Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain

J. Scott Sawyer, Bryan D. Anderson, Douglas W. Beight, +14

Journal of Medicinal Chemistry

Drug TargetPyrazole-based InhibitorsPharmaceutical ChemistryMolecular PharmacologyMedicinal Chemistry +18

Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor

Jonathan M. Yingling, William T. McMillen, Lei Yan, +20

Oncotarget

Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain

J. Scott Sawyer, Douglas W. Beight, Karen S. Britt, +13

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyMedicinal ChemistryPharmaceutical ChemistryBiochemistryMedicine +7

LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models

S. Betty Yan, Victoria L. Peek, Rose T. Ajamie, +19

Investigational New Drugs

Reduced SMAD7 Leads to Overactivation of TGF-β Signaling in MDS that Can Be Reversed by a Specific Inhibitor of TGF-β Receptor I Kinase

Li Zhou, Christine M. McMahon, Tushar D. Bhagat, +24

Cancer Research

Smad7 LeadsTgf-β ReceptorImmunologyImmune RegulationPathology +21

Kinetic Characterization of Novel Pyrazole TGF-β Receptor I Kinase Inhibitors and Their Blockade of the Epithelial−Mesenchymal Transition

Sheng-Bin Peng, Lei Yan, Xiaoling Xia, +10

Biochemistry

Transcriptomic landscape regulated by the 14 types of bone morphogenetic proteins (BMPs) in lineage commitment and differentiation of mesenchymal stem cells (MSCs)

Linghuan Zhang, Qing Luo, Yi Shu, +21

Genes & Diseases

Monensin inhibits cell proliferation and tumor growth of chemo-resistant pancreatic cancer cells by targeting the EGFR signaling pathway

Xin Wang, Xingye Wu, Zhonglin Zhang, +27

Scientific Reports

A Quantitative, Facile, and High-Throughput Image-Based Cell Migration Method Is a Robust Alternative to the Scratch Assay

Wendy H. Gough, Keren I. Hulkower, Renee Lynch, +4

SLAS DISCOVERY

NanotherapeuticsEngineeringCell AdhesionCell CultureBiomedical Engineering +26

Inhibition of Tumor Growth and Metastasis in Non–Small Cell Lung Cancer by LY2801653, an Inhibitor of Several Oncokinases, Including MET

Wenjuan Wu, Bi Chen, Kelly M. Credille, +7

Clinical Cancer Research