Structure-based design of novel human Pin1 inhibitors (II)

A series of non-phosphate small molecular Pin1 inhibitors was discovered utilizing SBDD approach. The structure–activity relationship of phosphate replacement groups was investigated. Following the discovery of a novel series of phosphate-containing small molecular Pin1 inhibitors, the drug design s...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2210-2214
Hauptverfasser:	Dong, Liming, Marakovits, Joseph, Hou, Xinjun, Guo, Chuangxing, Greasley, Samantha, Dagostino, Eleanor, Ferre, RoseAnn, Johnson, M. Catherine, Kraynov, Eugenia, Thomson, James, Pathak, Ved, Murray, Brion W.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-cancer agents Antineoplastic agents Binding Sites Biological and medical sciences Carboxylates Crystallography, X-Ray Drug Design Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology General aspects Humans Medical sciences Models, Molecular NIMA-Interacting Peptidylprolyl Isomerase Peptidylprolyl Isomerase - antagonists & inhibitors Peptidylprolyl Isomerase - chemistry Peptidylprolyl Isomerase - metabolism Pharmacology. Drug treatments Phosphate replacement Pin1 Pin1 inhibitors PPIase Protein Binding SBDD Structure-Activity Relationship Tetrazoles
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