P53 peptidomimetic macrocycles

FIELD: biotechnology.

SUBSTANCE: stable cross-linked p53 peptidomimetic macrocycle, a method for its preparation and its use are proposed. The p53 peptidomimetic macrocycle has a structure represented in the formula, and interferes with binding of p53 to MDM2 and/or p53 to MDMX. The P53 peptidomimetic macrocycle can be used to prepare pharmaceutical compositions for treatment of cancer characterized by undesirably low or low p53 activity and/or for the treatment of cancer characterized by undesirably high levels of MDM2 or MDMX activity.

EFFECT: proposed cross-linked p53 macrocycle has cell permeability that is at least twice as high as that of the corresponding macrocycle without cross-links.

50 cl, 7 dwg, 9 tbl, 22 ex

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to biotechnology and medicine. A compound (I) has an affinity to some subtypes of somatostatin receptors, and therefore can be used as a therapeutically active peptide in developing formulations of therapeutic agents for treating pathological conditions or diseases, which involve one or more somatostatin receptors. Besides, the compound (I) can be used as a peptide used as a carrier in prescription formulations.

EFFECT: what is presented is a new octapeptide compound of general formula (I): H-2-Nal1-cyclo(Cys2-Tyr3-AA4-Lys5-Val6-Cys7)-Thr8-NH2.

20 cl, 3 tbl, 25 ex

FIELD: medicine.

SUBSTANCE: present invention refers to biotechnology, more specifically to cyclic peptides of TNF, and can be used in medicine. The cyclic peptide consisting of CGQRETPEGAEAKPWYC is used to prepare a therapeutic agent for preventing or treating vascular complications in the patients suffering diabetes, including as a part of a pharmaceutical composition.

EFFECT: invention enables preventing the vascular complications in the patients with diabetes effectively, herewith inducing no TNF-mediated pro-inflammatory reaction.

8 cl, 5 dwg, 1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound selected from a group consisting of compounds presented by formula:

In the above formula, R1 represents S-Alk-R, wherein Alk represents methylene, C2-C6 polymethylene bond or C3-C6 alkenylene bond, R represents -N=C(NR3R4)(NR5R6) or -NR7[(NR3R4)C=NR5], or -N=C(R8)(NR9R10), wherein R3-R10 represents H, Alk, Ar or (CH2)nAr, wherein Ar represents an aryl group, and n represents an integer from 1 to 13, or R3 and R4, or R4 and R5, or R5 and R7, or R3 and R7, or R9 and R10, or R8 and R9 together can represent -(CH2)x-, wherein x represents an integer from 2 to 5, and R2 is specified in a group consisting of hydroxyl, alkyl having from 1 to 7 carbon atoms, and substituted by alkyl hydroxyl having from 1 to 7 carbon atoms.

EFFECT: preparing new cyclosporine derivatives.

5 cl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to cyclosporine analogues, which possess antiviral activity with respect to HCV, their pharmaceutical compositions and method of treating viral infection in person.

EFFECT: elaboration of method of treating viral infection in person.

12 cl, 1 tbl, 131 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound and a pharmaceutically acceptable salt thereof to be used as an antifungal agent, particularly, a therapeutic agent for deep fungal disease. The fungus Acremonium persicinum is collected, and a cyclic compound is recovered from its cultural fluid.

EFFECT: what is presented is the compound applicable as an antifungal agent.

10 cl, 16 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to cyclic cationic peptides and use thereof in treating fungal infections.

EFFECT: high efficiency of application.

14 cl, 4 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: invention refers to biologically active peptides able to inhibit myosin light chain kinase and thereby regulate the variability of vascular endothelial permeability. What is offered is a cyclic nonapeptide of formula cyclo[-Arg-Lys-Lys-Tyr-Lys-Tyr-Arg-Arg-Lys-].

EFFECT: peptide can find application as a decongestant in various fields of medicine.

2 dwg, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a novel cyclic peptide compound of pharmaceutically acceptable salt thereof, having activity against hepatitis C virus, based on inhibiting activity against replication of the hepatitis C virus RNA replicon, a pharmaceutical composition containing said compound or pharmaceutically acceptable salt thereof, and use of the compounds or pharmaceutically acceptable salt thereof to prepare a medicinal agent with anti-HCV activity.

EFFECT: high efficiency of the compounds.

9 cl, 19 tbl, 259 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a new cyclic peptide compound or its pharmaceutically acceptable salt which shows a hepatitis C virus activity based on an inhibiting activity of RNA replication of a hepatitis C virus replicon, to a method of producing it involving regrouping in a soft acid medium followed by amino acid exchange reactions, to a pharmaceutical composition containing said compound.

EFFECT: preparation of the drug exhibiting the anti-HCV activity.

16 cl, 44 tbl, 228 ex

FIELD: chemistry.

SUBSTANCE: in cyclosporine derivatives of general formula A, B, R1, R2 and X are defined in the description, for use in treating viral hepatitis C.

EFFECT: more effective treatment.

