Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors

Autor:	Stanley F. Barnett, Tony Siu, Jeannie M. Arruda, Deborah Defeo-Jones, Jun Liang, Raymond E. Jones, Ronald G. Robinson, Yiwei Li
Rok vydání:	2008
Předmět:	Chemistry Pharmaceutical Clinical Biochemistry Allosteric regulation Cell Pharmaceutical Science Biochemistry Piperazines Inhibitory Concentration 50 Structure-Activity Relationship Drug Discovery medicine Humans Phosphorylation Protein Kinase Inhibitors Molecular Biology Cell potency Protein kinase B chemistry.chemical_classification biology Chemistry Physical Kinase Organic Chemistry Stereoisomerism medicine.anatomical_structure Enzyme Models Chemical chemistry Enzyme inhibitor Drug Design Solvents biology.protein Molecular Medicine Signal transduction Proto-Oncogene Proteins c-akt Allosteric Site
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:4186-4190
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2008.05.085
Popis:	This paper describes the improvement of cell potency in a class of allosteric Akt 1 and 2 inhibitors. Key discoveries include identifying the solvent exposed region of the molecule and appending basic amines to enhance the physiochemical properties of the molecules. Findings from the structure-activity relationships are discussed.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70af821fe16a4a5150c2fa25cf74232d https://doi.org/10.1016/j.bmcl.2008.05.085 Zobrazit plný text záznamu Full Text from ScienceDirect