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51results about How to "Inhibition of transcriptional activity" patented technology
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Compositions and methods for inhibiting growth and metastasis of melanoma
InactiveUS20090054438A1Inhibition of transcriptional activityImpact their viabilityBiocideOrganic compound preparationAcetyl isogambogic acidCancer research
There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
Owner:SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INST
Polypeptide targeting to inhibit Wnt/beta-catenin signal activity and application thereof
ActiveCN110194787ASignificant effectSmall toxicityPolypeptide with localisation/targeting motifPeptide/protein ingredientsLymphatic SpreadBeta-catenin
The invention discloses a polypeptide targeting to inhibit beta-catenin or a derivative thereof, and an application thereof in drugs for treating and preventing tumors. The polypeptide has the following amino acid sequence: ARM7:Leu-His-Tyr-Gly-Leu-Pro-Val-Val-Val-Lys-Leu-His-Pro-Pro. The polypeptide is screened by a surface plasmon resonance (Biacore) method, has the abilities to specifically bind to TRIB3 and block the binding of TRIB3 and beta-catenin protein, inhibits the activity of Wnt / beta-catenin signaling pathways, and inhibits the growth and metastasis of tumor cells. Therefore, thepolypeptide and the derivative thereof are applied to the preparation of drugs for treating and preventing tumors. The prepared drugs can be used for treating tumors, such as colon cancer, liver cancer, lung cancer, pancreatic cancer, glioma and breast cancer.
Owner:INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
Traditional Chinese medicine extract composition with anti-skin stimulation effect and preparation method thereof
InactiveCN108014202AIt has the function of dispelling dampness and relieving itchingIncrease secretionDermatological disorderPlant ingredientsLigusticum chuanxiongSensitization
The invention discloses a traditional Chinese medicine extract composition with an anti-skin stimulating effect and a preparation method thereof, wherein the formula includes 1 to 20% of licorice, 1 to 20% of sophora flavescens, 1 to 20% of Scutellaria baicalensis, 1 to 20% of Chinese angelica, 1 to 20% of igusticum wallichii, 1 to 20% of herba schizonepetae, 1 to 20% of radices sileris and 1 to 20% of salix babylonica. The preparation methods includes S10, preparing of an ethanol extract of traditional Chinese medicines; S20, filtration, concentration, purification, and elution of the ethanolextract, and collection of eluate; S30, concentration of the eluate, addition of 1,3-butanediol, and collection of supernatant; and S40, obtaining of centrifugation supernatant. The composition can relieve external irritation to sensitive skin from multiple ways. The effective substances contained in the composition are all pure natural plant extracts, do not contain hormones, antihistamines, andthe like, thereby avoiding stimulation and sensitization effects of chemical agents on the skin.
Owner:SHANGHAI JAKA BIOTECH CO LTD
Site-Specific Nuclease Single-Cell Assay Targeting Gene Regulatory Elements to Silence Gene Expression
ActiveUS20160215280A1Inhibition of transcriptional activityImprove mobilityHydrolasesMicrobiological testing/measurementSilencing geneCell biology
This invention relates to a single cell assay for determining the effect of chromosomal contact on the transcriptional activity of genes of interest in a cell and to methods of silencing gene expression in a cell by way of perturbing gene regulatory elements which are engaged in chromosomal contact.
Owner:CSIR
Attenuated salmonella transporting recombinant plasmid and its application in treating tumor
ActiveCN1974759APlay a role in the treatment of tumorsEnhanced inhibitory effectSpecial deliveryBacteriaSalmonella wienLymphatic Spread
The present invention relates to attenuated salmonella transporting recombinant plasmid and its application in treating tumor, and belongs to the field of biotechnology. The present invention constitutes pH1Si-Stat3, pGRIM-19 and pGRIM-19-Si-Stat3 recombinant plasmid capable of expressing GRIM-19 and siRNA-Stat3 simultaneously, and translates the recombinant plasmid electrically into attenuated salmonella. Intracorporeal experiment proves that the coexpression of both GRIM-19 and siRNA-Stat3 results in excellent synergistic effect of inhibiting tumor growth and metastasis. Attenuated salmonella possesses tumor phagocytising characteristic and can propagate in tumor cell in the specificity to that in health cell over 1000 times, so that attenuated salmonella carrying transporting recombinant plasmid capable of expressing GRIM-19 and siRNA-Stat3 simultaneously to the depth of tumor can inhibit tumor growth and metastasis obviously.
