39 results about "RHOA Protein" patented technology

Conjugated nitro alkene compounds hamper or prevent proliferation of cancer cells in cell culture and in cancer patients, which can result in a decrease in tumor size and / or disappearance of the cancer. The compounds may act by interference with cancer cell biochemistry, in which isoprenoid groups such as farnesyl and geranylgeranyl become bonded to various oncogenic proteins such as Ras, RhoA, RhoB, or some other growth-related cellular protein(s).

The invention provides the construction for a farnesyl pyrophosphoric acid synthetase RNA (Ribonucleic Acid) interference recombinant lentivirus vector, which comprises the following steps of: sieving the most effective target sequence of an FDS (farnesyl diphosphate synthase) gene RNAi (RNA interference) in a tool cell 293T cell, synthesizing the double-stranded DNA of the most effective target sequence, connecting to a pGCSIL-GFP vector and successfully constructing the recombinant vector through enzyme cutting, sequencing and identification. Researches indicate that the constructed RNA interference vector LV-sh-FDS can downwards modulate the expression of an FDS mRNA (Messenger RNA) level in a neonatal rat cardiac myocyte, simultaneously can downwards modulate the expression of myocardial hypertrophy markers such as cell areas and marker genes beta-MHC (Myosin Heavy Chain) and BNP (Brain Natriuretic Peptide), additionally can effectively inhabit the activity of RhoA while downwards modulating the FDS, can be applied in preparing medicaments for treating myocardial hypertrophy diseases and also can be applied in preparing medicaments for cholesterol metabolic control.

The present invention relates to the use of short interfering nucleic acid molecules (siNA, such as siRNA) that modulate the expression of VEGF-C and / or RhoA involved in neovascular angiogenesis. In the present invention, inhibition of VEGF-C and / or RhoA gene expression results in decreased expression of VEGF-A, which is required for the initiation and persistence of angiogenesis. Furthermore, the present invention also relates to the inhibition of RhoA expression levels and VEGF-C expression levels to gain the benefit of downregulating two different targets required for angiogenesis. The present invention describes compounds, compositions and methods for the inhibition of neovascularization. In certain embodiments, the present invention relates to methods for inhibiting neovascularization, and compounds for treating ocular diseases such as age-related macular degeneration (AMD), diabetic retinopathy, glaucoma, and other neovascular diseases , such as VEGF-C siRNA and RhoAsiRNA.

The invention discloses a method for inducing hepatic oval cells to differentiate towards bile duct cells and a special culture medium used in the method. The culture medium is added with 1 to 6 percent of fetal calf serum, 1 to 3 percent of B27 and 0.05 to 0.15 percent of penicillin-streptomycin on the basis of an RPMI1640 culture medium. The method for inducing the differentiation comprises the following steps: 1) leading RhoA mutant genes into the oval cells WB-F344 to obtain WB-F344 cells of a high-expression RhoA gene activity mutant; and 2) inoculating the WB-F344 cells of the high-expression RhoA gene activity mutant into the special culture medium where the hepatic oval cells are induced in vitro to differentiate into the bile duct cells, and culturing the WB-F344 cells at a temperature of 37 DEG C with 5 percent of CO2 to obtain the bile duct cells. The method provides a new approach to obtain the bile duct cells and has wide application prospect.

Inhibitors of RhoA kinase production and / or activation are suited for relaxing the features and / or for decontracting the skin and thus are useful for preventing and / or combating the signs of aging of the skin, in particular wrinkles and notably expression wrinkles.

