An inhibitor of Bcl-2 family proteins induces regression of solid tumours

Tilman Oltersdorf, Steven W. Elmore, Alexander R. Shoemaker, +30

Nature

Tumor BiologyBcl-2 Family ProteinsMedicineSolid TumoursCell Death +7

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

Andrew J. Souers, Erwin R. Boghaert, Scott Ackler, +36

Nature Medicine

ThrombopoiesisThrombosisHematological MalignancyOncologyAntitumor Activity +9

ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor

Christin Tse, Alexander R. Shoemaker, Jessica Adickes, +15

Cancer Research

Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity

Wyndham H. Wilson, Owen A. O’Connor, Myron S. Czuczman, +14

The Lancet Oncology

Hematological MalignancyMedicineMalignant Blood DisorderImmunologyPharmacology +9

The promise and peril of chemical probes

C.H. Arrowsmith, James E. Audia, Christopher P. Austin, +51

Nature Chemical Biology

Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

Loren Lasko, Clarissa G. Jakob, Rohinton Edalji, +36

Nature

Lineage-specific TumoursMedicineImmune Checkpoint InhibitorAnti-cancer AgentTumor Suppressor +6

ABT-888, an Orally Active Poly(ADP-Ribose) Polymerase Inhibitor that Potentiates DNA-Damaging Agents in Preclinical Tumor Models

Cherrie K. Donawho, Yan Luo, Yanping Luo, +34

Clinical Cancer Research

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

Darren C. Phillips, Michael J. Mitten, Erwin R. Boghaert, +29

Science Translational Medicine

Cancer TherapyChemoprevention StrategyBcl-2/bcl-xl/bcl-w Inhibitor Abt-263ImmunologyPharmacotherapy +18

Potent, Orally Active Heterocycle-Based Combretastatin A-4 Analogues:  Synthesis, Structure−Activity Relationship, Pharmacokinetics, and In Vivo Antitumor Activity Evaluation

Le Wang, Keith W. Woods, Qun Li, +13

Journal of Medicinal Chemistry

Medicinal ChemistryDrug TargetingOncologyHeterocyclicStructure−activity Relationship +12

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Emily J. Faivre, Keith F. McDaniel, Daniel H. Albert, +31

Nature

Bd2 BromodomainMedicineNatural SciencesMolecular BiologyCancer Biology +7