A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1

Crystal structures of S6K1 provide insights into the regulation mechanism of S6K1 by the hydrophobic motif

(2013) Jianchuan Wang et al.   BIOCHEMICAL JOURNAL

Selective 3-Phosphoinositide-Dependent Kinase 1 (PDK1) Inhibitors: Dissecting the Function and Pharmacology of PDK1

(2013) Jesús R. Medina   JOURNAL OF MEDICINAL CHEMISTRY

Strategies for the Selective Regulation of Kinases with Allosteric Modulators: Exploiting Exclusive Structural Features

(2012) Zhizhou Fang et al.   ACS Chemical Biology

Akt is efficiently activated by PIF-pocket- and PtdIns(3,4,5)P3-dependent mechanisms leading to resistance to PDK1 inhibitors

(2012) Ayaz Najafov et al.   BIOCHEMICAL JOURNAL

Substrate-Selective Inhibition of Protein Kinase PDK1 by Small Compounds that Bind to the PIF-Pocket Allosteric Docking Site

(2012) Katrien Busschots et al.   CHEMISTRY & BIOLOGY

2-(3-Oxo-1,3-diphenylpropyl)malonic Acids as Potent Allosteric Ligands of the PIF Pocket of Phosphoinositide-Dependent Kinase-1: Development and Prodrug Concept

(2012) Adriana Wilhelm et al.   JOURNAL OF MEDICINAL CHEMISTRY

PDK1 Attenuation Fails to Prevent Tumor Formation in PTEN-Deficient Transgenic Mouse Models

(2011) K. Ellwood-Yen et al.   CANCER RESEARCH

Allosteric Regulation of Protein Kinase PKCζ by the N-Terminal C1 Domain and Small Compounds to the PIF-Pocket

(2011) Laura A. Lopez-Garcia et al.   CHEMISTRY & BIOLOGY

Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors

(2011) Jesús R. Medina et al.   JOURNAL OF MEDICINAL CHEMISTRY

Catalytic Control in the EGF Receptor and Its Connection to General Kinase Regulatory Mechanisms

(2011) Natalia Jura et al.   MOLECULAR CELL

Turning a protein kinase on or off from a single allosteric site via disulfide trapping

(2011) J. D. Sadowsky et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1

(2010) Ayaz Najafov et al.   BIOCHEMICAL JOURNAL

Design and synthesis of benzoazepin-2-one analogs as allosteric binders targeting the PIF pocket of PDK1

(2010) Linyi Wei et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors

(2010) Jianming Zhang et al.   NATURE

Identification of Allosteric PIF-Pocket Ligands for PDK1 using NMR-Based Fragment Screening and1H-15N TROSY Experiments

(2009) Brian J. Stockman et al.   Chemical Biology & Drug Design

Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1

(2009) Valerie Hindie et al.   Nature Chemical Biology

The nuts and bolts of AGC protein kinases

(2009) Laura R. Pearce et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Stoichiometry and Physical Chemistry of Promiscuous Aggregate-Based Inhibitors

(2008) Kristin E. D. Coan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY