Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D

C D Carroll; T O Johnson; S Tao; G Lauri; M Orlowski; I Y Gluzman; D E Goldberg; R E Dolle

doi:10.1016/s0960-894x(98)00554-x

Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D

Bioorg Med Chem Lett. 1998 Nov 17;8(22):3203-6. doi: 10.1016/s0960-894x(98)00554-x.

Authors

C D Carroll¹, T O Johnson, S Tao, G Lauri, M Orlowski, I Y Gluzman, D E Goldberg, R E Dolle

Affiliation

¹ Department of Biology, Pharmacopeia, Inc., Princeton, NJ 08543, USA.

PMID: 9873703
DOI: 10.1016/s0960-894x(98)00554-x

Abstract

A structure-based 18,900-member combinatorial library was synthesized containing a statine template and three cyclic diamino acids as potential P1, P2-P4 surrogates. Evaluation of this encoded library against two aspartyl proteases, plasmepsin II and cathepsin D, led to the identification of selective inhibitors for each enzyme.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amides / pharmacology*
Amino Acids / pharmacology*
Aspartic Acid Endopeptidases / antagonists & inhibitors*
Cathepsin D / antagonists & inhibitors*
Humans
Protease Inhibitors / pharmacology*
Protozoan Proteins
Structure-Activity Relationship

Substances

Amides
Amino Acids
Protease Inhibitors
Protozoan Proteins
Aspartic Acid Endopeptidases
plasmepsin II
Cathepsin D
statine