Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases

Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ–PI3Kδ Dual Inhibitors

(2019) Hong Jia et al.   JOURNAL OF MEDICINAL CHEMISTRY

Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective

(2018) Aimie E. Garces et al.   JOURNAL OF MEDICINAL CHEMISTRY

Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases

(2018) Matthew W. D. Perry et al.   JOURNAL OF MEDICINAL CHEMISTRY

Atropisomerism and Conformational Equilibria: Impact on PI3Kδ Inhibition of 2-((6-Amino-9H-purin-9-yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one (IC87114) and Its Conformationally Restricted Analogs

(2017) Alessio Lodola et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phase 2 study of idelalisib and entospletinib: pneumonitis limits combination therapy in relapsed refractory CLL and NHL

(2016) P. M. Barr et al.   BLOOD

Idelalisib in the management of lymphoma

(2016) C. Y. Cheah et al.   BLOOD

2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective Inhibitors

(2016) Leena Patel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases

(2016) Montse Erra et al.   ACS Medicinal Chemistry Letters

Idelalisib-associated Enterocolitis

(2015) Christine Y. Louie et al.   AMERICAN JOURNAL OF SURGICAL PATHOLOGY

Idelalisib-associated Colitis

(2015) Anna-Sophie Weidner et al.   AMERICAN JOURNAL OF SURGICAL PATHOLOGY

PI3K signalling in inflammation

(2015) P.T. Hawkins et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Structural, Biochemical, and Biophysical Characterization of Idelalisib Binding to Phosphoinositide 3-Kinase δ

(2015) John R. Somoza et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors

(2015) Youngsook Shin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecules in medicine mini-review: isoforms of PI3K in biology and disease

(2015) Bart Vanhaesebroeck et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Discovery and in Vivo Evaluation of (S)-N-(1-(7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and Related PI3Kδ Inhibitors for Inflammation and Autoimmune Disease

(2014) Timothy D. Cushing et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting phosphoinositide 3-kinase δ for the treatment of respiratory diseases

(2013) Srividya Sriskantharajah et al.   Annals of the New York Academy of Sciences

Signaling by the Phosphoinositide 3-Kinase Family in Immune Cells

(2013) Klaus Okkenhaug   Annual Review of Immunology

Enantiomeric Atropisomers Inhibit HCV Polymerase and/or HIV Matrix: Characterizing Hindered Bond Rotations and Target Selectivity

(2013) Steven R. LaPlante et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting phosphoinositide 3-kinase δ for allergic asthma

(2012) Wendy C. Rowan et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Discovery and in Vivo Evaluation of Dual PI3Kβ/δ Inhibitors

(2012) Felix Gonzalez-Lopez de Turiso et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Methylation Effect in Medicinal Chemistry

(2011) Eliezer J. Barreiro et al.   CHEMICAL REVIEWS

Small-molecule inhibitors of the PI3K signaling network

(2011) Colleen R McNamara et al.   Future Medicinal Chemistry

Assessing Atropisomer Axial Chirality in Drug Discovery and Development

(2011) Steven R. LaPlante et al.   JOURNAL OF MEDICINAL CHEMISTRY

PI3K  Plays a Critical Role in Neutrophil Activation by Immune Complexes

(2011) S. Kulkarni et al.   Science Signaling

The SMARTCyp cytochrome P450 metabolism prediction server

(2010) Patrik Rydberg et al.   BIOINFORMATICS

The emerging mechanisms of isoform-specific PI3K signalling

(2010) Bart Vanhaesebroeck et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

The Challenge of Atropisomerism in Drug Discovery

(2009) Jonathan Clayden et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Animal models of rheumatoid arthritis

(2009) Darren L. Asquith et al.   EUROPEAN JOURNAL OF IMMUNOLOGY

Phosphatidylinositol 3-kinase inhibitors: promising drug candidates for cancer therapy

(2008) Dexin Kong et al.   CANCER SCIENCE

Class IA phosphatidylinositol 3-kinase: from their biologic implication in human cancers to drug discovery

(2008) Sauveur-Michel Maira et al.   EXPERT OPINION ON THERAPEUTIC TARGETS