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37 results about "Cyp3A4 Inducer" patented technology

Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14.13.97), is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body.

CYP3A4 gene SNP detection specific primer, liquid-phase chip and method

The invention discloses a CYP3A4 gene SNP detection specific primer, a liquid-phase chip and a method; and the liquid-phase chip comprises wild-type and mutant ASPE primers which are respectively designed for each type of mutation points, microspheres which are respectively coated with specific anti-tag sequences, and the primer which is used for amplifying a CYP3A4 gene target sequence with CYP3A4*1B, CYP3A4*2, CYP3A4*3, CYP3A4*4, CYP3A4*5, CYP3A4*6, CYP3A4*15, CYP3A4*17, CYP3A4*18 and / or CYP3A4*19SNP sites. The CYP3A4 gene SNP detection liquid-phase chip has very good signal-noise ratio, and a designed probe and the anti-tag sequences essentially have no cross reaction. The designed ASPE primers have very good specificity and can accurately distinguish all types of mutation points. The detection method has simple steps and ten types of SNP sites can be detected at one step, so that the operation is convenient, thereby preventing a plurality of uncertain factors in a plurality of operation processes, and greatly improving the detection accuracy rate.
Owner:SUREXAM BIO TECH

Inhibiting cyp3a4 induction

The present invention is directed to a method of inhibiting CYP3A4 induction. The method involves administering a compound of the following formula:R1—X—(CH2)n—N═C═Swith R1, X, and n defined herein, binds to a Pregnane X Receptor or Steroid and Xenobiotic Receptor (SXR or NR1I2) under conditions effective to inhibit CYP3A4 gene induction. The present invention also include a method of administering a compound, described herein, together with the CYP3A4 inducer to prevent a loss of efficacy in the subject to whom the CYP3A4 inducer is repeatedly administered. In addition, such compounds can be administered to block the interaction between a CYP3A4 inducer and another drug being administered that is a substrate of CYP3A4.
Owner:UNIV OF WASHINGTON

Isolation and identification of mouse and human transcription control elements associated with cytochrome expression

The present invention relates to transcription control elements derived from mouse and human genes associated with cytochrome expression, e.g., Cyp3A11 and CYP3A4, respectively. Isolated polynucleotides, expression cassettes, vectors, recombinant cells, and transgenic animals, may comprise such transcription control elements as described herein.
Owner:XENOGEN CORP

Methods of treatment

ActiveUS20190262328A1Avoid and reduce incidenceSafety managementOrganic active ingredientsNervous disorderDose ReducedReduced dose
The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug, wherein the patient is treated with posaconazole. In some embodiments, the patient stops posaconazole treatment, waits for at least 2 days, and then is treated with the CYP3A4 substrate drug as soon as it is safe to do so. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 2-42 days after stopping posaconazole. In some embodiments, the patient is treated with a reduced dose of the CYP3A4 substrate drug for about 2-42 days.
Owner:BOW RIVER LLC

Method of treating a patient with a CYP3A4 substrate drug

ActiveUS10376507B2Reduce morbidityAvoid and reduce incidenceNervous disorderHydroxy compound active ingredientsReduced doseCYP3A4 Inhibitor
The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug contraindicated for concomitant administration with a strong CYP3A4 inhibitor, wherein the patient is treated with multiple doses of posaconazole, stops posaconazole treatment, and then is treated with the CYP3A4 substrate drug. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 2-21 after stopping posaconazole. In some embodiments, the patient is treated with or prescribed a reduced dose of the CYP3A4 substrate drug for about 2-21 after stopping posaconazole.
Owner:BOW RIVER LLC

Methods of treatment

InactiveUS20180333411A1Avoid and reduce incidenceSafety managementNervous disorderHydroxy compound active ingredientsReduced doseCYP3A4 Inhibitor
The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug contraindicated for concomitant administration with a strong CYP3A4 inhibitor, wherein the patient is treated with multiple doses of posaconazole, stops posaconazole treatment, and then is treated with the CYP3A4 substrate drug. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 5-21 after stopping posaconazole. In some embodiments, the patient is treated with or prescribed a reduced dose of the CYP3A4 substrate drug for about 5-21 after stopping posaconazole.
Owner:BOW RIVER LLC

Gene marker for human hepatocellular carcinoma diagnosis

The present invention relates to a gene marker for diagnosis of human hepatocellular carcinoma (HCC), which is selected from the group consisting of IGF2, VEGF, MET, SUMO2, CDK4, MMP9, PLK1, AFP, Rb1, CYP3A4, LAP3, RIZ, DLC1, ITIH1, FetB, ALDOB, SULT2A1, ASS, HP, SERIND1, EI24, HGD, RODH, F2, SORD, and KNG. The HCC is diagnosed effectively and efficiently based on detecting the expression levels of the present gene marker from the liver tissue sample of an individual to be diagnosed.
Owner:NAT TAIWAN UNIV

