug candidates displaying clinically useful activity against both HIV and FIV protease are identified as being potentially resistive against a loss of inhibitory activity due to development of resistant strains of HIV.
摘要:
A medicament for treatment of a viral infection which comprises as an active ingredient a compound represented by the following formula (I) or its Pharmaceutically acceptable salt, or a hydrate thereof or a solvate thereof. wherein R1 represents hydrogen atom or a C1-6 alkyl group; R2 represents an optionally substituted phenyl group, a C1-20 alkyl group, a C1-20 alkenyl group, or—(CH2)k—[NH—(CH2)m—NH]n—Y or —(CH2)k—[NH—(CH2CH2O)m-1—CH2CH2NH]n—Y in which Y represents phosphatidylethanolamine residue or polyglutamic acid residue, k and m independently represent an integer of from 2 to 10, n represents 0 or 1, provided that when n represents 1, Y represents phosphatidylethyl group; R3 represents hydrogen atom or an optionally substituted hydroxyl group; R4 represents hydrogen atom, a halogen atom, azide group, an optionally substituted amino group, or an optionally substituted hydroxyl group; and R5, R6, R7 and R8 independently represent an optionally substituted hydroxyl group.
摘要翻译:一种用于治疗病毒感染的药物,其包含作为活性成分的由下式(I)表示的化合物或其药学上可接受的盐或其水合物或其溶剂合物。其中R 1表示氢原子或C1 -6烷基; R 2表示任选取代的苯基,C 1-20烷基,C 1-20链烯基或 - (CH 2)k - [NH-(CH 2)m -NH] n Y或 - (CH 2) [NH-(CH2CH2O)m-1-CH2CH2NH] nY其中Y表示磷脂酰乙醇胺残基或聚谷氨酸残基,k和m独立地表示2至10的整数,n表示0或1,条件是当n表示1时, Y表示磷脂酰乙基; R 3表示氢原子或任选取代的羟基; R 4表示氢原子,卤素原子,叠氮基,任选取代的氨基或任选取代的羟基; R 5,R 6,R 7和R 8独立地表示任选取代的羟基。
摘要:
Hydroxyazepanes display inhibitory activity with respect to glycosidase, with Ki values from-moderate to low micromolar range. Benzyl and 3,6-dibenzyl derivatives of hydroxyazepanes display inhibitory activity with respect to HIV protease. These compounds are synthesized either by chemoenzymatic or chemical methodologies.
摘要:
A polymer compound or a salt thereof which comprises a biodegradable polymer such as polyglutamic acid acetylated at N-terminal thereof containing a glycosphingolipid such as lysoganglioside GM3, and which exerts antiviral activity against variety of viruses and is useful as an active ingredient of a medicament.