Owner:吉林启众生物科技有限公司
Stable polypeptide used for resisting estrogenic receptor alpha and application thereof
InactiveCN108084249AStable helicityHigh membrane penetration abilityOrganic active ingredientsPeptide/protein ingredientsDrugChemistry
The invention provides a polypeptide of which the structure is disclosed in the description. The invention also provides application of the polypeptide for preparing a medicine capable of inhibiting the growth activity of positive cancer cells of estrogenic receptors. The invention develops one category of stable polypeptide estrogenic receptor antagonist which has relatively good stability and can penetrate through a cytomembrane. The antagonist can be combined with the activated estrogenic receptor alpha to inhibit the transcription activity of the estrogenic receptor alpha, relatively goodbiological activity is displayed, and the growth of the positive cancer of the estrogenic receptor is inhibited. Furthermore, the estrogenic receptor alpha is combined with a clinical medicine-tamoxifen to display better anti-cancer activity better than the anti-cancer activity obtained when medicines are singly used.
Owner:PEKING UNIV SHENZHEN GRADUATE SCHOOL
Application of p65 in preparation of medicament for up-regulating SIRT1 expression
InactiveCN102049039AInhibition of transcriptional activityNervous disorderPeptide/protein ingredientsMitophagyCancer research
The invention relates to application of p65 in preparation of a medicament for up-regulating silence information regulator 1 (SIRT1) expression. Particularly, the medicament is a purified protein type medicament, and the formulation of the medicament is the one suitable for protein medicament application; and particularly, the medicament is a recombinant nucleic acid construct for expressing p65 protein. The invention also relates to application of p65 in preparation of a medicament for treating diseases of mammals comprising people benefiting from SIRT1 expression up-regulation, wherein the diseases of mammals comprising people benefiting from SIRT1 expression up-regulation are selected from metabolic syndromes, tumors, neurodegenerative diseases, cardiovascular diseases, inflammations or mitochondria related diseases.
Owner:THE INST OF BASIC MEDICAL SCI OF CHINESE ACAD OF MEDICAL SCI
Dual inhibitors of AR and BET and use thereof
PendingCN110960528AHepatic drug enzyme metabolism stability is goodRepress transcriptionAntibacterial agentsIsotope introduction to heterocyclic compoundsDiseaseMetabolite
The present invention provides a polycyclic compound represented by formula (I) and a use in dual inhibitors of AR and BET. Specifically, the present invention provides the use of a compound represented by formula (I) or optical isomers, solvates, pharmaceutically acceptable salts, prodrugs, tautomers, mesomers, racemates, enantiomers, diastereomers, mixture form, metabolites, metabolic precursorsor isotopic substitution form thereof in the preparation of dual inhibitors of AR and BET. Experimental results show that the compounds of the present invention can not only inhibit the transcriptionof PSA and FKBP5 downstream of AR, but also inhibit the transcriptional activity of AR-F876L mutants resistant to anthralin, and also downregulate the expression of BRD4 downstream protein c-Myc, andthe compounds have good binding affinity to AR and BET proteins. The experiment suggests that the compound of the present invention can inhibit the activity of AR and BET protein at the same time, and has a good application prospect in the preparation of medicine for preventing and / or treating diseases related to BET protein.