The invention provides a polyethylene composition and a thin film prepared from the same. The polyethylene composition comprises a component A, a component B, a component C, a nucleating agent and petroleum resin. The component A refers to ethylene / alpha-olefin copolymerized linear low-density polyethylene, and at a temperature of 190 DEG C and with a load of 2.16kg, a melt index MFRA (mass flow rate A) of the linear low-density polyethylene is 0.01-2g / 10min, and a density RhoA is 0.880-0.936g / cm<3>. The component B refers to ethylene / alpha-olefin copolymerized linear low-density polyethylene, and at a temperature of 190 DEG C and with a load of 2.16kg, a melt index MFRB (mass flow rate B) of the linear low-density polyethylene is 2.1-9.9g / 10min, and a density RhoB is 0.910-0.930g / cm<3>. The component C refers to ethylene / alpha-olefin copolymerized linear low-density polyethylene, and at a temperature of 190 DEG C and with a load of 2.16kg, a melt index MFRC (mass flow rate C) of the linear low-density polyethylene is 10-80g / 10min, and a density RhoC is 0.880-0.930g / cm<3>. When the polyethylene composition is applied to prepare a polyethylene thin film by a flat film stretching method, the polyethylene composition is excellent in film-forming property, and the prepared thin film is high in modulus.

Disclosed are compositions and methods for slowing, preventing, or reversing platelet damage, particularly as may occur during blood banking or during refrigeration of platelets. The composition may include one or more of a RAC inhibitor, a CDC42 inhibitor, a RHOA inhibitor, or a combination thereof. The compositions may further include a pharmaceutically acceptable carrier.

This invention provides a stent for implantation in a blood vessel or other tissue, wherein the stent is coated with or contains C3 exoenzyme, a chimeric version thereof or an inhibitor of RhoA. This invention also provides a method for treating or inhibiting the onset of restenosis in a subject which comprises implanting one of the instant stents in the subject's blood vessel.

The invention mainly relates to an N,N-double substituted benzoazacyclo-2-amide compound and an application thereof. The N,N-double substituted benzoazacyclo-2-amide compound is a compound shown as formula I or a salt formed by a medical acid or alkali. The compound provided by the invention has strong inhibition activity on RhoA protease which is tightly related with cardiovascular and cerebrovascular diseases. The compound provided by the invention is hopeful to be developed into a RhoA protease small-molecule inhibitor type cardiovascular and cerebrovascular disease treatment medicine.

Cells within liver tumour mass comprise a unique set of proteins / tumour antigens when compared to the normal liver tissues epithelial cells juxtaposed to the tumour. The presence of tumour antigens couples the production of auto-antibodies against these tumour antigens. The present invention relates to the identification and elucidation of a protein set that can act as a novel marker set for liver cancer diagnosis and prognosis. Specifically, it relates to a kit that enables diagnostic and prognostic measurement of auto-antibodies in serum of liver cancer patients. The present invention provides a non-invasive, specific, sensitive, and cost effective detection and quantification method by evaluating a set of validated liver cancer proteins / tumour antigens, which includes Bmi-1, VCC1, SUMO-4, RhoA, TXN, ET-1, UBE2C, HDGF2, FGF21, LECT2, SOD1, STMN4, Midkine, IL-17A or IL26, to complement the conventional diagnostic methods.

Isolated peptides, peptidomimetics, and antibodies which bind to the viral fusion protein binding domain of the RhoA protein or the RhoA binding domain of a viral fusion protein are useful for inhibiting infection in susceptible cells, in vitro and in vivo. Among these viruses are the Paramyxovirus respiratory syncytial virus (RSV) and the Lentivirus human immunodeficiency virus (HIV).

The present disclosure relates to methods, compositions, and kits for the inhibition of signaling by members of the Rho GTPase family. Specifically, the disclosure relates to methods, compositions and kits for the inhibition of RhoA and / or RhoC transcriptional signaling and action of the transcription co-factors MRTF-A and / or MRTF-B. The disclosure finds use in treatment of Rho-mediated disease states (e.g., tumor metastasis and fibrosis), Rho-mediated biological conditions, and in cell signaling research.

