title: Oxime ether lipids containing hydroxylated head groups are more superior siRNA delivery agents than their nonhydroxylated counterparts.
abstract: OBJECTIVE
  To evaluate the structure-activity relationship of oxime ether lipids (OELs) containing modifications in the hydrophobic domains (chain length, degree of unsaturation) and hydrophilic head groups (polar domain hydroxyl groups) toward complex formation with siRNA molecules and siRNA delivery efficiency of resulting complexes to a human breast cancer cell line (MDA-MB-231).
  
  
  METHODS
  Ability of lipoplex formation between oxime ether lipids with nucleic acids were examined using biophysical techniques. The potential of OELs to deliver nucleic acids and silence green fluorescent protein (GFP) gene was analyzed using MDA-MB-231 and MDA-MB-231/GFP cells, respectively.
  
  
  CONCLUSIONS
  Introduction of hydroxyl groups to the polar domain of the OELs and unsaturation into the hydrophobic domain favor higher transfection and gene silencing in a cell culture system.
authors.affiliation: Gene Regulation & Chromosome Biology Lab, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
authors.forename: Kshitij
authors.initials: K
authors.lastname: Gupta
authors.affiliation: Department of Chemistry, University of Louisville, Louisville, KY 40292, USA.
authors.forename: Stephanie J
authors.initials: SJ
authors.lastname: Mattingly
authors.affiliation: Department of Chemistry, University of Louisville, Louisville, KY 40292, USA.
authors.forename: Ralph J
authors.initials: RJ
authors.lastname: Knipp
authors.affiliation: Gene Regulation & Chromosome Biology Lab, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.|Department of Chemistry, University of North Carolina at Charlotte, 9201 University City Boulevard, Charlotte, NC 28223, USA.
authors.forename: Kirill A
authors.initials: KA
authors.lastname: Afonin
authors.affiliation: Basic Research Lab, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.|Basic Science Program, Leidos Biomedical Research, Inc., National Cancer Institute, Center for Cancer Research, Frederick National Laboratory for Cancer Research, Frederick, MD 21702-1201, USA.
authors.forename: Mathias
authors.initials: M
authors.lastname: Viard
authors.affiliation: Gene Regulation & Chromosome Biology Lab, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
authors.forename: Joseph T
authors.initials: JT
authors.lastname: Bergman
authors.affiliation: Gene Regulation & Chromosome Biology Lab, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
authors.forename: Marissa
authors.initials: M
authors.lastname: Stepler
authors.affiliation: Department of Chemistry, University of Louisville, Louisville, KY 40292, USA.
authors.forename: Michael H
authors.initials: MH
authors.lastname: Nantz
authors.affiliation: Gene Regulation & Chromosome Biology Lab, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
authors.forename: Anu
authors.initials: A
authors.lastname: Puri
authors.affiliation: Gene Regulation & Chromosome Biology Lab, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
authors.forename: Bruce A
authors.initials: BA
authors.lastname: Shapiro
mesh_terms: D001943:Breast Neoplasms / Q000235:genetics; D045744:Cell Line, Tumor; D004987:Ethers / Q000737:chemistry; D005260:Female; D049452:Green Fluorescent Proteins / Q000235:genetics; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes / Q000737:chemistry*; D010091:Oximes / Q000737:chemistry*; D034622:RNA Interference; D034741:RNA, Small Interfering / Q000008:administration & dosage* / Q000235:genetics; D014162:Transfection / Q000379:methods
chemical_list: D004987:Ethers; D008055:Lipids; D008081:Liposomes; D010091:Oximes; D034741:RNA, Small Interfering; D049452:Green Fluorescent Proteins
keywords: RNA interference; breast cancer cells; lipoplexes; nonsymmetric hydrophobic domain; oxime ether lipids; structure–activity relationship