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IP Update: Recent RNAi- and microRNA-Related Patents and Patent Applications: Oct 6, 2011

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Title: Carrier Compositions for Nucleic Acid Transport

Patent Number: 8,030,075

Filed: Oct. 17, 2006

Lead Inventor: Hidekazu Toyobuku, Otsuka Pharmaceutical

The invention, the patent's abstract states, comprises a “nucleic acid delivery carrier composition of low toxicity and high safety. … When used to administer a nucleic acid such as an siRNA into an animal-derived cell or organism, [the carrier can deliver] efficiently the nucleic acids into the cell while protecting it from being degraded.

“The carrier composition ... is prepared by mixing a cationic lipid having a steroid skeleton with a tertiary ammonium salt-type cationic lipid,” it adds. “The nucleic acid delivery composition is prepared by mixing the nucleic acid delivery carrier with a nucleic acid.”


Title: Treatment of Eye Disorders Characterized by an Elevated Intraocular Pressure by siRNAs

Patent Number: 8,030,284

Filed: Aug. 23, 2005

Lead Inventor: Ana Jimenez, Sylentis

The invention, the patent's abstract states, comprises “sequences and protocols for treatment of eye conditions by use of RNA interference. … Target genes are selected from those responsible for aqueous flow or aqueous outflow, while particularly preferred conditions to be treated include glaucoma and uveitis.”


Title: Cell Type-Specific Aptamer-siRNA Delivery System for HIV-1 Therapy

Patent Number: 8,030,290

Filed: Dec. 5, 2008

Lead Inventor: John Rossi, City of Hope

The invention relates to “compositions and methods for delivery of siRNA to specific cells or tissue,” according to the patent's abstract. “More particularly, the ... invention relates to compositions and methods for cell type-specific delivery of anti-HIV siRNAs via fusion to an anti-gp120 aptamer.”


Title: Method to Trigger RNA Interference

Patent Number: 8,030,473

Filed: Jan. 6, 2006

Lead Inventor: James Carrington, Oregon State University

The invention comprises “a method to generate siRNAs in vivo … [as well as] constructs and compositions useful in the method,” the patent's abstract states. “The method does not depend on the use of DNA or synthetic constructs that contain inverted duplications or dual promoters so as to form perfect or largely double-stranded RNA. Rather, the method depends on constructs that yield single-stranded RNA transcripts, and exploits endogenous or in vivo-produced miRNAs or siRNAs to initiate production of siRNAs. The miRNAs or siRNAs guide cleavage of the transcript and set the register for production of siRNAs encoded adjacent to the initiation cleavage site within the construct. The method results in specific formation of siRNAs of predictable size and register relative to the initiation cleavage site. The method can be used to produce specific siRNAs in vivo for inactivation or suppression of one or more target genes or other entities, such as pathogens.”


Title: siRNA Targeting Cyclin-Dependent Kinase 4

Patent Number: 8,030,474

Filed: April 8, 2009

Lead Inventor: Anastasia Khvorova, Dharmacon (Thermo Fisher Scientific)

“Efficient sequence-specific gene silencing for cyclin-dependent kinase 4 is possible through the use of siRNA technology,” the patent's abstract states. “By selecting particular siRNAs by rational design, one can maximize the generation of an effective gene-silencing reagent, as well as methods for silencing genes. Methods, compositions, and kits generated through rational design of siRNAs are disclosed.”


Title: siRNA Targeting Gremlin

Patent Number: 8,030,476

Filed: April 7, 2010

Lead Inventor: Anastasia Khvorova, Dharmacon (Thermo Fisher Scientific)

“Efficient sequence-specific gene silencing is possible through the use of siRNA technology,” the patent's abstract states. “By selecting particular siRNAs by rational design, one can maximize the generation of an effective gene silencing reagent, as well as methods for silencing genes. Methods, compositions, and kits generated through rational design of siRNAs are disclosed including those directed to CKSF1B1.”


Title: Multicistronic siRNA Constructs to Inhibit Tumors

Application Number: 20110236956

Filed: Jan. 26, 2011

Lead Inventor: Jasti Rao, University of Illinois

The patent describes “multicistronic short interfering RNA constructs targeting, in various combinations, a human urokinase-type plasminogen activator receptor, human urokinase-type plasminogen activator, human matrix metalloprotease 9, and cathepsin B inhibit tumors.”