Owner:SICHUAN UNIV
Application of ailanthone to preparation of medicines for treating prostatic disease
ActiveCN105078969AGrowth inhibitionInhibits androgen receptor activityOrganic active ingredientsAntineoplastic agentsReceptor for activated C kinase 1Chinese traditional
The invention provides application of ailanthone (AIL) which is shown in a formula (I) and is a monomer of Chinese traditional herbs to preparation of medicines for treating prostatic disease. By a compound, in-vitro and / or in-vivo growth and migration of prostate carcinoma cells can be suppressed obviously, protein expression level of an androgen receptor in the prostate carcinoma cells is reduced, and a signal path of the androgen receptor is suppressed. The compound has a prostate cancer treatment application prospect.
Owner:EAST CHINA NORMAL UNIVERSITY
Cell growth inhibitor and screening method thereof
InactiveUS20130184327A1Growth inhibitionSuppresses transcriptional activity of signalOrganic active ingredientsSugar derivativesBinding siteScreening method
An object is to provide a cell growth inhibitor also effective for androgen-independent prostate cancer. The present invention provides a cell growth inhibitor having, as an active ingredient, an expression inhibitor or function inhibitor of an antisense RNA (CTBP1-AS) expressed in the vicinity of an androgen receptor (AR) binding site of a C-terminal binding protein (CTBP1) gene.
Owner:THE UNIV OF TOKYO
Benzothiazole meroterpenoid compounds and derivatives thereof, and preparation method and application thereof
ActiveCN112047901ANovel structureSimple stepsOrganic chemistryMicroorganism based processesTumor targetThiazole
The invention relates to a benzothiazole meroterpenoid compound derived from deep sea fungi and a derivative, a preparation method and application thereof in antitumor drugs. The benzothiazole meroterpenoid compound is a compound shown as formulas I to III or salts thereof. The compound is separated from a fermentation product of Penicillium allii-sativi and inhibits the transcriptional activity of RXRalpha by combining with an anti-tumor target RXRalpha so as to achieve a remarkable anti-tumor effect. The compound can be used for preparing, researching and developing anti-cancer drugs, and has a good application prospect.
Owner:THIRD INST OF OCEANOGRAPHY MINIST OF NATURAL RESOURCES
New medicinal application of morin hydrate
InactiveCN105311012AInhibition of transcriptional activityInhibition of in vitro effectsOrganic active ingredientsMetabolism disorderC57BL/6 MouseWeight gain
The invention discloses a new medicinal application of morin hydrate, wherein the new medicinal application refers that the morin hydrate is used as an active component for preparing a liver X receiver-[beta] antagonist and as an active component for preparing a medicine for preventing, alleviating and / or treating metabolic diseases induced by the liver X receiver-[beta]. A test result proves that the morin hydrate can selectively inhibit transcriptional activity of the LXR-[beta] and has a significant in-vitro effect of inhibiting differentiation of fat cells, and also has the in-vivo effects of blocking C57BL / 6 mouse weight gain induced by high-fat diet, inhibiting volume gain of body fat cells, improving fasting blood-glucose, insulin resistance and dyslipidemia of mice. The morin hydrate is hopeful to be developed into a low-toxic and high-effective LXR[beta] receiver antagonist and the medicine for preventing, alleviating and / or treating the metabolic diseases induced by the liver X receiver-[beta].
Owner:SHANGHAI UNIV OF T C M
Novel aryl ethene derivative and pharmaceutical composition containing same as active ingredient
ActiveUS20200078476A1Strong inhibitory activityHigh activityOrganic chemistryRadioactive preparation carriersArylReceptor
Owner:DAEGU GYEONGBUK MEDICAL INNOVATION FOUND +2
Novel aryl ethene derivative and pharmaceutical composition containing same as active ingredient
InactiveUS20190167820A1Strong inhibitory activityImprove drug stabilityOrganic chemistryRadioactive preparation carriersArylEstrogen-related receptor gamma
The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERRγ) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient.
