title: Rapid identification of the pharmacophore in a peptoid inhibitor of the proteasome regulatory particle.
abstract: Here we report a simple and effective method to identify the minimal pharmacophore in the first peptoid inhibitor of the 19S proteasome regulatory particle, which has led to the development of a derivative that exhibits improved cellular activity, presumably due to a reduction in mass of about two-fold and the elimination of positively charged lysine-like residues.
authors.affiliation: Division of Translational Research, Department of Internal Medicine, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, Texas 75390-9185, USA.
authors.forename: Hyun-Suk
authors.initials: HS
authors.lastname: Lim
authors.forename: Chase T
authors.initials: CT
authors.lastname: Archer
authors.forename: Young-Chan
authors.initials: YC
authors.lastname: Kim
authors.forename: Troy
authors.initials: T
authors.lastname: Hutchens
authors.forename: Thomas
authors.initials: T
authors.lastname: Kodadek
mesh_terms: D001665:Binding Sites; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008958:Models, Molecular; D015394:Molecular Structure; D008970:Molecular Weight; D046988:Proteasome Endopeptidase Complex / Q000737:chemistry; D061988:Proteasome Inhibitors; D011687:Purines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D007211:Indoles; D061988:Proteasome Inhibitors; D011687:Purines; C528646:Regulatory particle-Inhibiting Peptoid-1; D046988:Proteasome Endopeptidase Complex; C119011:26S proteasome non-ATPase regulatory subunit 13