In:
CHIMIA, Swiss Chemical Society, Vol. 57, No. 4 ( 2003-04-01), p. 179-
Abstract:
Peptidomimetics have been commonly used as lead compounds to design inhibitors with high affinity and specificity for a particular enzyme. The discovery that a 2-aminobenzylstatine derivative originally designed to target an aspartyl protease was able to inhibit specifically and non-covalently
the chymotrypsin-like activity of the 20S proteasome represented a unique starting point for our medicinal chemistry endeavor for this target. Utilizing a structure-based design approach, we have been able to improve the potency of this new class of proteasome inhibitors without affecting its in vitro selectivity profile.
Type of Medium:
Online Resource
ISSN:
2673-2424
,
0009-4293
DOI:
10.2533/000942903777679415
Language:
Unknown
Publisher:
Swiss Chemical Society
Publication Date:
2003
detail.hit.zdb_id:
2179192-2