Owner:HWANG SUNG YEOUN +1
New application of casein kinase2-interacting protein-1 (CKIP-1) protein and coding gene thereof
InactiveCN102793910AIncreased sensitivitySpeed up entryPeptide/protein ingredientsGenetic material ingredientsDiseaseClinical diagnosis
The invention discloses new application of a casein kinase2-interacting protein-1 (CKIP-1) protein and a coding gene thereof. The invention provides the CKIP-1 protein, the coding gene of the CKIP-1 protein or application of plasmids containing the coding gene of the CKIP-1 protein in preparation of medicaments for preventing and / or treating myocardial hypertrophy; and the CKIP-1 protein is shown as a sequence 1 of a sequence table. The regulating effect of the CKIP-1 protein and the coding gene thereof in myocardial hypertrophy diseases is discovered, so that a new target and a new method are sought for diagnosis and treatment of the myocardial hypertrophy, and a foundation is laid for seeking clinical diagnosis and treatment of related diseases. The new application has great value for treating and preventing the myocardial hypertrophy.
Owner:SCI RES TRAINING CENT FOR CHINESE ASTRONAUTS +1
Coumarin esterified derivative with effect of inhibiting transcriptional activity of RXRalpha (Retinoid X Receptor) as well as preparation method and application of coumarin esterified derivative
InactiveCN107089963AReduce yieldShort reaction timeOrganic chemistryAntineoplastic agentsSolventTranscriptional activity
The invention discloses a coumarin esterified derivative with an effect of inhibiting transcriptional activity of RXRalpha (Retinoid X Receptor) as well as a preparation method and application of the coumarin esterified derivative. The coumarin esterified derivative is a 4-chloromethyl-7-hydroxy coumarin esterified derivative shown by the following general formula. The invention also discloses a preparation method of the 4-chloromethyl-7-hydroxy coumarin esterified derivatives. The preparation method comprises the following steps: preparing 4-chloromethyl-7-hydroxy coumarin under solvent-free conditions by taking anhydrous bismuth chloride as a catalyst; preparing corresponding acyl chloride through different side chain acids; and reacting with the 4-chloromethyl-7-hydroxy coumarin, thereby obtaining the corresponding compound. The coumarin esterified derivative disclosed by the invention has a certain effect of inhibiting the transcriptional activity of RXRalpha and provides a thought for developing medicines taking the RXRalpha as a target. The structural formula is as shown in the specification.
Owner:XIAMEN UNIV
Pharmaceutical use of protopanaxatriol or/and derivatives thereof
InactiveCN104490896AStrong therapeutic activityInhibition of volume increaseOrganic active ingredientsMetabolism disorderDyslipidemiaIn vivo
Owner:SHANGHAI UNIV OF T C M
Triaromatic ring compounds targeting STAT3 bifunctional phosphorylation site and application thereof
ActiveCN112300145AImprove bindingPromote apoptosisOrganic active ingredientsOrganic chemistryMetaboliteSimple aromatic ring
The invention discloses triaromatic ring compounds targeting an STAT3 bifunctional phosphorylation site. The triaromatic ring compounds are compounds shown as formulas (I)-(V) or pharmaceutically acceptable salts, hydrates, solvates, metabolites or prodrugs thereof. The invention further provides a pharmaceutical composition containing the compounds shown in the formulas (I)-(V). The invention also provides application of the triaromatic ring compounds in preparation of medicines for preventing and / or treating diseases caused or regulated by STAT3 bifunctional phosphorylation site activation.
