33 results about "Hiv 1 integrase" patented technology

Peptides comprising an Rpt1 domain of an INI1 / hSNF5 which inhibit HIV-1 production in a human cell, and vectors encoding those peptides are provided. Also provided are methods of inhibiting HIV-1 production in a cell, or spread of the HIV-1 to another cell, by treating the cells with the above peptides or vectors. Other methods of inhibiting HIV-1 production in a cell, or spread of the HIV-1 to another cell, by inhibiting production of INI1 / hSNF5 are provided. Additionally, methods of determining whether a test compound inhibits HIV-1 virion production in a mammalian cell, or spread of the HIV-1 to another cell, are provided. Those methods comprise determining whether the test compound inhibits the production of INI1 / hSNF5 or disrupts the interaction of HIV-1 integrase with INI1 / hSNF5.

Isolated peptides comprising sequences derived from the protein integrase of HIV-1, as well as their analogs, mixtures, conjugates with permeability enhancing moieties, and pharmaceutical compositions are disclosed. The peptides and compositions are capable of selectively killing HIV-1 infected cells and are used in treatment of HIV infection and AIDS.

The invention provides a preparation method of a fungal extract for inhibiting human immunodeficiency virus (HIV-1). The dependent bacterial strain is hypoxylon fungi Q-s-4(hypoxylon sp.). The fungi Q-s-4 is fermented and cultured in liquid to prepare extract of fermentation products. The method can be applied to the mass industrial culture of fungi Q-s-4 and industrial production of extract of fermentation products by taking fermentation products as the raw materials. The extract prepared by the method has a prominent activity on inhibiting HIV-1 integrase, an antibacterial activity, and an important value on research and development of novel drugs for curing AIDS and bacterial infections.

The invention discloses a method for preparing a soluble HIV-1 integrase recombinant protein, and belongs to the technical field of biology. The preparation method comprises the steps of induced expression, bacteria disruption, purification and the like. The adopted expression medium contains 15 to 35 g / L of tryptone, 10 to 20 g / L of yeast extract, 2 to 3 g / L of sodium chloride, 1 g / L of glucose, 10 to 15 g / L of glycerin, 2.05 g / L of disodium hydrogen phosphate, 1.27 g / L of sodium dihydrogen phosphate, 50 mg / L of magnesium sulfate, and 60 mg / L of kanamycin; and the adopted cracking buffer solution contains 20 mM of 4-hydroxyethyl piperazine ethanesulfonic acid, 1 M of sodium chloride, 2 mM of beta-mercaptoethanol, 0.3 mg / ml of lysozyme and 5 mM of imidazole, and the pH value of the buffer solution is 9.0. The expression medium can ensure normal growth of host bacteria and efficient expression of the objective protein; and the cracking buffer solution can enhance the disruption effect of bacteria, improve the solubility of the objective protein and finally improve the yield of the objective protein.

The invention provides an integrase inhibitory peptide, which is one of seven polypeptide organic compounds selected from a, b, c, d, e, f, and g, soluble in water, and connected by peptide bonds between amino acids, capable of inhibiting HIV-1 integrase activity, the molecular weights are: 974.3, 770.8, 822.9, 830.9, 849.0, 789.8, 788.8. The polypeptide organic compound of the invention can inhibit the activity of HIV-1 integrase, interrupt the proliferation of virus DNA in host cells and its life cycle, and can be used in the preparation of drugs for treating AIDS. At the same time, it can also be used for further research on the structure, mechanism of action of integrase and AIDS treatment drugs.

The invention discloses a preparation method for a drug for treating aids. A chemical structure of the drug is shown in formula (I); when concentration is 5 mu g / ml, an inhibition ratio of a compoundHIV-1 integrase as shown in formula (I) is 45%-95%, and an inhibition ratio of Ib is as high as 94.8%, which exceed the inhibition ratio of the drug elvitegravir in the market. The inhibition ratio ofIa is low which is lower than 50%. The compound as shown in the formula (I) can be used as HIV-1 integrase inhibitor for treating aids.

The present invention discloses one kind of compound, citiofuran. The compound, citiofuran has very high combination activity, KD=16.4 microM, with HIV-1 integrase, and effective inhibition of the combination of the integrase to the substrate, IC50=120 microM, in substrate competition test. Therefore, the compound exhibits very high medicine preparing value.

The invention belongs to the technical field of medicine compounds, and discloses a 1-N-substituted benzyl-6-N'-substituent-2,3,6,9-tetralin-1H-[1,4] benzoxazine [3,2-g] quinolone-9-ketone-8-formic acid compound and a preparation method and application thereof. According to the formula (I) of the 1-N-substituted benzyl-6-N'-substituent-2,3,6,9-tetralin-1H-[1,4] benzoxazine [3,2-g] quinolone-9-ketone-8-formic acid compound, R1 represents a benzyl or a substituted benzyl, and R2 represents hydrogen or an alkyl or a hydroxyalkyl or a substituted benzyl or a carboxyalkyl. The method comprises the steps that firstly, 2-amino-5-nitrophenol is used as a raw material, acetylation protection, affinity substitute ring closure and deprotection are performed, affinity substitute is introduced into substituted benzyl, nitro reduction is performed through stannous chloride, condensation is performed, Gould-Jacobs reaction ring closure is performed, affinity substitute is introduced into different substituent groups, and finally hydrolysis is performed to obtain the compound of the formula (I). The compound has the inhibiting effect on the HIV-1 integrase.

The invention relates to a (E)-N-3-(4-substituted benzene propenyl piperazine-1-base) alkyl benzamide compound shown in a formula (I) or a salt thereof, wherein R<1>, R<2> and R<3> express -H, -OH, -ONa, -OK or -ONH4, R<4> and R<5> express-H, halogen, C(1-3) linear or branched alkyl, -OH, -ONa, -OK, -ONH4, -NO2 or -CN, and n is an integer of 1-3. The invention also relates to a preparation methodof the compound, which comprises the following steps: synthesizing multi-alkoxy benzoyl chloride substituted alkylamine by using multi-substituted benzoyl chloride and hydrochloride of chlorinated alkyl amino as raw materials; carrying out reaction on the compound and piperazine to prepare N-piperazinyl alkyl multi-substituted benzamide; reacting with substituted benzene acryloyl chloride to prepare (E)-N-3-(4-substituted benzene propenyl piperazine-1-base) alkyl benzamide; acting with BBr3 or BF3 aether solution to be further hydrolyzed to generate the corresponding (E)-N-3-(4-substituted benzene propenyl piperazine-1-base) alkyl polyhydric benzamide compound, and then reacting with alkaline to generate the corresponding salt. The compound has inhibition function to HIV-1 integrase.