Synthesis and conformation-activity relationships of the peptide isosteres of FK228 and largazole.
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.
Bowers
Albert A
AA
Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA.
Greshock
Thomas J
TJ
West
Nathan
N
Estiu
Guillermina
G
Schreiber
Stuart L
SL
Wiest
Olaf
O
Williams
Robert M
RM
Bradner
James E
JE
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*
D047630:Depsipeptides; D056572:Histone Deacetylase Inhibitors; D047029:Lactams, Macrocyclic; D013844:Thiazoles; C527895:largazole; C087123:romidepsin; C110550:HDAC1 protein, human; D056284:Histone Deacetylase 1