5′-(E)-Vinylphosphonate: A Stable Phosphate Mimic Can Improve the RNAi Activity of siRNA-GalNAc Conjugates

ChemBioChem

Volumn 17, Issue 11, 2016, Pages 985-989

  Parmar, Rubina ^a   Willoughby, Jennifer L S ^a   Liu, Jingxuan ^a   Foster, Donald J ^a   Brigham, Benjamin ^a   Theile, Christopher S ^a   Charisse, Klaus ^a   Akinc, Akin ^a   Guidry, Erin ^b   Pei, Yi ^b   Strapps, Walter ^b   Cancilla, Mark ^b   Stanton, Matthew G ^b   Rajeev, Kallanthottathil G ^a   Sepp Lorenzino, Laura ^a   Manoharan, Muthiah ^a   Meyers, Rachel ^a   Maier, Martin A ^a   Jadhav, Vasant ^a  

^a ALNYLAM PHARMACEUTICALS   (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Clp1 kinase; oligonucleotides; phosphate mimic; RISC loading; siRNA

Indexed keywords

5' VINYLPHOSPHONATE SMALL INTERFERING RNA N ACETYLGALACTOSAMINE CONJUGATE; ACID PHOSPHATASE; APOLIPOPROTEIN B; BLOOD CLOTTING FACTOR 9; LOW DENSITY LIPOPROTEIN; LYSOSOME ENZYME; N ACETYLGALACTOSAMINE; PHOSPHONIC ACID DERIVATIVE; SMALL INTERFERING RNA; UNCLASSIFIED DRUG; ARGONAUTE PROTEIN; HEXIM1 PROTEIN, MOUSE; RNA INDUCED SILENCING COMPLEX; TRANSCRIPTION FACTOR; VINYL DERIVATIVE; VINYLPHOSPHONIC ACID;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DEPHOSPHORYLATION; DRUG DOSE COMPARISON; DRUG POTENCY; ENZYME ACTIVITY; IC50; IN VITRO STUDY; IN VIVO STUDY; LIPOPROTEIN BLOOD LEVEL; LIVER CELL; LYSOSOME; METABOLIC STABILITY; MOUSE; NONHUMAN; PRIORITY JOURNAL; RAT; RNA CLEAVAGE; RNA INTERFERENCE; SINGLE DRUG DOSE; ANIMAL; ANTAGONISTS AND INHIBITORS; BLOOD; C57BL MOUSE; CELL CULTURE; CHEMISTRY; CYTOLOGY; DRUG EFFECTS; GENETICS; HUMAN; METABOLISM;

ACETYLGALACTOSAMINE; ANIMALS; APOLIPOPROTEINS B; ARGONAUTE PROTEINS; CELLS, CULTURED; FACTOR IX; HEPATOCYTES; HUMANS; LIPOPROTEINS, LDL; MICE; MICE, INBRED C57BL; ORGANOPHOSPHONATES; RNA INTERFERENCE; RNA, SMALL INTERFERING; RNA-INDUCED SILENCING COMPLEX; TRANSCRIPTION FACTORS; VINYL COMPOUNDS;

EID: 84964582919     PISSN: 14394227     EISSN: 14397633     Source Type: Journal    
DOI: 10.1002/cbic.201600130     Document Type: Article

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