New protease inhibitors for HCV – Help is on the way
✍ Scribed by Dahlene N. Fusco; Raymond T. Chung
- Book ID
- 116652368
- Publisher
- Elsevier Science
- Year
- 2011
- Tongue
- English
- Weight
- 280 KB
- Volume
- 54
- Category
- Article
- ISSN
- 0168-8278
No coin nor oath required. For personal study only.
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## Abstract Plasmepsin II (PMII), a malarial aspartic protease involved in the catabolism of hemoglobin in parasites of the genus __Plasmodium__, and renin, a human aspartic protease, share 35% sequence identity in their mature chains. Structures of 4‐arylpiperidine inhibitors complexed to human re
## Abstract A new class of nonpeptidic inhibitors of the malarial aspartic protease plasmepsin II (PMII) with up to single‐digit micromolar activities (__IC__~50~ values) was developed by structure‐based __de novo__ design. The active‐site matrix used in the design was based on an X‐ray crystal str