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as ER-112022 ( 9 ) also have shown agonistic activity through the TLR4
receptor without the need for CD14 (Lien et al. , 2001).
NHBz
AcO
O
Ph
O
OH
HO
O
O
O
Taxol ( 7 )
HO
H
NH
HN
O
BzO
OAc
O
HO
O
O
P
O
O
P
O
O
(HO) 2 P
OH
HO
O
O
H
O
NH
O
ER-112022 ( 9 )
O
HN
NH
O
O
O
O
HO
O
O
O
O
O
O
O
O
GLA-60 ( 8 )
Fig. 6.5 Some LPS agonists.
6.1.4.2 LPS antagonists
There are considerably more reports of LPS antagonists than LPS
agonists in the literature (Black et al. , 1997b, Newton and Decicco,
1999, Paul et al. , 2006). One of the earliest approaches to developing
LPS antagonists relied on analogues of active lipid A itself. These
analogues competitively inhibited LPS/lipid A binding to the
TLR4/CD14 receptor complex. For example, the lipid A's of the non-
pathogenic Gram-negative bacteria Rhodobacter capsulatus ( 10 ) and
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