AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies

Garrett W. Rhyasen, Maureen M. Hattersley, Yi Yao, +26

Molecular Cancer Therapeutics

Azd5153 ExposurePathologyPharmacotherapyTumor BiologyMyeloid Neoplasia +15

Potent and selective bivalent inhibitors of BET bromodomains

Michael J. Waring, Huawei Chen, Alfred A. Rabow, +27

Nature Chemical Biology

Medicinal ChemistrySelective Bivalent InhibitorsMedicineDrug DevelopmentPharmacology +1

Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6

William McCoull, Tony Cheung, Erica Anderson, +34

ACS Chemical Biology

Hematological MalignancyLymphoid NeoplasiaB-cell Lymphoma 6MedicineMalignant Blood Disorder +12

Discovery and Mechanistic Study of a Small Molecule Inhibitor for Motor Protein KIFC1

Jiaquan Wu, Keith Mikule, Wenxian Wang, +12

ACS Chemical Biology

Molecular BiologySmall Molecule InhibitorCytoskeletonMechanistic StudyCell Cycle +19

Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering

Jeffrey W. Johannes, Lynsie Almeida, Kevin Daly, +24

Bioorganic & Medicinal Chemistry Letters

MedicineNatural SciencesMolecular BiologyDrug DevelopmentChemical Biology +3

Shear Stress Decreases Endothelial Cell Tissue Factor Activity by Augmenting Secretion of Tissue Factor Pathway Inhibitor

Eríc F. Grabowski, Armin J. Reininger, Philip Petteruti, +2

Arteriosclerosis Thrombosis and Vascular Biology

EngineeringImmune RegulationImmunologyBlood CellTotal Rna +26

MEDI0639: A Novel Therapeutic Antibody Targeting Dll4 Modulates Endothelial Cell Function and Angiogenesis <i>In Vivo</i>

David W. Jenkins, Sarah J. Ross, Margaret H. Veldman-Jones, +15

Molecular Cancer Therapeutics

AngiogenesisNovel TherapyMedicineTumor GrowthImmunology +11

Pharmacological Inhibition of PARP6 Triggers Multipolar Spindle Formation and Elicits Therapeutic Effects in Breast Cancer

Zebin Wang, Shaun Grosskurth, Tony Cheung, +22

Cancer Research

Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors

Ryan T. Howard, Paul Hemsley, Philip Petteruti, +5

ACS Chemical Biology

Identification of CCR2 and CD180 as Robust Pharmacodynamic Tumor and Blood Biomarkers for Clinical Use with BRD4/BET Inhibitors

Tammie C. Yeh, Greg O’Connor, Philip Petteruti, +4

Clinical Cancer Research