title: Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D.
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.
authors.affiliation: Department of Biology, Pharmacopeia, Inc., Princeton, NJ 08543, USA.
authors.forename: C D
authors.initials: CD
authors.lastname: Carroll
authors.forename: T O
authors.initials: TO
authors.lastname: Johnson
authors.forename: S
authors.initials: S
authors.lastname: Tao
authors.forename: G
authors.initials: G
authors.lastname: Lauri
authors.forename: M
authors.initials: M
authors.lastname: Orlowski
authors.forename: I Y
authors.initials: IY
authors.lastname: Gluzman
authors.forename: D E
authors.initials: DE
authors.lastname: Goldberg
authors.forename: R E
authors.initials: RE
authors.lastname: Dolle
mesh_terms: D000577:Amides / Q000494:pharmacology*; D000596:Amino Acids / Q000494:pharmacology*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D002402:Cathepsin D / Q000037:antagonists & inhibitors*; D006801:Humans; D011480:Protease Inhibitors / Q000494:pharmacology*; D015800:Protozoan Proteins; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000596:Amino Acids; D011480:Protease Inhibitors; D015800:Protozoan Proteins; D016282:Aspartic Acid Endopeptidases; C100637:plasmepsin II; D002402:Cathepsin D; C013165:statine