48 results about "Egfr expression" patented technology

The present invention provides p97-antibody conjugates and related compositions and methods, which may be used in any of a variety of therapeutic methods, including methods for the treatment of cancers such as Her2 / neu-expressing and Her1 / EGFR-expressing cancers.

Methods for labeling synthesis of radiolabeled gallium complex by microwave activation are provided. The resultant gallium-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). A method for imaging EGFR overexpression in tumors using PET is also provided.

The invention relates to biomarkers based on gene expression products and methods for determining the efficacy of anti-EGFR antibodies in the treatment of EGFR expressing cancer. The invention is further related to the prediction of sensitivity or resistance of a patient suffering from EGFR expressing cancer to the treatment of said patient with a specific anti- EGFR antibody. The invention is preferably related to the identification of respective biomarkers that allow a better prediction of the clinical outcome of the treatment with anti- EGFR antibodies in patients with KRAS wild-type tumors. In this context, the invention especially relates to anti-EFGR antibody c225 / cetuximab (Erbitux TM ) and its use in patients suffering from colorectal Cancer (CRC).

The invention discloses a siRNA inhibiting EGFR expression as well as precursor sequence and an application of siRNA. The EGFR siRNA can highly inhibit EGFR gene expression, and an in-vivo experimentshows that the EGFR siRNA has a certain inhibition effect on EGER tumors with high expression. The precursors and carriers of siRNA can form stable siRNA in a host and come into effect.

The invention discloses wild type EGFR stably and high expressing recombinant HEK 293-EGFR cells constructed on the basis of exogenous recombinant plasmids pcDNA3.1(+)-EGFR, which can improve the expression of EGFR by 4 to 5 times compared with the expression before transfection. EGF serving as an EGFR accelerator and gefitinib serving as a tyrosine kinase inhibitor are used to induce transfected HEK293 cells, and the examination of the change of the number of expressed phosphorylated EGFR and ERK in the cells shows that the transfected EGFR has activities; the medicinal gefitinib also has an inhibiting effect on the transfected EGFR, so EGFR-targeted medicament screening can improve the screening specificity and flexibility; and the wild type EGFR stably and high expressing recombinant HEK 293-EGFR cells can be used in comparative researches on the differences of EGFR pathway proteins.

The invention discloses an EGFR positron tracer, a preparation method and application thereof. The structural formula of the EGFR positron tracer is shown as the specification. The EGFR positron tracer has good tracing effect, and compared with 18F-FDG that is the most common in clinical practice at current, the tracer has very good specificity, can achieve positive identification of epidermal growth factor receptor (EGFR) high expression tumors. The preparation method is convenient, simple and fast, can realize fully automatic production, and can meet scientific research and clinical demands. In the aspect of application, the PET imaging of 18F-Erlotinib not only can be used for screening of clinical anticancer drug Erlotinib sensitive individuals, and also has very good application prospects in detection of EGFR expression level and screening of small molecule EGFR inhibitors in the pharmaceutical industry.

The invention relates to a small interference RNA recombinant adenovirus of a targeted epidermal growth factor receptor and the role the recombinant adenovirus plays in inhibiting the in vivo growth of the human lung adenocarcinoma cell, belonging to the technical field of biotechnique. The small interference RNA recombinant adenovirus adopts the technical proposal that: an adenovirus vector system is used to construct a shuttle vector and a backbone vector, so as to conduct homologous recombination in a packaging cell 293 and obtain the replication-deficient recombinant adenovirus. By giving specific attention to the difficulties of lung cancer treatment and gene regulation technique, the small interference RNA recombinant adenovirus constructs the expression vector of the small interference RNA virus; therefore, the small interference RNA recombinant adenovirus of a targeted epidermal growth factor receptor has the advantages of improving the introduction efficiency of the small interference RNA, and prolonging the time of the RNA interference effects. Moreover, the experiments done in animal body prove that: the small interference RNA recombinant adenovirus can generate RNA interference effect, down-regulate the EGFR expressions, and inhibit the growth of the tumor.

