title: Synthesis and conformation-activity relationships of the peptide isosteres of FK228 and largazole.
abstract: The peptide isosteres (10 and 11) of the naturally occurring and potent histone deacetylase (HDAC) inhibitors FK228 and largazole have been synthesized and evaluated side-by-side with FK228, largazole, and SAHA for inhibition of the class I HDACs 1, 2, 3, and 6.
authors.affiliation: Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA.
authors.forename: Albert A
authors.initials: AA
authors.lastname: Bowers
authors.forename: Thomas J
authors.initials: TJ
authors.lastname: Greshock
authors.forename: Nathan
authors.initials: N
authors.lastname: West
authors.forename: Guillermina
authors.initials: G
authors.lastname: Estiu
authors.forename: Stuart L
authors.initials: SL
authors.lastname: Schreiber
authors.forename: Olaf
authors.initials: O
authors.lastname: Wiest
authors.forename: Robert M
authors.initials: RM
authors.lastname: Williams
authors.forename: James E
authors.initials: JE
authors.lastname: Bradner
mesh_terms: D020134:Catalytic Domain; D047630:Depsipeptides / Q000138:chemical synthesis / Q000737:chemistry*; D056284:Histone Deacetylase 1 / Q000037:antagonists & inhibitors / Q000737:chemistry; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D007536:Isomerism; D047029:Lactams, Macrocyclic / Q000138:chemical synthesis / Q000737:chemistry; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D013816:Thermodynamics; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D047630:Depsipeptides; D056572:Histone Deacetylase Inhibitors; D047029:Lactams, Macrocyclic; D013844:Thiazoles; C527895:largazole; C087123:romidepsin; C110550:HDAC1 protein, human; D056284:Histone Deacetylase 1