Definition of the binding mode of a new class of phosphoinositide 3-kinase α-selective inhibitors usingin vitromutagenesis of non-conserved amino acids and kinetic analysis

The Evolution of Protein Kinase Inhibitors from Antagonists to Agonists of Cellular Signaling

(2011) Arvin C. Dar et al.   Annual Review of Biochemistry

A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types

(2011) Stephen Jamieson et al.   BIOCHEMICAL JOURNAL

New phosphatidylinositol 3-kinase inhibitors for cancer

(2011) Daniel W Bowles et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Conformational adaptation in drug–target interactions and residence time

(2011) Robert A Copeland   Future Medicinal Chemistry

Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform

(2011) Timothy P. Heffron et al.   JOURNAL OF MEDICINAL CHEMISTRY

Isoform-Selective Inhibition of Phosphoinositide 3-Kinase: Identification of a New Region of Nonconserved Amino Acids Critical for p110  Inhibition

(2011) Z. Zheng et al.   MOLECULAR PHARMACOLOGY

Drugging the PI3 Kinome: From Chemical Tools to Drugs in the Clinic

(2010) P. Workman et al.   CANCER RESEARCH

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

(2010) Alex Berndt et al.   Nature Chemical Biology

The emerging mechanisms of isoform-specific PI3K signalling

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

Cancer-derived mutations in the regulatory subunit p85  of phosphoinositide 3-kinase function through the catalytic subunit p110 

(2010) M. Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A frequent kinase domain mutation that changes the interaction between PI3K  and the membrane

(2009) D. Mandelker et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Dissecting isoform selectivity of PI3K inhibitors: the role of non-conserved residues in the catalytic pocket

(2008) Mark Frazzetto et al.   BIOCHEMICAL JOURNAL

Phosphoinositide-3-kinases (PI3Ks):  Combined Comparative Modeling and 3D-QSAR To Rationalize the Inhibition of p110α

(2008) Raphaël Frédérick et al.   Journal of Chemical Information and Modeling