Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1<i>H</i>-indol-5-yl)-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

Jeffrey M. Axten, Jesús R. Medina, Yanhong Feng, +21

Journal of Medicinal Chemistry

Chemoprevention StrategyChemical BiologyPharmaceutical ChemistryTumor BiologyMolecular Pharmacology +22

Suppression of angiogenesis and tumor growth by selective inhibition of angiopoietin-2

Jonathan D. Oliner, Hosung Min, Juan Leal, +40

Cancer Cell

Selective InhibitionAngiogenesisMedicineTumor GrowthVascular Biology +6

Discovery of 5-[[4-[(2,3-Dimethyl-2<i>H</i>-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a Novel and Potent Vascular Endothelial Growth Factor Receptor Inhibitor

Philip A. Harris, Amogh Boloor, Mui Cheung, +18

Journal of Medicinal Chemistry

Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity

Nelson Rhodes, Dirk A. Heerding, Derek R. Duckett, +19

Cancer Research

Tumor XenograftsAntitumor ActivityChemoprevention StrategyApoptosisImmunology +19

Demonstration of a Genetic Therapeutic Index for Tumors Expressing Oncogenic <i>BRAF</i> by the Kinase Inhibitor SB-590885

Alastair J. King, Denis R. Patrick, Roberta S. Batorsky, +26

Cancer Research

PathologyOncogenic Braf AllelesTumor BiologyOncologyTumor Phenotype +15

Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development

Jeffrey M. Axten, Stuart P. Romeril, Arthur Y. L. Shu, +15

ACS Medicinal Chemistry Letters

Drug Discovery ProgramTumor BiologyPhysical PropertiesMedicinal ChemistrySignaling Pathway +16

The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma

Klaus Podar, Giovanni Tonon, Martin Sattler, +10

Proceedings of the National Academy of Sciences

OncologyAngiogenesisEndothelial CellsMedicineImmunology +11

p21-activated Kinase-1 Signaling Mediates Cyclin D1 Expression in Mammary Epithelial and Cancer Cells

Seetharaman Balasenthil, Ayşegül A. Şahin, Christopher J. Barnes, +4

Journal of Biological Chemistry

Association Between Pak1 Expression and Subcellular Localization and Tamoxifen Resistance in Breast Cancer Patients

Caroline Holm, Suresh K. Rayala, Karin Jirström, +3

JNCI Journal of the National Cancer Institute

Filamin A regulates focal adhesion disassembly and suppresses breast cancer cell migration and invasion

Yingjie Xu, Tarek A. Bismar, Jie Su, +8

The Journal of Experimental Medicine

Cell AdhesionMolecular BiologyCytoskeletonCancer BiologyCellular Physiology +15