Biomedical Engineering Reference
In-Depth Information
TABLE 11.1 Applications Reported for the De Novo Discovery of Small Molecules
Reference
Format a
Size
Target Protein
Selection Results
Institution/Company
Section
Halpin & Harbury
2004 [59]
1 million
DNA routed
Anti-enkephalin mAb
Proof of principle
Stanford University
11.2.2.2
Gartner et al. 2004
[60]
65
DNA templated
Carbonic anhydrase
Proof of principle
Harvard University
11.2.2.3
Melkko et al. 2004
[92]
138
Dual pharmacophore
(ESAC)
Streptavidin
Proof of principle
ETH Z urich
11.2.3
Melkko et al. 2007
[95]
550
Dual pharmacophore
(ESAC)
Trypsin
98 nM (based on lead
structure)
ETH Z urich
11.2.3
Wrenn and
Harbury 2007
[115]
100 million
DNA routed
N-CrkSH3
16
M (focused library)
Stanford University
11.2.2.2
M (de novo) b
Mannocci et al.
2008 [54]
4,000
DNA conjugate (2)
Streptavidin
0.35
ETH Z urich/Philochem
AG
11.2.2.1
Mannocci et al.
2008 [54]
4,000
DNA conjugate (2)
Poly-IgG
Chromatography resin
ETH Z urich/Philochem
AG
11.2.2.1
Tse et al. 2008 [61]
13,824
DNA templated
Not reported
Harvard University
11.2.2.3
M (de novo) d
ETH Z urich/Philochem
AG
Dumelin et al.
2008 [64]
550
Dual pharmacophore
(ESAC)
HSA
3.2
11.2.3
Scheuermann et al.
2008 [94]
550
Dual pharmacophore
(ESAC)
MMP-3
9.9
M (de novo) d
ETH Z urich/Philochem
AG
11.2.3
Clark et al. 2009
[58]
ca. 7 million
DNA conjugate (3)
p38 MAP kinase
2 nM (based on lead
structure) c
GSK/Praecis
Pharmaceuticals
11.2.2.1
Clark et al. 2009
[58]
ca. 7 million
DNA conjugate (3)
Aurora A kinase
0.27-6.3
M (de novo) c
GSK/Praecis
Pharmaceuticals
11.2.2.1
M (de novo) c,d
Clark et al. 2009
[58]
ca. 800 million
DNA conjugate (4)
p38 MAP kinase
0.25
GSK/Praecis
Pharmaceuticals
11.2.2.1
 
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