Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance

Gerrit J.P. Dijkgraaf, Bruno Alicke, Lasse Weinmann, +11

Cancer Research

Molecular BiologyGliomaSmall Molecule InhibitionTumor BiologyDrug Resistance +16

The antiangiogenic protein kinase inhibitors SU5416 and SU6668 inhibit the SCF receptor (c-kit) in a human myeloid leukemia cell line and in acute myeloid leukemia blasts

Beverly D. Smolich, Helene A. Yuen, Kristina West, +3

Blood

MAP4K4 regulates integrin-FERM binding to control endothelial cell motility

Philip Vitorino, Stacey Yeung, Ailey Crow, +9

Nature

Signal TransductionSignaling PathwayCell-matrix InteractionVascular BiologyEndothelial Cell Motility +5

Pharmacokinetic–Pharmacodynamic Analysis of Vismodegib in Preclinical Models of Mutational and Ligand-Dependent Hedgehog Pathway Activation

Harvey Wong, Bruno Alicke, Kristina West, +6

Clinical Cancer Research

X Chromosome-linked Inhibitor of Apoptosis Regulates Cell Death Induction by Proapoptotic Receptor Agonists

Eugene Varfolomeev, Bruno Alicke, J. Michael Elliott, +8

Journal of Biological Chemistry

Discovery of Selective 4-Amino-pyridopyrimidine Inhibitors of MAP4K4 Using Fragment-Based Lead Identification and Optimization

Terry D. Crawford, Chudi Ndubaku, Huifen Chen, +19

Journal of Medicinal Chemistry

Drug TargetBioorganic ChemistryHit IdentificationLead IdentificationPharmacotherapy +14

Gene expression profiling of human colon xenograft tumors following treatment with SU11248, a multitargeted tyrosine kinase inhibitor

Alyssa Morimoto, Nguyêñ Duy Tân, Kristina West, +5

Oncogene

OncologyMedicineColorectal CancerPathologyCancer Genomics +5

Discovery of Highly Potent, Selective, and Efficacious Small Molecule Inhibitors of ERK1/2

Li Ren, Jonas Grina, David Moreno‐Mateos, +17

Journal of Medicinal Chemistry

Chemoprevention StrategyPharmacotherapyChemical BiologyTumor BiologyMedicinal Chemistry +16

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2

James F. Blake, John J. Gaudino, Jason De Meese, +22

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryBiochemistryNatural SciencesMedicine +4

Toxicity Profile of Small-Molecule IAP Antagonist GDC-0152 Is Linked to TNF-α Pharmacology

Rebecca I. Erickson, Jacqueline M. Tarrant, Gary Cain, +12

Toxicological Sciences

Iap AntagonismApoptosisImmunologyImmune RegulationCell Death +19