The effect of various chemical modifications of nitrogen atoms on the efficiency of polyethylenimines (PEIs) as synthetic vectors for the delivery of plasmid DNA into monkey kidney cells in vitro has been systematically investigated. The resultant structure-activity relationship has both provided mechanistic insights and led to PEI derivatives with markedly enhanced performance. For example, N-acylation of PEI with the molecular mass of 25 kDa (PE125, one of the most potent polycationic gene delivery vectors) with alanine nearly doubles its transfection efficiency in the presence of serum and also lowers its toxicity. Furthermore, dodecylation of primary amino groups of 2-kDa PEI yields a nontoxic polycation whose transfection efficiency in the presence of serum is 400 times higher than the parent's and which exceeds 5-fold even that of PE125.
机构:
Univ Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USAUniv Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USA
Ahn, CH
;
Chae, SY
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Univ Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USAUniv Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USA
Chae, SY
;
Bae, YH
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机构:
Univ Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USAUniv Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USA
Bae, YH
;
Kim, SW
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h-index: 0
机构:
Univ Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USAUniv Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USA
机构:
OCHSNER MED FDN, DIV RES, MOLEC GENET LAB, 1516 JEFFERSON HIGHWAY, NEW ORLEANS, LA 70121 USAOCHSNER MED FDN, DIV RES, MOLEC GENET LAB, 1516 JEFFERSON HIGHWAY, NEW ORLEANS, LA 70121 USA
ALAM, J
;
COOK, JL
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机构:
OCHSNER MED FDN, DIV RES, MOLEC GENET LAB, 1516 JEFFERSON HIGHWAY, NEW ORLEANS, LA 70121 USAOCHSNER MED FDN, DIV RES, MOLEC GENET LAB, 1516 JEFFERSON HIGHWAY, NEW ORLEANS, LA 70121 USA
机构:
Univ Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USAUniv Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USA
Ahn, CH
;
Chae, SY
论文数: 0引用数: 0
h-index: 0
机构:
Univ Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USAUniv Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USA
Chae, SY
;
Bae, YH
论文数: 0引用数: 0
h-index: 0
机构:
Univ Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USAUniv Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USA
Bae, YH
;
Kim, SW
论文数: 0引用数: 0
h-index: 0
机构:
Univ Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USAUniv Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USA
机构:
OCHSNER MED FDN, DIV RES, MOLEC GENET LAB, 1516 JEFFERSON HIGHWAY, NEW ORLEANS, LA 70121 USAOCHSNER MED FDN, DIV RES, MOLEC GENET LAB, 1516 JEFFERSON HIGHWAY, NEW ORLEANS, LA 70121 USA
ALAM, J
;
COOK, JL
论文数: 0引用数: 0
h-index: 0
机构:
OCHSNER MED FDN, DIV RES, MOLEC GENET LAB, 1516 JEFFERSON HIGHWAY, NEW ORLEANS, LA 70121 USAOCHSNER MED FDN, DIV RES, MOLEC GENET LAB, 1516 JEFFERSON HIGHWAY, NEW ORLEANS, LA 70121 USA