The present invention discloses a drug for treating glaucoma. According to the drug, a RNA interference sequence RhoA siRNA is adopted as an active ingredient, wherein a sense strand of the RhoA siRNA is 5'GAAGUCAAGCAUUUCUGUCdTdT3', an antisense strand is 3'dTdTCUUCAGUUCGUAAAGACAG5'. With the RhoA siRNA prepared according to a RNA interference target sequence 5'-GAAGTCAAGCATTTCTGTC-3' of the RhoA in the present invention, an expression level of RhoA mRNA can be effectively reduced, an expression level of RhoA protein in anterior chamber tissue can be efficiently down-regulated, stress fiber formation is affected so as to affect changes of cytoskeleton structures and distributions of actin of trabecular meshwork cells, such that trabecular meshwork cell channel configuration is changed, aqueous humor discharge resistance is changed, and intraocular pressure is affected so as to achieve a purpose of treatment of glaucoma.

Research finds that exocrine protein SCGB3A2 in lung tracheal bronchus is combined with a receptor PDPN on the cell surface and activates RhoA protein, so that the strength of pneumonia and the expression quantity of inflammatory factors are enhanced, and lung inflammation can be relieved and expression of inflammatory factors and infiltration of lung inflammatory cells can be reduced by blocking combination of SCGB3A2 and PDPN through an antibody. Therefore, the invention provides a brand new target for controlling lung inflammatory factor storm caused by bacteria or viruses. The target spot has a relatively clear signal transmission path, so that the side effect of the medicine for inhibiting the inflammatory factor storm, which is prepared aiming at the target spot, is smaller than that of glucocorticoid.

The invention provides a polyethylene composition and an antistatic film. The polyethylene composition contains a conductive filling material, a component A, a component B and a component C; the component A is ethane / alpha alkene copolymerized linear low density polyethylene, the fusion index MIA is 0.01-2 g / 10 min under temperature of 190 DEG C and loading of 2.16 kg, density RhoA is 0.880-0.936 g / cm<3>; the component B is ethane / alpha alkene copolymerized linear low density polyethylene, the fusion index MIB is 2.1-14.9 g / 10 min under temperature of 190 DEG C and loading of 2.16 kg, density RhoB is 0.910-0.930 g / cm<3>; the component C is ethane / alpha alkene copolymerized linear low density polyethylene, the fusion index MIC is 15-150 g / 10 min under temperature of 190 DEG C and loading of 2.16 kg, and density RhoC is 0.880-0.930 g / cm<3>. The polyethylene composition employs a flat membrane stretching method for preparing a polyethylene film, the stretching ratio is large, film forming rate is high, and the obtained film has good antistatic property.

Disclosed are compositions and methods for slowing, preventing, or reversing platelet damage, particularly as may occur during blood banking or during refrigeration of platelets. The composition may include one or more of a RAC inhibitor, a CDC42 inhibitor, a RHOA inhibitor, or a combination thereof. The compositions may further include a pharmaceutically acceptable carrier.

The present invention relates to the identification of the cytosolic phosphoprotein CRMP4b as a protein that physically and functionally interacts with RhoA to mediate neurite outgrowth inhibition. siRNA-mediated knockdown of CRMP4 promotes neurite outgrowth on myelin substrates indicating a critical role for CRMP4 in neurite outgrowth inhibition. Disruption of CRMP4b-RhoA binding with a competitive inhibitor attenuates neurite outgrowth inhibition on myelin and aggrecan substrates. Stimulation of neuronal growth cones with Nogo leads to co-localization of CRMP4b and RhoA at discrete regions within the actin-rich central and peripheral domains of the growth cone indicative of a potential function in cytoskeletal rearrangements during neurite outgrowth inhibition. Together these data indicate that a RhoA-CRMP4b complex forms in response to inhibitory challenges in the growth cone environment and regulate cytoskeletal dynamics at distinct sites necessary for axon outgrowth inhibition. Competitive inhibition of CRMP4b-RhoA binding suggests a novel, highly specific therapeutic avenue for promoting regeneration following CNS injury.