Owner:SHANGHAI YUYAO BIOTECH LTD
Application of Sphondin as effective component in preparation of drugs for treating hepatitis B
InactiveCN113069445AInhibition of secretionRepress transcription levelDigestive systemAntiviralsLiver tissuePharmaceutical Substances
Owner:CHONGQING MEDICAL UNIVERSITY
New application of drug screening cell model targeting HBV core promoter, Tricirine and structural analogue
ActiveCN113025651AInhibition of transcriptional activityCompound screeningApoptosis detectionHepatitis B immunizationHbv replication
The invention discloses a plasmid pcore-HU-SMAR, a framework vector of the plasmid pcore-HU-SMAR is plasmid PCMV-Gluc, a HiBiT-unaG fusion gene is inserted into the framework vector, the HiBiT-unaG fusion gene is connected with a puromycin resistance gene through a T2A sequence, an SMAR sequence is inserted between the puromycin resistance gene and a polyA sequence, and the HiBiT-unaG fusion gene is a fusion gene of a luciferase tag HiBiT and a fluorescent protein reporter gene UnaG. The invention further discloses a drug screening cell model of the targeted HBV core promoter, wherein the drug screening cell model is obtained by transfecting the AML12 with the plasmid pcore-HU-SMAR. The invention further discloses application of Tricirine and a structural analogue thereof to preparation of a medicine for inhibiting HBV core promoter transcription and / or HBV replication or application of the Tricirine and the structural analogue thereof to preparation of a medicine for treating hepatitis B.
Owner:CHONGQING MEDICAL UNIVERSITY
Method for inhibiting geminivirus infection by using arabidopsis ABI5 protein overexpression
ActiveCN114107321AEffect controlInhibition of transcriptional activityVectorsPlant peptidesPromoterArabidopsis sp.
The invention discloses a method for inhibiting geminivirus infection by overexpression of arabidopsis ABI5 protein, which inhibits transcription of geminivirus coding genes by overexpression of plant transcription factor ABI5 protein and combination of ABI5 protein and a promoter of geminivirus through specificity, and realizes improvement of virus resistance of plants.
Owner:SOUTH CHINA NORMAL UNIVERSITY
Application of small-molecule inhibitor to preparation of antitumor medicine
ActiveCN112294812AInhibition of transcriptional activityEnhanced inhibitory effectOrganic active ingredientsAntineoplastic agentsPharmacophorePharmaceutical drug
The invention belongs to the field of biological medicines, and particularly relates to a differentiation inhibition factor 2, namely an ID2 inhibitor, and an application of the inhibitor to preparation of brain glioma medicines. According to the research, an effective ID2 inhibitor is obtained through a computer pharmacophore virtual screening technology and CCK-8 cytotoxicity experiment. Throughdetection by a surface plasmon resonance technology, the inhibitor is found to have high affinity with ID2. In-vitro and in-vivo experiments show that the inhibitor can reduce the expression of the ID2 in glioma and significantly inhibit the proliferation of glioma cells, and has potential clinical application prospects.
Owner:XINXIANG MEDICAL UNIV
Aryl ethene derivative and pharmaceutical composition containing same as active ingredient
ActiveUS10934303B2Strong inhibitory activityHigh activityOrganic active ingredientsSenses disorderArylReceptor
The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERRγ) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient.
Owner:NOVMETAPHARMA CO LTD
Cell growth inhibitor and screening method thereof
InactiveUS8853182B2Growth inhibitionInhibition of transcriptional activityOrganic active ingredientsMicrobiological testing/measurementAndrogenScreening method
Owner:THE UNIV OF TOKYO
Site-specific nuclease single-cell assay targeting gene regulatory elements to silence gene expression
InactiveUS20190112592A1Inhibition of transcriptional activityImprove mobilityHydrolasesMicrobiological testing/measurementSilencing geneCell biology
This invention relates to a single cell assay for determining the effect of chromosomal contact on the transcriptional activity of genes of interest in a cell and to methods of silencing gene expression in a cell by way of perturbing gene regulatory elements which are engaged in chromosomal contact.