Primers for detecting polymorphism of CYP3A4, CYP3A5 and MDR1 genes with ARMs-PCR (amplification refractory mutation system-polymerase chain reaction) method and prepared kit

The invention discloses primers for detecting polymorphism of CYP3A4, CYP3A5 and MDR1 genes with an ARMs-PCR (amplification refractory mutation system-polymerase chain reaction) method and a prepared kit. Primer sequences are shown in SEQ 1-SEQ 18. The primers can perform typing testing on CYP3A4, CYP3A5 and MDR1 genes of humans quickly and accurately through specific amplification after primer combination. Genetic typing or preparation of the typing kit can be performed according to the primers and the primers are used for detecting metabolic capacity of Chinese people for related drugs such as tacrolimus, cyclosporine A and the like, so that a reference basis can be provided for special doctors who determine optimal drug dosage and individual drug use, and drug use risks are reduced.
Owner:UNION STEMCELL & GENE ENG

DNA micro-array chip, detection method thereof and uses in CYP3A4, CYP3A5 and MDR1 gene polymorphism detection

The invention discloses a DNA micro-array chip and a detection method thereof and the application on detecting the polymorphism of CYP3A4, CYP3A5 and MDR1 genes. The chip comprises a solid phase carrier and a probe. The nucleotide sequence of the probe is shown as SEQ ID No: 1-SEQ ID No: 49. The probe is firstly arranged on the solid phase carrier. And then the target nucleotide sequence of a sample to be detected is marked and prepared. After that, the target nucleotide sequence is hybridized with the probe on the chip. Finally, the hybridization result is detected to obtain the information of the CYP3A4, CYP3A5 and MDR1 genes in the sample to be detected. The chip of the invention can be used for the detection of a plurality of genes of a plurality of samples simultaneously once only and has the advantages of simple operation and high result accuracy. Large amount of genetic information of patients can be obtained through detection once. The DNA micro-array chip and the detection method thereof can be used for instructing the formulation of reasonable drug schemes and realizing the personalized medical treatment.
Owner:SUN YAT SEN UNIV

Absolute quantitative method for biomass spectra of CYP450 enzyme hypotypes

The invention relates to an absolute quantitative method for biomass spectra of CYP450 enzyme hypotypes, and belongs to the technical field of proteomics. In the method, on the basis of liquid chromatography (LC) / mass spectrometry (MS) / MS, the absolute quantification of four CYP450 enzyme hypotypes, namely CYP1A2, CYP2B6, CYP3A4 and CYP3A5 in systems such as liver microsome and the like is realized simultaneously by a strategy that CYP450 generates specific peptide quantitative enzymes by pancreatic enzyme hydrolysis. The method mainly comprises the following steps of: preprocessing a proteinsample, preparing a standard curve, measuring the protein sample and preparing a quality control sample. The absolute quantitative method has excellent linear relations, is high in accuracy and repeatability, is sensitive, precise and reliable, and can be used for medicinal metabolism and the evaluation of the mutual effect of medicaments.
Owner:JILIN UNIV

Primer pair, kit and method for detection of related genes for guiding individualized administration of fentanyl drugs

The invention relates to a primer pair for the detection of related genes for guiding the individualized administration of fentanyl drugs. The primer pair comprises specific primers and a probe aimingat a CYP3A4*1G gene site. The invention relates to a kit for the detection of related genes for guiding the individualized administration of fentanyl drugs. The kit comprises a PCR reaction solutioncontaining the primers and the probe mentioned above, PCR buffer, dNTP, nuclease-free water, and HS Tag enzymes. The invention also relates to a method for the detection of related genes for guiding the individualized administration of fentanyl drugs. The provided kit and detection method thereof have the advantages that the operation is simple, the detection is rapid, the accuracy is high, the specificity and sensitivity are good, the use is convenient, and the clinical requirements can be satisfied effectively.
Owner:韩林志

Application of two-photon fluorescence probe for detecting cytochrome oxidase CYP3A4

The invention discloses application of a two-photon fluorescence probe for detecting cytochrome oxidase CYP3A4, and belongs to the technical field of biomedicine. The specific probe substrate can be used for measuring the enzyme activity of the CYP3A4 in a biological system. The procedure for determining CYP3A4 enzyme activity is as follows: Naphthalimide 4-position hydroxylation is selected as aprobe reaction, and the CYP3A4 enzyme activity in various biological samples can be determined by quantitatively detecting the amount of hydroxylated metabolites generated per unit time. The two-photon fluorescence probe can be used for quantitative evaluation of the CYP3A4 enzyme activity in the biological samples of different species and different individual sources, and quantitative determination of CYP3A4 activity in animal tissue cell culture fluids and cell preparations of different sources so as to realize evaluation of drug disposal capability of the important drug metabolizing enzymeCYP3A4. The two-photon fluorescence probe can also be used to rapidly screen inhibitors of the CYP3A4 in vitro, evaluate inhibitory ability of the inhibitors and detect the CYP3A4 activity in tumors,can detect the CYP3A4 activity in zebrafish, and can be used to detect drug-drug interaction of the CYP3A4 in vivo.
Owner:DALIAN MEDICAL UNIVERSITY

2, 3, 5, 7-tetrasubstituted dihydro-pyrazolo piperidine derivative and preparation method and application thereof

The invention provides 2, 3, 5, 7-tetrasubstituted dihydro-pyrazolo piperidine derivative and a preparation method and application thereof. The derivative is 2, 3-bis(substituted phenyl)-5-subsituted arylmethyl-7-substituted benzylidene dihydro-pyrazolo piperidine derivative, having the following formula (I). The preparation method includes using substituted arylmethyl amine and methyl acrylate as raw materials; subjecting the materials to Michael addition, Dieckmann condensation and hydrolysis-decarboxylation sequentially; allowing for Aldol reaction with substituted benzaldehyde to obtain intermediate N-substituted arylmethyl-3, 5-bis(substituted benzylidene)-4-piperidone; allowing for condensation with substituted phenylhydrazine to obtain a compound according to the formula (I). The derivative is efficient in inhibiting multiplication of various carcinoma cell lines such as leukemia, esophagus cancer, ovarian cancer and breast cancer in human, is well stably metabolic in liver microsomes of human and rat, is free of direct and competitive inhibition on five enzymes of liver microsomes, such as CYP3A4, CYP2D6, CYP2C9, CYP1A2 and CYP2C19, is highly bioavailable, is low in toxicity to normal cells, and is available for the preparation of drugs for the cancers.
Owner:SHANGHAI NORMAL UNIVERSITY

Method and kit for detecting SNP sites related to tacrolimus and cyclosporin A individalized medication

The invention relates to a method and kit for detecting SNP sites related to tacrolimus and cyclosporin A individalized medication. The detection method comprises the following steps: (1) designing specific primers aiming at CYP3A4, CYP3A5 and MDR1 genes; (2) performing specific polymerase chain reaction (PCR) amplification so as to obtain target fragments containing CYP3A4, CYP3A5 and MDR1 genes;(3) performing restrictive enzyme disgestion on PCR product fragments; (4) performing single base extension reaction; (5) performing desalting purification treatment; and (6) then detecting and analyzing gene sequences of target genes CYP3A4, CYP3A5 and MDR1 genes. The method for detecting SNP sites related to tacrolimus and cyclosporin A individalized medication is high in detection accuracy, high in experiment repeatability, great in flux and low in cost. The invention also provides a kit for detecting SNP sites related to tacrolimus and cyclosporin A individalized medication. The kit comprises a specific primer pair for amplifying CYP3A4, CYP3A5 and MDR1 genes. The kit for detecting SNP sites related to tacrolimus and cyclosporin A individalized medication has the advantages of simplified experimental procedure, short manual operation time, low difficulty and high experiment automation degree.
Owner:苏州道尔盾基因科技有限公司

Recombination human CYP3A4 (cytochrome P450 3A4) /CPR (cytochrome P450 oxidoreductase) /cyt b5 (cytochrome b5) protein co-transfection co-expression method

The invention discloses a recombination human CYP3A4 (cytochrome P450 3A4) / CPR (cytochrome P450 oxidoreductase) / cyt b5 (cytochrome b5) protein co-transfection co-expression method. Expression vectors with CYP3A4, CPR and cyt b5 cDNA (complementary deoxyribonucleic acid) fragments and screening plasmids are co-transfected into drosophila S2 cells, the expression vectors are integrated into a drosophila cell genome, the cells are screened with blasticidin to obtain stable monoclonal cell strains, and the stably transfected monoclonal cell strains are subjected to enlargement culture for induction expression of three kinds of protein including CYP3A4, CPR and cyt b5. According to the method, the recombination vectors are easy to build, high in stability and capable of expressing three kinds of protein simultaneously, and have the advantages of high expression quantity, high activity and the like. The method can be widely used for researches of drug metabolism in vitro, drug screening development and application and the like.
Owner:EAST CHINA NORMAL UNIV

