Biomedical Engineering Reference
In-Depth Information
O
O
O
N
O
R 1
O
R 2
R 3
9.19
O
O
O
N
O
O
COOH
C
O
9.20
O
O
N
O
HO
O
C
9.21
O
HTS can yield novel lead compounds that require single-step optimization by
molecular modeling and simple group replacements to increase anity.
O
O
N
H 3 C
9.22
NO 2
Recently, modified peptides carrying either aldehyde or borate groups were
synthesized based on the recognition sequence of KLK3/PSA. 112 The Cbz-Ser-
Ser-Lys-Leu-(boro)Leu (Cbz, benzyloxycarbonyl) (Compound 9.23) has a K i of
65 nM for KLK3/PSA which is 60 times lower than that for chymotrypsin. Its
 
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