32 results about "AKT1" patented technology

Provided are methods for the rapid detection of ovarian cancer. The methods employ a multiplex immunoassay to detect levels of two or more of the markers EGF, G-CSF, IL-6, IL-8, CA-125, VEGF, MCP-1, anti-IL6, anti-IL8, anti CA-125, anti-c-myc, anti-p53, anti-CEA, anti-CA 15-3, anti-MUC-1, anti-survivin, anti-bHCG, anti-osteopontin, anti-PDGF, anti-Her2 / neu, anti-Akt1, anti-cytokeratin 19, cytokeratin 19, EGFR, CEA, kallikrein-8, M-CSF, FasL, ErbB2 and Her2 / neu in a sample of the patient's blood, where the presence of abnormal levels of two or more of the markers indicates the presence of ovarian cancer in the patient. An array also is provided to quantitate levels of these markers in a patient's blood. Also provided is a method of predicting onset of clinical ovarian cancer comprising determining the change in concentration over time of two or more of anti-Her2 / neu, anti-MUC-1, anti-c-myc, anti-p53, anti-CA-125, anti-CEA, anti-CA 72-4, anti-PDGFRα, IFNγ, IL-6, IL-10, TNFα, MIP-1α, MIP-1β, EGFR and Her2 / neu in a patient's blood.

The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to prevent and treat cancer and other conditions.

The invention discloses a glioma detection panel based on next-generation sequencing, a detection kit and their application, wherein the glioma detection panel comprises glioma-related genes and loci;the glioma-related genes and loci include SNP (single-nucleotide polymorphism) locus on No. 1 chromosome, SNP locus on No. 19 chromosome, MGMT, ATRX, H3F3A, ACVR1, CTC, HIST1H3B, MLH1, PLCG1, SMO, AKT1, CTNNB1, HIST1H3C, MSH2, PMS2, TERT, ATRX, DAXX, HRAS, MSH6, PPM1D, TP53, BCOR, DDX3X, IDH1, MYC, PTCH1 and the like. The glioma detection panel herein is suitable for providing a patient with precise comprehensive diagnostic and treatment services just through next-generation sequencing.

The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site derived from the crystal structure of a ternary complex involving Akt1, a nonhydrolyzable ATP analogue, and a peptide substrate derived from a physiological AKT substrate such that the protein active site is defined including those residues within a defined distance from the nonhydrolyzable ATP analogue; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds from compounds high ranked by goodness of fit in docking by using one or more screening criteria; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1 in order to select compounds with Akt1 inhibitory activity. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to treat cancer and other conditions.

A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 μM concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.

The invention relates to the field of biochemical detection, in particular to a primer set, a kit, a library and an application for the multi-gene combined detection of gynecological tumors. The primer set for the multi-gene combined detection of gynecological tumors can be used for carrying out specific amplification of 14 oncogenes APC, AKT1, BRAF, CTNNB1, EGFR, FBXW7, KRAS, NRAS, PIK3CA, PPP2R1A, PTEN, TP53, BRCA1 and BRCA2 in the same PCR reaction system. The invention also provides a kit comprising the above primer set, and the kit is based on multiplex PCR targeted capture technology, and can easily complete the enrichment of target sequences within 8 h and obtain the high-quality library which can be directly sequenced on the machine. Using the sequencing library constructed by thekit and combining with the second-generation sequencing technology, the mutations of 1% or lower can be detected, and the false positive rate is extremely low.

High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498-505) is extended to the screening of Ser / Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser / Thr kinase AKT1 is presented.

High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498–505) is extended to the screening of Ser / Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser / Thr kinase AKT1 is presented.