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Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity
- Source :
- Bioorganicmedicinal chemistry letters. 18(1)
- Publication Year :
- 2007
-
Abstract
- This letter describes the development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved aqueous solubility (approximately 18 mg/mL) that translates into enhanced cell activity and caspase-3 induction.
- Subjects :
- Serine Proteinase Inhibitors
medicine.drug_class
Clinical Biochemistry
Allosteric regulation
Pharmaceutical Science
Carboxamide
Biochemistry
Cell Line, Tumor
Quinoxalines
Drug Discovery
medicine
Humans
Phosphorylation
Molecular Biology
chemistry.chemical_classification
biology
Kinase
Caspase 3
Organic Chemistry
Water
Biological activity
Enzyme Activation
Kinetics
Enzyme
chemistry
Solubility
Enzyme inhibitor
Cell culture
embryonic structures
biology.protein
Biophysics
Molecular Medicine
Signal transduction
HT29 Cells
Proto-Oncogene Proteins c-akt
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 18
- Issue :
- 1
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....f92b96e5755356731f132077bb118ea0