DDS C ,bc ]^ · 17 % cell growth DMBL 100.00 ppm DMBL 33.33 ppm DMBL 11.11 ppm control DMBL 3.70 ppm DMBL 1.23 ppm DPBL 100.00 ppm DPBL 33.33 ppm DPBL 11.11 ppm DPBL 3.70 ppmDPBL
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5
FFGH�iFG�t��¾¿IJKLM=�FGHNOP
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4-Boronophenylalanine Ethylester(BPA-OEt)
4-Boronobenzylcysteine Ethylester(BBC-OEt)
NH N
HNN
NHHN O O
HO NO
O
NaOONa
O
10BHO OH
10BHOOH
NH N
HNN
NHHN O O
HO NO
O
NaOONa
O S
10BHO OH
S
10BHOOHEC-028 EC-031
10B
COOEt
HO
OH
NH2 10B
SHO
OH
COOEt
NH2
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6
FFGH.�� Jß�]±FGH�i�*�J�=t��¾¿IJKLM=�FGHNOP
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4-Carboran-1-ylmethoxybenzoic acid (CMBA)
OC
HC
OH
O
: nBH
NH N
HNN
NN O O
HO NOHN
O
ONa
O
ONaOONa
O
O
NaO
O C
HC
: nBH
EC-032
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7
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9
FFGHNOPQRHVJ-Envelope (HVJ-E) Vector���
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-Nucleocapsid, -Polymerase
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45V
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BSHSH
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��.� P.127
HVJ-E��89:ê;<=>?@A�4BCÉ(�DEêFGàH�
10
Inactivation BSHLipid mixture
HVJ-liposome
Liposome with boronated compound
HVJ
SH
BSH
HVJ-liposome�I��89:ê9JM��4BCÉ(�DEêKaneda, Y., Dzau, VJ�
11
0
20
40
60
10 12 14 16
Added B (ug)Cel
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KL�rs67i40 ppmtMNkFGHxy�[\r!Í(HVJ-E�OPQ�
BSH�RS���TOU 0.12 – 0.18 Vg/107cells (4.8-7.2ppm)
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13
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14
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15
FFGHMIUB����
double tail
H. Nakamura, Y. Miyajima, T. Takei, S. Kasaoka, K. Maruyama, Chem. Commun. (Hot paper) 2004, 1910.
hydrophilic part
rs��J�=tu�À��XÌO4qvæwm濼xyai�æ ÓÊz¿FGH@�AB�
ý{E5�| Ó¿rh�ö÷�| Óf�}¿~ý{E5�| Ó¿rh�ö÷�| Óf�}¿~FGHxy�FGHxy�7.2 mg/kg7.2 mg/kgr�����Æhr�����Æh14.4mg/kg14.4mg/kg������r| Ó¿~������r| Ó¿~
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n = 16: Stearoyln = 14: Parmitoyln = 12: Myristoyl
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DMCBL (n = 12)DPCBL (n = 14)DSCBL (n = 16)
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17
% c
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DM
BL
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MB
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.33
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MB
L
3.70
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DM
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1.23
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cont
rol
DPB
L10
0.00
ppm
DPB
L 33
.33
ppm
DPB
L 11
.11
ppm
DPB
L 3.
70 p
pmD
PBL
1.23
ppm
DSB
L
100.
00 p
pmD
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33
.33
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DSB
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3.
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.33
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3.33
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DPC
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1.11
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DPC
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3.70
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DPC
BL
1.23
ppm
DSC
BL
100
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DSC
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3
3.33
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DSC
BL
1
1.11
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DSC
BL
3.70
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BL
1.23
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BSH
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33
.33
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B(O
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100.
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100.
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23
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HVJ-E(BSH)��ìi�íØ��� 32mg 10B/kg �ÙG�{õ,ê�xyê86.4 ppm, ÝÞ�xyê0.5 ppmÙG�µ0q�,ê�xyê135 ppm, ÝÞ�xyê0.5 ppmwFGHxy40ppmpq, T/B>10tu4BSH�ÙG�{õ,ìi�íØ��wxy:12-27 ppmhÝÞ�xyê0.6-1.1 ppm
�2��FGHMIUB��ÙG�{õ, ¶Ji�áî��20mg 10B/kg ��24�n!�wxyê13.4 ppm, T/B=17.6T/B>10tu4
��?@AB�ÙG�{õ, ¶Ji���� >40ppm, T/B>10 �u4�!Í��1���FGHMIUB�(Bioconjugate Chem. 17, 1314-20, 2006)7.2mg 10B/kg ��24�n!�wxyê23.1 ppm, T/B=2.3BSHQRTf-PEG-liposome (J. Control. Release 98, 195-207, 2004)35 mg 10B/kg ��72�n!�wxyê33.1ppm, T/B=6.0BSHQRPEG-liposome (J. Control. Release 98, 197-205, 2004)35 mg 10B/kg ��72�n!�wxyê24.3ppm, T/B=2.5
24
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27
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28
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CT26 inoculationin the right flank
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CT26 inoculationin the left flank
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34
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