Chemistry Reference
In-Depth Information
(a)
O
O
O
(b)
50
40
30
20
10
0
1
10
20
30
35
60
120
200
Number of mixes
(c)
120
100
80
60
40
20
EC50
=
123
ยต
M
0
-6
-5
-4
-3
-2
Log [ZB787]
Figure 6.7
Ligand screening of a bacterial membrane protein. (A) The structure of
Ubiquinone-5 used to asses the integrity of immobilized DsbB during the screen. (B)
Ubiquinone-5 binding to immobilized DsbB during the screen. Binding is defined as in Figure
6.5. (C) Enzyme inhibition curve of a hit from the screen.
6.5 Outlook
In the past decade, an impressive repertoire of methods has been developed to permit drug
development against soluble targets at themolecular level. In addition to fragment screening
methods, structural biology has played a key role in this process. Although at present no
