A class of highly selective inhibitors bind to an active state of PI3Kγ

Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors

(2018) Nils Pemberton et al.   JOURNAL OF MEDICINAL CHEMISTRY

PKIDB: A Curated, Annotated and Updated Database of Protein Kinase Inhibitors in Clinical Trials

(2018) Fabrice Carles et al.   MOLECULES

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology

(2017) Florent Beaufils et al.   JOURNAL OF MEDICINAL CHEMISTRY

PI3Kγ activity in leukocytes promotes adipose tissue inflammation and early-onset insulin resistance during obesity

(2017) Ludovic Breasson et al.   Science Signaling

Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

(2017) Thomas Bohnacker et al.   Nature Communications

PI3Kγ activity in leukocytes promotes adipose tissue inflammation and early-onset insulin resistance during obesity

(2017) Ludovic Breasson et al.   Science Signaling

PI3Kγ is a molecular switch that controls immune suppression

(2016) Megan M. Kaneda et al.   NATURE

Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate

(2016) Catherine A. Evans et al.   ACS Medicinal Chemistry Letters

Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase γ

(2015) Philip N. Collier et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting PI3 kinase in cancer

(2015) Todd M. Bauer et al.   PHARMACOLOGY & THERAPEUTICS

Structural and dynamic insights into the energetics of activation loop rearrangement in FGFR1 kinase

(2015) Tobias Klein et al.   Nature Communications

Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kβ inhibitors, useful as antiplatelet agents

(2014) Fabrizio Giordanetto et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting PI3Kγ activity decreases vascular trauma-induced intimal hyperplasia through modulation of the Th1 response

(2014) Natalia F. Smirnova et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Structural Basis for Isoform Selectivity in a Class of Benzothiazole Inhibitors of Phosphoinositide 3-Kinase γ

(2014) Philip N. Collier et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of phosphoinositide 3-kinase γ attenuates inflammation, obesity, and cardiovascular risk factors

(2013) Matthias P. Wymann et al.   Annals of the New York Academy of Sciences

Elastin-derived peptides potentiate atherosclerosis through the immune Neu1–PI3Kγ pathway

(2013) Stephanie Gayral et al.   CARDIOVASCULAR RESEARCH

Transient targeting of phosphoinositide 3-kinase acts as a roadblock in mast cells' route to allergy

(2013) Emilie Collmann et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Molecular determinants of PI3K -mediated activation downstream of G-protein-coupled receptors (GPCRs)

(2013) O. Vadas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

PKCβ Phosphorylates PI3Kγ to Activate It and Release It from GPCR Control

(2013) Romy Walser et al.   PLOS BIOLOGY

Overview of theCCP4 suite and current developments

(2011) Martyn D. Winn et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Structure of Lipid Kinase p110β/p85β Elucidates an Unusual SH2-Domain-Mediated Inhibitory Mechanism

(2011) Xuxiao Zhang et al.   MOLECULAR CELL

PI3K  within a nonhematopoietic cell type negatively regulates diet-induced thermogenesis and promotes obesity and insulin resistance

(2011) B. Becattini et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Dynamics of the Phosphoinositide 3-Kinase p110δ Interaction with p85α and Membranes Reveals Aspects of Regulation Distinct from p110α

(2011) John E. Burke et al.   STRUCTURE

Integration, scaling, space-group assignment and post-refinement

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Interaction Kinetic and Structural Dynamic Analysis of Ligand Binding to Acetylcholine-Binding Protein

(2010) Matthis Geitmann et al.   BIOCHEMISTRY

The Utility of Hydrogen/Deuterium Exchange Mass Spectrometry in Biopharmaceutical Comparability Studies

(2010) Damian Houde et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

The p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitors

(2010) Alex Berndt et al.   Nature Chemical Biology

PI3K  Adaptor Subunits Define Coupling to Degranulation and Cell Motility by Distinct PtdIns(3,4,5)P3 Pools in Mast Cells

(2009) T. Bohnacker et al.   Science Signaling

Genetic and Pharmacological Targeting of Phosphoinositide 3-Kinase-γ Reduces Atherosclerosis and Favors Plaque Stability by Modulating Inflammatory Processes

(2008) Anne Fougerat et al.   CIRCULATION

Type-II Kinase Inhibitor Docking, Screening, and Profiling Using Modified Structures of Active Kinase States

(2008) Irina Kufareva et al.   JOURNAL OF MEDICINAL CHEMISTRY