The invention relates to the technical field of radioactive medicinal chemistry and clinic nuclear medicine and particularly relates to a 68Ga marked EGFR targeted tracer agent 68Ga-NOTA-ZEGFR:1907 and a preparation method and application thereof. The molecular imaging probe 68Ga-NOTA-ZEGFR:1907 is specific and targeted to combination of EGFR; a HCC827 hetero-transplanted tumor can be displayed clearly after injection of 30 min, and tumor imaging quality is good in a later period (tumor uptake values are 2.58% ID / g and 2.69% ID / g after injection of 1 h and 2 h respectively); the tumor uptake values are higher than uptake values of most other organs, and satisfactory imaging effects can be obtained; and an autoradiography grey level of 68Ga-NOTA-ZEGFR:1907 in a human tumor tissue specimen is in positive linear correlation with an EGFR expression degree (R2=0.62, P (0.0001).

The invention provides a compound, which is obtained by splicing a heptamethine cyanine structure and an epidermal growth factor receptor(EGFR) targeted drug molecular structure. The compound providedby the invention can be used as a hypoxia and EGFR double-targeted near infrared fluorescence probe, can realize the purpose of accurate imaging on malignant tumor lesions with high EGFR expression by targeting the tumor marker EGFR and the hypoxia state of tumor cells; in addition, the compound provided by the invention can be used as a photosensitizer for cancer treatment.

The invention relates to biomarkers based on gene expression products and methods for determining the efficacy of anti-EGFR antibodies in the treatment of EGFR expressing cancer. The invention is further related to the prediction of sensitivity or resistance of a patient suffering from EGFR expressing cancer to the treatment of said patient with a specific anti-EGFR antibody. The invention is preferably related to the identification of respective biomarkers that allow a better prediction of the clinical outcome of the treatment with anti-EGFR antibodies in patients with KRAS wild-type tumors. In this context, the invention especially relates to anti-EFGR antibody c225 / cetuximab (Erbitux®) and its use in patients suffering from colorectal Cancer (CRC).

The present invention concerns polymorphisms in the epidermal growth factor receptor (EGFR), gene. In some embodiments, the present invention is directed at compositions and methods involving single nucleotide polymorphisms (SNPs) in the promoter of the EGFR gene that affect EGFR expression. The identification of polymorphisms associated with EGFR expression or activity enables novel methods and compositions for evaluating the potential efficacy and toxicity of an EGFR-targeting therapeutic agent, predicting a patient's clinical prognosis, and evaluating a patient's risk of developing a disease that is associated with EGFR dysregulation.

We identify markers capable of guiding the decision to incorporate epidermal growth factor receptor (EGFR) inhibitors, in particular EGFR tyrosine kinase inhibitors (TKIs), into chemotherapeutic regimens. Mitogen-inducible gene 6 (Mig6), a negative regulator of EGFR, is selectively upregulated during the development of resistance to the EGFR tyrosine kinase inhibitor (TKI) erlotinib, resulting in decreased EGFR phosphorylation. The ratio of Mig6 / EGFR expression highly correlates with erlotinib sensitivity. A low Mig6 / EGFR ratio correlates with a high response rate to gefitinib and a marked increase in progression-free survival for patients. The ratio of Mig6 to EGFR is a major predictor of biologic and clinical responses to EGFR inhibitors.

The invention belongs to the field of a medicinal preparation, and relates to an EGFR (epidermal growth factor receptor) modified platinum drug albumin nano preparation with a target tumor cell identification function. According to the invention, albumin is used for supporting platinum drugs, medical PEG (polyethylene glycol) is taken as a dispersing and cross-linking agent, and amination EGFR aptamer is taken as a target modifying molecule, so that the soluble albumin nano (Apt-PtNPs) preparation is prepared. The nanoparticle can be specifically combined with the EGFR on the surface of the tumor cell and has a cell endocytosis function, so that the toxic and side effects of the platinum drugs can be reduced, the purposes of toxicity reduction and efficacy enhancement are achieved, EGFR expression can be inhibited by prompting EGFR protein phosphorylation, and the anti-tumor effect of the nanoparticle in combination of the platinum drugs is achieved; the nanoparticle can be used for preparing the anti-tumor drugs, and particularly, the treatment research of the nanoparticle in the aspects of cervical cancer and ovarian cancer proves that the nanoparticle is good in targeting and good in killing effect and has good application prospect in gene therapy of tumors and combined treatment by chemotherapeutic drugs.

The inventors of the present invention have surprisingly discovered that EGFR expression in nonmetastatic breast cancer patients with CK-negative CTCs could induce EMT process. A simultaneous detection of both EGFR and EMT markers (VIM and Slug) in CTCs might improve prognostic or predictive information in patients with operable breast cancer.

The present invention relates to prognostic methods which are useful in medicine, particularly cancer chemotherapy. The object of the invention to provide a method for assessing HER2-neu and / or EGFR expression levels in fixed or fixed and paraffin embedded tissues and prognosticate the probable sensitivity of a patient's tumor to treatment with receptor tyrosine kinase targeted chemotherapy by examination of the amount of HER2-neu and / or EGFR mRNA in a patient's tumor cells and comparing it to a predetermined threshold expression level for those genes. More specifically, the invention provides to oligonucleotide primer pairs EGFR and HER2-neu and methods comprising their use for detecting levels of EGFR and HER2-neu mRNA, respectively.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a 4,6-pyrimidine diamine compound and a preparing method and an application thereof; the 4,6-pyrimidine diamine compound is an N4,N6-(2,5-dialkoxy phenyl)-pyrimidine diamine compound or an N4-(2,5-dialkoxy phenyl)-N6-(3-alkoxy phenyl)-pyrimidine diamine compound, and in particular, alkoxy can be C1-C4 alkane. The 4,6-pyrimidine diamine compound can be used for broad-spectrum inhibition of the activity of an EGFR kinase and resisting of EGFR expressed tumor cell activity. The EGFR kinase is a wild-type or drug-resistant mutant EGFR kinase, and provides a basis for new drug screening. And the synthesis method of the 4,6-pyrimidine diamine compound provided by the invention is simple in synthesis process and is in favor of industrialized production.

The invention discloses a method for detecting a peripheral blood circulating tumor cell EGFR of an advanced rectal cancer patient. CTC in peripheral blood of the advanced rectal cancer patient from whom a tissue specimen cannot be obtained is obtained through separation by means of a membrane filtration device, a thin slice is manufactured through the cell wax block technology, and accordingly the EGFR expression situation of the CTC in the peripheral blood of the advanced rectal cancer patient from whom the tissue specimen cannot be obtained is detected. By means of the technological method, the EGFR expression situation of the CTC in the peripheral blood of the advanced rectal cancer patient from whom the tissue specimen cannot be obtained can be detected without colorectal cancer tissue. The technology belongs to minimal invasion and can achieve real-time detection.

The invention discloses application of basic fuchsin in tumor resistance, and a drug, and relates to the technical field of tumor treatment. The invention discloses application of basic fuchsin in preparation of an antitumor drug. The tumor is a tumor with positive EGFR expression. It is found for the first time that basic fuchsin can significantly improve the life quality of patients with advanced lung adenocarcinoma and prolong the lifetime, meanwhile, proliferation of human lung adenocarcinoma cells can be inhibited, mRNA expression of PI3K, Akt and mTOR can be reduced, protein expression of p-PI3K, p-Akt and p-mTOR can be weakened, and it is prompted that the basic fuchsin can be used for treating tumors such as tumors with positive EGFR expression. The invention provides a new treatment method, a new strategy and a new thought for preventing and treating tumors with positive EGFR expression, especially tumors with drug resistance after being treated by an epidermal growth factor receptor tyrosine kinase inhibitor.

Mutants of recombinant immunoregulatory protein of Ganoderma lucidum (rLZ-8) and applications thereof are provided. It is found by the present invention that: an anti-EGFR (epidermal growth factor receptor) domain exists in a structure of the rLZ-8; particularly, the domain through positive potential characteristics thereof induces a killing effect to an abnormal EGFR-expressed tumor. Based on the above scientific discovery, with utilizing computational simulation technology, the mutants of the rLZ-8, having better antitumor effects, are obtained.

The invention belongs to the technical field of medicinal chemistry and nuclear pharmacy, and discloses an <18>F-labeled EGFR positron imaging agent as well as a preparation method and application thereof. The <18>F-labeled EGFR positron imaging agent has a structure as shown in a formula (II) which is described in the specification. The tracing effect is good, the specificity is relatively good, and high-expression or variant tumors of an epidermal factor receptor (EGFR) can be positively recognized. Meanwhile, the compound is good in in-vitro stability, is mainly metabolized through intestines, galls and kidneys, is quick to remove in vivo, is low in background uptake of background visceral organs and tissues such as muscles, bones, hearts, lungs and livers, and can be used for tumor PET imaging agents, EGFR expression level detection agents and EGFR inhibitor screening agents.

The invention relates to the technical field of medical biology and biological pharmacy, and in particular to an anti-EGFR nano antibody and an application thereof. The provided anti-EGFR nano-antibody is at least one selected from the follows: (1) CDR1 shown by GYTGCKNGMS, CDR2 shown by IDRDGSP and CDR3 shown by ATNPQRNIYGGSWCNY; and (2) a material with substitution of at least one conservative amino acid compared with (1). The provided anti-EGFR nano-antibody has a small molecular weight, strong specificity, and strong binding capacity with an EGFR active region CD3, and can be used for diagnosing and treating tumors with high EGFR expression.

The present invention relates to prognostic methods which are useful in medicine, particularly cancer chemotherapy. The object of the invention to provide a method for assessing HER2-neu and / or EGFR expression levels in fixed or fixed and paraffin embedded tissues and prognosticate the probable sensitivity of a patient s tumor to treatment with receptor tyrosine kinase targeted chemotherapy by examination of the amount of HER2-neu and / or EGFR mRNA in a patient s tumor cells and comparing it to a predetermined threshold expression level for those genes. More specifically, the invention provides to oligonucleotide primer pairs EGFR and HER2-neu and methods comprising their use for detecting levels of EGFR and HER2-neumRNA, respectively.

A nucleic acid is provided comprising an expression cassette which includes transcription control sequences of a member of a class of Pol III-transcribed genes in which no transcribed portion of the Pol III gene is required for transcription of the gene. In the expression cassette, the transcribed 5′ hairpin structure of the Pol III gene is deleted. The transcription control sequences are operably linked to a sequence of an EGFR gene in an antisense orientation suitable for decreasing expression of EGFR in the cell when transcribed. Lastly, a method for decreasing expression of EGFR in cells is provided that includes the step of contacting target cells either parenterally or directly into the tumor or tissue adjacent to the tumor cells with the nucleic acid of the present invention.

This invention relates to the use of short nucleic acid molecules that modulate Aurora-B kinase (AurkB) expression. The invention includes compounds, compositions and methods useful for the modulation of expression and activity of genes involved in the AurkB pathway. In one embodiment, the present invention provides short nucleic acid molecules, such as siRNA, which can be used in treating, preventing, or inhibiting cancer, and any other proliferative disease, trait or condition, which respond to a reduction in AurkB expression in a cell or tissue. Such short nucleic acid molecules can be used alone or in combination with other treatments or therapies, including short nucleic acid molecules that modulate expression of EGFR.

The invention relates to an antitumor traditional Chinese medicine composition and applications thereof, wherein the traditional Chinese medicine composition is prepared from the following bulk drugsby weight: 9-15 parts of Rhizoma Sparganii, 9-15 parts of Curcuma zedoaria, 15-20 parts of processed Pinellia ternata, 15-20 parts of processed Arisaema heterophyllum Blume, 15-30 parts of Milkvetch Root, and 15-30 parts of Atractylodes macrocephala. According to the present invention, the traditional Chinese medicine composition has effects of blood stasis removing, abdominal mass eliminating, phlegm removing, hard mass softening, body resistance supporting, spleen strengthening, qi benefiting and the like; the animal experiment results show that the traditional Chinese medicine composition can significantly inhibit the growth of MKN-45 gastric adenocarcinoma transplanted tumor in nude mice, down-regulate the PCNA expression and the EGFR expression in the gastric cancer tissue of nude mice, change the tumor microenvironment of walker-256 ascites model rats, and provide good treatment effects on tumors; and the traditional Chinese medicine composition has advantages of less variety ofbulk drugs, easy preparation, abundant and easily available raw materials and low cost.

The invention relates to a method for detecting EGFR (epidermal growth factor receptor) gene mutation of circulating tumor cells by digital PCR (polymerase chain reaction) and application thereof, belonging to the technical field of biomedicine. The method comprises the following steps: (1) enriching circulating tumor cells; (2) extracting the circulating tumor cells to obtain a DNA sample; (3) preparing a PCR reaction system; (4) preparing the PCR reaction system into liquid drops with uniform sizes by adopting a liquid drop generation instrument; (5) carrying out PCR (Polymerase Chain Reaction) amplification on the liquid drops; and (6) carrying out fluorescence signal detection on the amplified liquid drops. According to the detection method provided by the invention, the EGFR expression condition of a patient with advanced or recurrent non-small cell lung cancer can be detected without acquiring a tissue specimen through needle biopsy, the technology is non-invasive and can be used for multiple times of real-time detection, and the feasibility of circulating tumor cells in clinical application is improved. The method has the characteristics of high sensitivity, high accuracy, low cost and the like, and is convenient to operate.

An EGFR immunohistochemical detection kit based on Fe<3>O4 nanoprobes and a using method thereof are disclosed. The kit includes a citric acid restoring powder agent, an endogenous peroxidase blocker, a non-specific binding site blocker, a DAB concentrate liquid, a DAB chromogenic substrate, a DAB diluting liquid, the Fe<3>O4 nanoprobes, a TBS powder agent and a hematoxylin dyeing liquor. A novel method of bonding nanometer particles and an antibody is provided to skillfully combine high peroxidase-like activity of the Fe<3>O4 nanometer particles and biological characteristics of an EGFR single-domain antibody, and a high amount of the EGFR single-domain antibody is loaded on the surfaces of the prepared Fe<3>O4 nanoprobes. The Fe<3>O4 nanoprobes are formed by the Fe<3>O4 nanometer particles surfaces of which are loaded with metal ions and the EGFR single-domain antibody the C end of which is provided with His-Tags, and has advantages of a small size, good stability, high specificity, high sensitivity and high catalytic activity. The EGFR expression level of a tumor pathological tissue can be rapidly and conveniently detected through the kit, thus providing bases for tumor treatment.

The invention provides a compound, which is obtained by splicing a heptamethine cyanine structure and an epidermal growth factor receptor(EGFR) targeted drug molecular structure. The compound providedby the invention can be used as a hypoxia and EGFR double-targeted near infrared fluorescence probe, can realize the purpose of accurate imaging on malignant tumor lesions with high EGFR expression by targeting the tumor marker EGFR and the hypoxia state of tumor cells; in addition, the compound provided by the invention can be used as a photosensitizer for cancer treatment.

The invention relates to an SPIO-shRNA (superparamagnetic iron oxide-short hair ribonucleic acid) molecular probe with dual actions of MR (magnetic resonance) gene imaging and targeting therapy. The SPIO-shRNA comprises an SPIO nanoparticle and a pGenesil1-shRNA plasmid, wherein the sequence of the plasmid is AGTGTGTAACGGAATAGGT. The molecular probe can be used for MR (magnetic resonance) scanning gene imaging and detecting the specificity and targeting property on one hand, and for observing that the probe inhibits the EGFR (epidermal growth factor receptor) expression in cells, inducing cell apoptosis, regulating and controlling cell cycle redistribution and the like on the other hand, thus realizing targeting gene therapy.