Synthesis and Evaluation of MGB Polyamide-Oligonucleotide Conjugates as Gene Expression Control Compounds

Table 1

values of modified dsDNAs and respective values.

dsDNAs	Complementary DNA		Mismatch DNA ^d)
	-d(GCCTTAAACCG)-		-d(GCCTTcAACCG)-		-d(GCaTTcAACCG)-
	(°C)^b)	(°C)^c)	(°C)^b)	(°C)^c)	Tm(°C)^b)	(°C)^c)
Unmodified DNA	34.1	—	22.1	—	n.d.^e)	—
Modified DNA ^a)
ON 1 ()	59.5	+25.4^f)	45.6	+23.5	n.d.^e)	—
ON 1 ()	60.2	+26.1
ON 1 ()	52.9	+18.8
ON 2 ()	50.8	+16.7	39.1	+17.0	n.d.^e)	—

^a)modified DNA: -d(CGGAATTTGGC)-, ON 1 (G = Py₄-NH(CH₂)_n-G); ON 2 (G = Py₃-NH(CH₂)_n-G). ^b)dsDNA (4.3 μM) in 10 mM sodium phosphate buffer (pH 7.0) containing 10 mM NaCl and 0.1 mM Na₂EDTA. ^c)ΔT_m (°C) = T_m [modified dsDNA]-T_m (unmodified dsDNA). ^d)mismatch base: a: adenine; c: cytosine. ^e) n.d.: not detected. ^f)it was confirmed that ON 1 () formed stable dsDNA with complementary DNA [13].