Cells within liver tumour mass comprise a unique set of proteins / tumour antigens when compared to the normal liver tissues epithelial cells juxtaposed to the tumour. The presence of tumour antigens couples the production of auto-antibodies against these tumour antigens. The present invention relates to the identification and elucidation of a protein set that can act as a novel marker set for liver cancer diagnosis and prognosis. Specifically, it relates to a kit that enables diagnostic and prognostic measurement of auto-antibodies in serum of liver cancer patients. The present invention provides a non-invasive, specific, sensitive, and cost effective detection and quantification method by evaluating a set of validated liver cancer proteins / tumour antigens, which includes Bmi-1, VCC1, SUMO-4, RhoA, TXN, ET-1, UBE2C, HDGF2, FGF21, LECT2, SOD1, STMN4, Midkine, IL-17A or IL26, to complement the conventional diagnostic methods.

The invention belongs to the field of biological pharmacy, relates to application of recombinant ADAMTS13 to preparation of cerebral hemorrhage medicaments, and especially relates to application of recombinant ADAMTS13 to preparation for medicaments for reducing cerebral hemorrhage caused by tPA thrombolytic therapy on cerebral ischemia. Experiment results show that: VEGF generated by tPA induction at ischemic condition can be blocked by a specific inhibitor of RhoA or Akt, and recombinant ADAMTS13 substantially reduces activation of RhoA and phosphorylation of Akt, which means that recombinant ADAMTS1 is capable of inhibiting tPA-induced VEGF expression through RhoA and Akt pathways. The recombinant ADAMTS13 provided by the invention helps to mitigate damage of tPA to blood cerebral barrier and further to reduce cerebral hemorrhage caused thereby by inhibiting cerebrovascular permeability increase mediated by RhoA and Akt, and therefore combination usage of recombinant ADAMTS13 and tPA is a novel countermeasure and means for increasing thrombolysis security.

The invention provides a polyethylene composition and a flame retardant film. The polyethylene composition contains a component A, a component B, a component C and a flame retardant; the component A is ethylene / alpha-olefin copolymerized linear low density polyethylene, the melt index MIA at a temperature of 190 DEG C and under a load of 2.16 kg is (0.01-3.5)g / 10min, and the density rhoA is 0.880-0.936 g / cm3; the component B is ethylene / alpha-olefin copolymerized linear low density polyethylene, the melt index MIB at a temperature of 190 DEG C and under a load of 2.16 kg is (3.6-9.9)g / 10min, and the density rhoB is 0.910-0.930 g / cm3; and the component C is ethylene / alpha-olefin copolymerized linear low density polyethylene, the melt index MIC at a temperature of 190 DEG C and under a load of 2.16 kg is (10-80)g / 10min, and the density rhoC is 0.880-0.930 g / cm3. The polyethylene composition has the advantages of large stretch rate, high film formation rate and very good film formation ability when the polyethylene composition undergoes a flat film stretching technology to produce a polyethylene film, and the obtained polyethylene film has excellent flame retardation performance.

Cells are genetically modified to express a luminophore, e.g., a modified (F64L, S65T, Y66H) Green Fluorescent Protein (GFP, EGFP) coupled to a component of an intracellular signalling pathway such as a transcription factor, a cGMP- or cAMP-dependent protein kinase, a cyclin-, calmodulin- or phospholipid-dependent or mitogen-activated serine / threonin protein kinase, a tyrosine protein kinase, or a protein phosphatase (e.g. PKA, PKC, Erk, Smad, VASP, actin, p38, Jnk1, PKG, IkappaB, CDK2, Grk5, Zap70, p85, protein-tyrosine phosphatase 1C, Stat5, NFAT, NFkappaB, RhoA, PKB). An influence modulates the intracellular signalling pathway in such a way that the luminophore is being redistributed or translocated with the component in living cells in a manner experimentally determined to be correlated to the degree of the influence. Measurement of redistribution is performed by recording of light intensity, fluorescence lifetime, polarization, wavelength shift, resonance energy transfer, or other properties by an apparatus consisting of e.g. a fluorescence microscope and a CCD camera. Data stored as digital images are processed to numbers representing the degree of redistribution. The method can be used as a screening program for identifying a compound that modulates a component and is capable of treating a disease related to the function of the component.

