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3,5-Diphenylpent-2-enoic Acids as Allosteric Activators of the Protein Kinase PDK1: Structure―Activity Relationships and Thermodynamic Characterization of Binding as Paradigms for PIF-Binding Pocket-Targeting Compounds

Author
STROBA, Adriana1 ; SCHAEFFER, Francis2 ; HINDIE, Valerie3 ; LOPEZ-GARCIA, Laura3 ; ADRIAN, Iris3 ; FRÖHNER, Wolfgang1 ; HARTMANN, Rolf W1 ; BIONDI, Ricardo M3 ; ENGEL, Matthias1
[1] Pharmaceutical and Medicinal Chemistry, Saarland University, P.O. Box 151150, 66041 Saarbrücken, Germany
[2] Unité de Biochimie Structurale (CNRS-URA 2185), Institut Pasteur, 75724 Paris, France
[3] Department of Internal Medicine I, University of Frankfurt. Theodor-Stern-Kai 7, 60590 Frankfurt a.M., Germany
Source

Journal of medicinal chemistry (Print). 2009, Vol 52, Num 15, pp 4683-4693, 11 p ; ref : 42 ref

CODEN
JMCMAR
ISSN
0022-2623
Scientific domain
Pharmacology drugs
Publisher
American Chemical Society, Columbus, OH
Publication country
United States
Document type
Article
Language
English
Keyword (fr)
Activation allostérique Chlore Composé organique Ciblage Dérivé de l'indane Dérivé de l'indole Dérivé du benzofurane Dérivé du benzothiophène Interaction électrostatique Non-specific serine/threonine protein kinase Relation structure activité Site fixation Synthèse chimique Thermodynamique Transduction signal Benzo[b]thiophène dérivé Cinnamique acide(β-[2-aryléthyl]) Enzyme Transferases
Keyword (en)
Allosteric activation Chlorine Organic compounds Targeting Indan derivatives Indole derivatives Benzofuran derivatives Benzothiophene derivatives Electrostatic interaction Non-specific serine/threonine protein kinase Structure activity relation Binding site Chemical synthesis Thermodynamics Signal transduction Enzyme Transferases
Keyword (es)
Activación alostérica Cloro Compuesto orgánico Blancado Indol derivado Benzotiofeno derivado Interacción electrostática Non-specific serine/threonine protein kinase Relación estructura actividad Sitio fijación Síntesis química Termodinámica Transducción señal Enzima Transferases
Classification
Pascal
002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02W Miscellaneous

Discipline
General pharmacology
Origin
Inist-CNRS
Database
PASCAL
INIST identifier
22098197

Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS

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