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OH
OH
HO
HO
OH
HO
O
O
NHAc
O
O
OH
O
HO
HO
O
O
AcH N
OH
HO
Tn
O
OH
H
3
C
O
OH
O
OH
HO
O
Globo H
OH
O
O
O
HO
HO
OH
O
N
N
N
A
HO
AcN H
H
SR
OH
O
O
O
OH
H
3
C
O
OH
OH
OH
O
HO
O
O
OH
O
O
O
O
O
O
Lewis y
NHAc
HO
OH
O
H
3
C
O
K
LH
N
OH
H
R=
OH
HO
O
OH
OH
CO
2
-
OH
OH
HO
HO
HO
OH
HO
Sialyl Tn
O
O
AcNH
O
O
NHAc
O
O
O
HO
OH
HO
HO
O
HO
O
AcH N
O
AcHN
OH
HO
HO
Tn
O
OH
H
3
C
O
OH
O
OH
HO
O
Globo H
OH
HO
O
O
O
HO
O
OH
B
O
O
N
N
NHR
AcN H
H
H
HO
OH
O
O
O
OH
H
3
C
O
OH
OH
O
OH
HO
O
O
OH
O
O
O
O
O
O
HO
AcHN
Lewis y
NHAc
HO
OH
TF
HO
O
O
OH
O
H
3
C
O
OH
HO
HO
OH
OH
HO
O
OH
O
N
N
b.
KLH
R=
Pal
N
a
.
R=
H
S
O
S
O
HN
O
O
O
Pal
Pal
Fig. 1 A) Unimolecular trivalent vaccine. B) Pentavalent vaccine conjugated to two
different carrier proteins, a. KLH and b. Pam
3
Cys (Pal
=
palmitoyl).
In order to target prostate cancer the pentavalent vaccine conjugate
containing five carbohydrate antigens known to be expressed in high
levels on prostate cancer cell surfaces, Tn, TF, sTn, Lewis y, and Globo H,
was prepared. The vaccine was conjugated separately to two different
carrier proteins, KLH and Pam
3
Cys (P
3
CS), (Fig. 1B). Also the hexavalent
vaccine containing Tn, TF, sTn, Le
y
, Globo H and GM2 TACAs was
synthesised.
27
In vivo preclinical serological analysis of this construct,
including ELISA assays and FACS analysis, were carried out. The cumu-
lative data suggests that the immunological properties of the individual
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