Primer group for detecting renal cancer and detecting method thereof

The invention provides a primer group for detecting the renal cancer and a detecting method thereof. The primers provided by the invention consist of SEQ ID No.1 to SEQ ID No.18; the combined detection can be performed on MN / CA9, TS, CYP3A4, PD.L1, VEGFR2, cadherin-6, CK19, CD24 and EPCAM genes. The target gene expression and the expression level can be sensitively detected in short time by a PCR (polymerase chain reaction) or fluorescent quantitation PCR method; the optimized PCR conditions are adopted ; through increasing the cycle number of amplification reaction, the observation result is more obvious; the method applicability is further improved; the amplification product has specificity; high accuracy and sensitivity of PCR and RT-PCR fluorescent quantitative detection are ensured. When the primer group for detecting the renal cancer is implemented, the renal cancer can be simply, conveniently and accurately diagnosed by detecting the target gene expression in patient samples.
Owner:ZHEJIANG UNIV +2

Method for improving detoxification function of hepatocyte-like cells derived from human stem cells and application of method

The invention belongs to the field of biological medicine, and particularly relates to a method for improving a detoxification function of hepatocyte-like cells derived from human stem cells and application of the method. The method is characterized in that the stem cells are transfected with miR-142-3p inhibitors during stem cell hepatic differentiation, and the nucleotide sequence of the miR-142-3p inhibitors is shown as SEQ ID No.1. After differentiation of the stem cells, the miR-142-3p inhibitors are transfected, after transfection, differentiation is performed and molecular and functional testing of the hepatocyte-like cells is detected, it is found that on the 8th day of stem cell hepatic differentiation, 10nM of the miR-142-3p inhibitors are transfected, and enzyme activity of CYP2E1 and CYP3A4 is the highest. The method overcomes the disadvantage of low detoxification ability of the hepatocyte-like cells derived from the human stem cells, facilitates the development of an artificial liver and the in-depth study of medical research and development by using the hepatocyte-like cells derived from the human stem cells or the artificial liver.
Owner:THE FIRST AFFILIATED HOSPITAL OF ARMY MEDICAL UNIV

Detection of curative effect of antilipemic and antiatherosclerotic drug

The invention discloses a kit for detecting the curative effect of an individual antilipemic and antiatherosclerotic drug. The kit comprises a specific primer pair, a specific fluorescent probe pair, a fluorescence quantitative PCR conventional assembly and the like, and the specific primer pair is used for detecting a medication target site, namely a CYP3A4 gene, CYP2D6 gene and CYP2C9 gene polymorphism site of the statin drug. The kit can be used for estimating the curative effect of the individual antilipemic and antiatherosclerotic drug by detecting the medication target site, namely CYP3A4 gene, CYP2D6 gene and CYP2C9 gene polymorphism siteCYP3A4 gene, CYP2D6 gene and CYP2C9 gene polymorphism site of the statin drug.
Owner:XINBAXIANG SHANGHAI MOLECULAR MEDICAL TECH SHANGHAI

Derivatives of dillapiol and related monolignans and use thereof

Derivatives of dillapiol, sesamol and related monolignans having the following general formula:These compounds have synergistic properties, inhibit cytochrome P450 enzymes such as human CYP3A4, and can be used as pesticide synergists or pharmaco-enhancers. Accordingly, methods for increasing the efficacy and / or bioavailability of a pharmaceutically active agent and for increasing the potency of a pesticide are described, as are synergistic pesticidal and pharmaceutical compositions.
Owner:UNIVERSITY OF OTTAWA +1

Assay for Cytochrome P450 Isoforms 3A4 and 3A5

A rapid and sensitive radiometric assay for assessing the activity of cytochrome P450 (CYP) 3A4 / 5 and the potential of an analyte to inhibit CYP3A4 / 5 activity or induce CYP3A4 / 5 expression is described. All the steps of the assay, including incubations, product separation, and radioactivity counting are preferably performed in a multiwell format, which can be automated.
Owner:IST DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI

Polymorphisms in the human cyp3a4 and cyp3a7 genes and their use in diagnostic and therapeutic applications

Described are general means and methods of diagnosing and treating the phenotypic spectrum as well as the overlapping clinical characteristics with several forms of inherited abnormal expression and / or function of the CYP3A4 and CYP3A7 genes. In particular, polynucleotides of molecular variant CYP3A4 and CYP3A7 genes which, for example, are associated with insufficient metabolization and / or sensitivity of drugs, and vectors comprising such polynucleotides are provided. Furthermore, host cells comprising such polynucleotides or vectors and their use for the production of variant CYP3A4 and CYP3A7 proteins are described. In addition, variant CYP3A4 and CYP3A7 proteins and antibodies specifically recognizing such proteins as well as transgenic non-human animals comprising the above-described polynucleotide or vectors are provided. Described are also methods for identifying and obtaining inhibitors for therapy of disorders related to the malfunction of the CYP3A4 and CYP3A7 genes as well as methods of diagnosing the status of such disorders. Pharmaceutical and diagnostic compositions comprising the above-described polynucleotides, vectors, proteins, antibodies and inhibitors by the above-described method are provided. Said compositions are particularly useful for diagnosing and treating various diseases with drugs that are substrates, inhibitors or modulators of the CYP3A4 or CYP3A7 gene product.
Owner:TRANSGENOMIC

Methods for evaluating the ability to metabolize pharmaceuticals

Methods for detecting variant genes having a polymorphism associated with reduced metabolism of a substrate selected from the group consisting of a CYP3A4 substrate, a CYP3A5 substrate and a GSTM1 substrate in an individual are disclosed. The methods are genotyping methods to identify specific polymorphisms which have been found to be associated with reduced metabolism of chemotherapeutic agents, such as cyclophosphamide and BCNU. Also disclosed are novel polymorphic nucleic acid molecules useful in the methods of the invention.
Owner:GENAISSANCE PHARMA INC +2

Cytochrome P450 Induction Assay

A method for identifying compounds that can induce expression of cytochrome P450, in particular, expression of the CYP3A4 isoform, is described. The method provides a reporter gene operably linked to a composite promoter comprising in tandem one or more cis-acting elements, which are bound by activated pregnane X receptor (PXR), operably linked to a heterologous promoter. Analytes, which are inducers CYP3A4 expression via PXR activation, induce expression of the reporter gene.
Owner:IST DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI

Specific Probe Substrate of Cytochrome p450_3a4 Enzyme and Its Application

The invention provides a specificity probe substrate Tenuifoliside A of cytochrome P450-3A4 enzyme and application thereof in CYP3A4 enzyme activity measurement. The enzyme activity measurement includes the following operation processes: (1) with the Tenuifoliside A as the high-specificity probe substrate, carrying out a CYP catalytic reaction of a specificity substrate by means of a CYP in-vitro incubation system; and (2) quantitatively detecting the product generation amount or substrate consumption amount in unit time for determining the activity of the CYP3A4 enzyme in various bio-samples and cells. The specificity probe substrate can be used for quantitative evaluation of the CYP3A4 enzyme activity in the bio-samples from different individual sources, and quantitative measurement of the CYP3A4 single-enzyme activity of cell culture fluids and cell prepared products from different animal tissue cell sources.
Owner:GENERAL HOSPITAL OF PLA

CYP3A4 gene SNP detection specific primer, liquid-phase chip and method

The invention discloses a CYP3A4 gene SNP detection specific primer, a liquid-phase chip and a method; and the liquid-phase chip comprises wild-type and mutant ASPE primers which are respectively designed for each type of mutation points, microspheres which are respectively coated with specific anti-tag sequences, and the primer which is used for amplifying a CYP3A4 gene target sequence with CYP3A4*1B, CYP3A4*2, CYP3A4*3, CYP3A4*4, CYP3A4*5, CYP3A4*6, CYP3A4*15, CYP3A4*17, CYP3A4*18 and / or CYP3A4*19SNP sites. The CYP3A4 gene SNP detection liquid-phase chip has very good signal-noise ratio, and a designed probe and the anti-tag sequences essentially have no cross reaction. The designed ASPE primers have very good specificity and can accurately distinguish all types of mutation points. The detection method has simple steps and ten types of SNP sites can be detected at one step, so that the operation is convenient, thereby preventing a plurality of uncertain factors in a plurality of operation processes, and greatly improving the detection accuracy rate.
Owner:SUREXAM BIO TECH

CYP3A4 polypeptide and preparation method of polypeptide antibody to human CYP3A4

The invention discloses a preparing method to produce CYP3A4 polypeptide with amino acid sequence: SQNSKETESHKALSD and antihuman CYP3A4 polypeptide antibody, which comprises the following steps: (1)analysis of CYP3A4 antigen epitope; (2) synthesis of CYP3A4 polypeptide; (3)crosslinking of CYP3A4 polypeptide and carrier protein; (4) preparing antirabbit CYP3A4 polypeptide antibody; (5) assembling, separating to get serum with antibody; purifying antibody; getting antihuman CYP3A4 polypeptide antibody.
Owner:HARBIN MEDICAL UNIVERSITY
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