Title: Nucleic Acid Compounds for Inhibiting BIRC5 Gene Expression and Uses Thereof

Application Number: 20110236972

Filed: Aug. 5, 2009

Lead Inventor: Steven Quay, Marina Biotech

The invention comprises “RNA molecules, for example, meroduplex ribonucleic acid molecules, capable of decreasing or silencing BIRC5 gene expression,” the patent application's abstract states. “An mdRNA of this disclosure comprises at least three strands that combine to form at least two non-overlapping double-stranded regions separated by a nick or gap wherein one strand is complementary to a BIRC5 mRNA. Also provided are methods of decreasing expression of a BIRC5 gene in a cell or in a subject to treat a BIRC5-related disease.”


Title: Lipophilic Nucleic Acid Delivery Vehicle and Methods of Use Thereof

Application Number: 20110237435

Filed: June 26, 2005

Inventor: Robert Rya, Children's Hospital & Research Center at Oakland

The patent application, its abstract states, claims “compositions and methods for delivery of nucleic acids to individuals and to cells, including nucleic acid delivery particles that comprising a lipid-binding polypeptide, a lipid bilayer comprising one or more cationic lipids, and a nucleic acid.”


Title: Identification of a Novel Repressor on IFN-Lambda Promoter and siRNA ZEB1 and BLIMP-1 to Increase IFN-Lambda Gene Activity

Application Number: 20110237643

Filed: May 5, 2010

Lead Inventor: Grant Gallagher, Medical Diagnostics Laboratories

The invention, the patent application's abstract states, “is directed to the identification of a novel repressor located between about 1.2 kb to about 1.6 kb from the translation start site of the IFN-lamda1 promoter. The ... invention provides a method of using siRNAs against ZEB1 and BLIMP-1, and increases the promoter activity of IFN-lamda 1.”

The siRNAs against ZEB1 mRNA or BLIMP-1 mRNA increase IFN-lamda 1 gene activity, it adds. “There is provided a therapeutic application of siRNAs against ZEB1 and BLIMP-1 mRNAs in treating a mammal by increasing the production of IFN-lamda1 protein that promotes an antiviral response as well as treats asthma diseases.”


Title: Use of RNAi Technology to Inhibit ASIC3

Application Number: 20110237645

Filed: Jan. 31, 2011

Lead Inventor: Kathleen Sluka, University of Iowa

In vitro studies using cells transfected with acid-sensing ion channel 3 or acid-sensing ion channel 1 cDNA demonstrated that the miRNAs against mouse ASIC3 selectively inhibit mouse ASIC3, but not ASIC1 as detected by protein expression and responses to pH,” according to the patent application's abstract. “When the [miRNAs] were used in vivo, delivered into the muscle of mice using a replication-defective herpes simplex viral vector, primary and secondary hyperalgesia were reduced after carrageenan-induced muscle inflammation. Accordingly, the ... invention provides RNAi agents that target ASIC3, methods of preparing such RNAi agents, and methods of using them to modulate in a cell the level of ASIC3 or activity of an ASIC including at least one ASIC3. Modulation of ASIC3 activity or levels can be used for different purposes such as treating pain associated with the expression of ASIC3 and the like.”


Title: Inhibitory RNA for Modulating the Molecular Function of ZFAT Gene

Application Number: 20110237647

Filed: Sept. 8, 2008

Lead Inventor: Senji Shirasawa, Fukuoka University

“The inhibitory RNA for inhibiting the expression of ZFAT gene according to this invention is a siRNA comprising a sense RNA having a base sequence of contiguous 20 to 20 bases, preferably 23 to 27 bases, of ZFAT mRNA and an antisense RNA having a base sequence complementary to the base sequence of the sense RNA or a shRNA,” the patent application's abstract states. “The inhibitory RNA for inhibiting the expression of ZFAT gene according to this invention decreases a rate of cell proliferation of cancer cells, etc., induces apoptosis of cells including cancer cells, or inhibits an immunoresponse by inhibiting the expression of the ZFAT gene. Therefore, the inhibitory RNA of this invention is useful for development of molecular target agents particularly for cancer cells or immunosuppressive agents.”


Title: RNA Interference in Skin Indications

Application Number: 20110237648

Filed: Sept. 22, 2009

Lead Inventor: Anastasia Khvorova, RXi Pharmaceuticals

The invention relates to “RNAi constructs with improved tissue and cellular uptake characteristics and methods of use of these compounds in dermal applications,” according to the patent application's abstract.

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