23 cl, 24 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula I and their pharmaceutically acceptable salts, method for preparing them by the fermentation of a microorganism of the species Streptomyces (PM0626271/MTCC 5447), and to their pharmaceutical compositions containing one or more compounds of formula I as an active ingredient.

EFFECT: compounds of formula I are used for treating and preventing the diseases caused by bacterial infections.

4 cl, 3 dwg, 6 tbl, 9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to RGD-containing cyclic peptidomimetics, conjugates of the said peptidomimetics and a functional group, selected from fluorescent probes, photosensitisers, chelating agents or cytotoxic agents; and to pharmaceutical compositions, which contain the said conjugates.

EFFECT: conjugates by the invention are suitable both for diagnostic purposes and for treatment of different diseases, disorders and states.

26 cl, 9 dwg, 10 tbl, 13 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) and their pharmacologically acceptable salts.

EFFECT: obtaining substances, which are applied for preparation of medicine for treatment and prevention of condition, in which inhibition of carboxypeptidase U is useful.

2 cl, 12 tbl, 5 ex

Cyclosporine // 2085589

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention deals with application of composition, which includes hydrolysate of pea protein and/or peptide for obtaining composition for treatment and/or prevention of infection Helicobacter pylori (versions), as well as such compositions (versions). Characterised compositions include lipid, protein and carbohydrate component, in which protein component includes protein source, which consists of pea protein hydrolysate, obtained by hydrolysis with protease, different from chymotrypsin, or from peptides, selected from group, which consists of Xaan-Asp-Phe-Leu-Glu-Asp-Ala-Phe-Asn-Val-Asn-Arg-Xaam and Xaan-Glu-Leu-Ala-Phe-Pro-Gly-Ser-Ala-Gln-Glu-Val-Asp-Arg-Xaam, where each Xaa independently can be any amino acid, and n and m are integer numbers, independently varying from 0-10, where peptide is contained in pea protein hydrolysate, or from both.

EFFECT: claimed inventions make it possible to treat or prevent diseases, caused by Helicobacter pylori infection, and/or diseases, associated with infection Helicobacter pylori in mammals.

17 cl, 2 tbl, 1 ex

FIELD: biotechnology.

SUBSTANCE: biologically active peptide is obtained, which has curative effect against Alzheimer disease, and consisting of the amino acid sequence Ala-Trp-Lys-Val-Leu-Ser-Pro-Gln-Gly-Gly-Gly-Pro-Trp-Asp-Ser-Val-Ala.

EFFECT: invention enables to use the resulting peptide to create a drug effective in the therapy of Alzheimer disease.

1 dwg, 2 ex

FIELD: medicine.

SUBSTANCE: skin regeneration is stimulated by using a synthetic analogue of indolicidine, a natural antimicrobial peptide having formula H-Lys-Lys-Pro-Trp-Lys-Trp-Pro-Lys-Lys-Pro-Trp-Arg-Arg-NH2.

EFFECT: accelerating reparative skin regeneration following a burn injury.

2 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of biochemistry, in particular to single variable domain, aimed against IL-6R, to polypeptide and construction, directed against IL-6R, containing said single variable domain, as well as to methods of obtaining them. Disclosed are nucleic acids, coding said single variable domain, polypeptide and construction, as well as genetic constructions, containing said nucleic acids. Described are host cells and host organisms, containing said nucleic acids. Invention also deals with composition for blocking interaction of IL-6/IL-6R, containing effective quantity of described single variable domain, polypeptide, construction, nucleic acid or genetic construction. Also disclosed is method of prevention and/or treatment of at least one of diseases or disorders, associated with IL-6, IL-6R, complex IL-6/IL-6R and/or signal pathways, in which IL-6, IL-6R or complex IL-6/IL-6R is involved and/or biological functions and reactions, win which IL-6, IL-6R or complex IL-6/IL-6R takes part with application of described single variable domain, polypeptide, construction or composition.

EFFECT: invention makes it possible to block interaction of IL-6/IL-6R effectively with increased affinity and biological activity.

25 cl, 70 dwg, 56 tbl, 61 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to polypeptides having hydrolysable covalent bonds with therapeutic agents for drug delivery. The invention also refers to pharmaceutical compositions which contain the compounds according to the invention, to using them in methods of treating cancer.

EFFECT: polypeptide conjugates can be used as vectors for a therapeutic agent transport through the blood-brain barrier (BBB) and for delivery into specific types of cells, such as the ovaries, liver, lungs or kidneys.

6 cl, 16 dwg, 8 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: invention refers to genetic engineering and can be used for methane-producing cell permeability control. What is prepared is a polypeptide able to permeate into a methane-producing cell and to increase its permeability, characterised by an amino acid sequence SEQ ID NO:117, 118 or 119 or being at least 90% identical to the above sequence, or at least 15 sequential amino acids of the above sequence. What is also prepared is a polynucleotide coding the above polypeptide cloning and expressing vectors used for producing host cells producing the polypeptide or used for the vector replication. The polypeptide can contain a fluorescent tag on an N-terminal amino acid residue.

EFFECT: invention enables providing higher methane-producing cell permeability.

18 cl, 35 dwg, 3 ex

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