The invention mainly relates to an N,N-double substituted benzoazacyclo-2-amide compound and an application thereof. The N,N-double substituted benzoazacyclo-2-amide compound is a compound shown as formula I or a salt formed by a medical acid or alkali. The compound provided by the invention has strong inhibition activity on RhoA protease which is tightly related with cardiovascular and cerebrovascular diseases. The compound provided by the invention is hopeful to be developed into a RhoA protease small-molecule inhibitor type cardiovascular and cerebrovascular disease treatment medicine.

The invention provides an evaluation gene group for prognosis prediction of gastric cancer and a corresponding kit. The evaluation gene group is obtained by screening genes comprised in a RhoA proteinactivity regulation pathway for regulating RhoA protein activity, wherein, the evaluation gene group comprises the following genes: RHOA, ARHGAP32, ARHGAP4, ARHGAP6, ARHGAP9, ARHGEF17, ARHGEF2, ARHGEF3, BCR, CDC42, CDKN1B, DLEC1, FARP1, NET1, NGEF, OBSCN, PRPF38B, SLC6A5, TSPAN1, VAV2, and VAV3.

The invention provides an evaluation gene group for prognosis prediction of gastric cancer and a corresponding kit. The evaluation gene group is obtained by screening genes comprised in a RhoA proteinactivity regulation pathway for regulating RhoA protein activity, wherein, the evaluation gene group comprises the following genes: RHOA, ARHGAP32, ARHGAP4, ARHGAP6, ARHGAP9, ARHGEF17, ARHGEF2, ARHGEF3, BCR, CDC42, CDKN1B, DLEC1, FARP1, NET1, NGEF, OBSCN, PRPF38B, SLC6A5, TSPAN1, VAV2, and VAV3.

Nitration shielding peptides that reduce or prevent nitration of a protein of interest are disclosed. The peptide can serve as molecular sink for nitrating agents, block access of the nitrating agents to the target tyrosine on the protein of interest, serve as substrate for the nitrating agent (i.e., provide an alternative nitratable tyrosine residue), provide a nitrating agent neutralizing moiety such as antioxidant, or a combination thereof. The nitration shielding peptide can be a fusion protein that includes one or more additional domains such a protein transduction domain, a targeting signal, a purification tag, or any combination thereof. Exemplary nitration shielding peptides for reducing nitration of RhoA and PKG-1α, and methods of use thereof for treating pathologies, disease, and disorders associated with nitration of RhoA and PKG-1α, respectively are also provided.

The invention discloses an application of RhoA recombinant protein in preparation of a culture solution for improving embryo freezing resistance and recovery rate after thawing. The research finds that by addition of in vitro recombined RhoA protein to a culture solution of normally hatched embryos of mice, compared with a control group, the thawing recovery rate of normally hatched embryos can be significantly increased. The RhoA recombinant protein is applied to the field of embryo freezing for the first time, through addition of the RhoA recombinant protein, the freezing resistance and the recovery rate after thawing of the embryos are significantly increased, and use of a toxic cryoprotectant is reduced to a certain extent, so that the adverse effects on the embryos are reduced, and the RhoA recombinant protein has a wide application prospect in the technical field of cryopreservation of the embryos.

The invention provides a polyethylene composition and an antistatic film. The polyethylene composition contains a conductive filling material, a component A, a component B and a component C; the component A is ethane / alpha alkene copolymerized linear low density polyethylene, the fusion index MIA is 0.01-2 g / 10 min under temperature of 190 DEG C and loading of 2.16 kg, density RhoA is 0.880-0.936 g / cm<3>; the component B is ethane / alpha alkene copolymerized linear low density polyethylene, the fusion index MIB is 2.1-14.9 g / 10 min under temperature of 190 DEG C and loading of 2.16 kg, density RhoB is 0.910-0.930 g / cm<3>; the component C is ethane / alpha alkene copolymerized linear low density polyethylene, the fusion index MIC is 15-150 g / 10 min under temperature of 190 DEG C and loading of 2.16 kg, and density RhoC is 0.880-0.930 g / cm<3>. The polyethylene composition employs a flat membrane stretching method for preparing a polyethylene film, the stretching ratio is large, film forming rate is high, and the obtained film has good antistatic property.