Owner:CSIR
Peptide having anticancer activity, and pharmaceutical composition and dietary supplement composition for preventing and treating cancer, both of which contain same as active ingredient
ActiveUS10611797B2Inhibitory activityImprove efficiencyPolypeptide with localisation/targeting motifPeptide/protein ingredientsCancer preventionCancer cell
A peptide binding to transcription factor CP2c, having an activity of preventing and treating cancer and represented by SEQ ID NO: 1: Asn-Tyr-Pro-Gln-Arg-Pro, and a pharmaceutical composition and a dietary supplement composition for preventing and treating cancer, both of which contain the same as an active ingredient are disclosed. When cancer cells are treated with the peptide and the pharmaceutical composition containing the same, the peptide can specifically bind to CP2c by passing, with very high stability, through the cell membrane and can inhibit the DNA binding ability of CP2c, thereby disturbing CP2c-mediated cancer cell-specific transcriptional activity through the inhibition of CP2c activity. Thus, the peptide and pharmaceutical composition containing the same can be effectively used for specifically treating only cancer cells and can be utilized for cancer prevention and as a dietary supplement additive therefor.
Owner:KONKUK UNIV GLOCAL CAMPUS IND COOP FOUND
Cell growth inhibitor and screening method thereof
InactiveUS8796240B2Growth inhibitionInhibit expressionOrganic active ingredientsGenetic material ingredientsBinding siteScreening method
An object is to provide a cell growth inhibitor also effective for androgen-independent prostate cancer. The present invention provides a cell growth inhibitor having, as an active ingredient, an expression inhibitor or function inhibitor of an antisense RNA (CTBP1-AS) expressed in the vicinity of an androgen receptor (AR) binding site of a C-terminal binding protein (CTBP1) gene.
Owner:THE UNIV OF TOKYO
Novel application of Danhong blood stasis dispersing composition
The invention discloses application of a Danhong blood stasis dispersing composition as a silent mating type information regulation 2 homolog 1 (SIRT1) agonist. The Danhong blood stasis dispersing composition comprises seven traditional Chinese medicines of salvia miltiorrhiza, Chinese angelica, ligusticum wallichii, peach kernel, safflower, bupleurum root and bitter orange. As the SIRT1 agonist,the Danhong blood stasis dispersing composition can regulate the expression of SIRT1 protein in blood vessels and play a key role in the prevention and treatment of related diseases. In particular, the Danhong blood stasis dispersing composition has fast onset time and definite effect, and can be used for early prevention of venous embolic diseases.
Owner:GUANGZHOU BAIYUSN HUTCHISON WHAMPOA CHINESE MEDICINE
Application of gene sox10 as a target in the preparation of drugs for delaying adaptive drug resistance of melanoma
ActiveCN108203733BInhibition of tumor suppressor effectPromotes tumor suppressive effectMicrobiological testing/measurementMelanomaAkt signalling
The invention discloses the application of a gene SOX10 as a target in the preparation of medicines for delaying the adaptive drug resistance of melanoma. It is disclosed that the SOX10 gene is a keyregulator of how an inhibitor induces FOXD3 expression to produce adaptive drug resistance; and further experiments indicate that down-regulation of SOX10 expression can effectively inhibit the FOXD3 / ERBB3 / AKT signaling pathways and significantly promote inhibitor-induced cells apoptosis and down-regulation of SOX10 expression significantly promotes the tumor suppression effect of RAF inhibitors and significantly inhibits the FOXD3 / ERBB3 / AKT signaling pathway in tumor tissues. Therefore, the gene SOX10 can be used as the target in the preparation of the medicines for delaying the adaptive drugresistance of melanoma, to prepare better and more medicines that delay the adaptive drug resistance of melanoma.
Owner:XI AN JIAOTONG UNIV
2-fuloro fumarate (formula I), and preparation method and application thereof
ActiveCN103483194AIncrease the difficulty of purificationLow yieldOrganic active ingredientsSenses disorderPsoriasisTranscriptional activity
The invention discloses 2-fuloro fumarate (formula I) and a preparation method thereof. Experiments show that: the kinds of compounds are capable of effectively inhibiting NF-kB transcriptional activity introduced by TNF-alpha, and further are capable of treating diseases introduced by NF-kB, such as psoriasis, multiple sclerosis, arthritis, eye inflammation or allergy, asthma and lupus erythematosus, and can be used as an immunosuppressant for organ transplantation.
Owner:深圳市博圣康生物科技有限公司
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