IAP Antagonists Induce Autoubiquitination of c-IAPs, NF-κB Activation, and TNFα-Dependent Apoptosis

Eugene Varfolomeev, John W. Blankenship, Sarah M. Wayson, +12

Cell

InflammationCytokineInduce AutoubiquitinationSignal TransductionMedicine +10

Novel antibody–antibiotic conjugate eliminates intracellular S. aureus

Sophie M. Lehar, Thomas H. Pillow, Min Xu, +29

Nature

Antimicrobial Drug DiscoveryAntimicrobial SusceptibilityAntibioticsMedicineMicrobiology +5

P-TEFb kinase is required for HIV Tat transcriptional activation in vivo and in vitro

Helena Mancebo, Gary Lee, John A. Flygare, +8

Genes & Development

Structure-guided design of a selective BCL-XL inhibitor

Guillaume Lessène, Peter E. Czabotar, Brad E. Sleebs, +18

Nature Chemical Biology

Drug TargetMedicineRational Drug DesignPharmacotherapySelective Bcl-xl Inhibitor +2

Discovery of a Potent and Selective BCL-X _L Inhibitor with <i>in Vivo</i> Activity

Zhi‐Fu Tao, Lisa Hasvold, Le Wang, +36

ACS Medicinal Chemistry Letters

Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)

John A. Flygare, Maureen H. Beresini, Nageshwar Budha, +39

Journal of Medicinal Chemistry

ApoptosisCell DeathClinical CandidatePharmacotherapyImmunotherapeutics +18

Design, Synthesis, and Biological Activity of a Potent Smac Mimetic That Sensitizes Cancer Cells to Apoptosis by Antagonizing IAPs

Kerry Zobel, Lan Wang, Eugene Varfolomeev, +8

ACS Chemical Biology

C-iaps 1Protein AssemblySmac InteractionsApoptosisCell Death +19

Targeting LGR5 ⁺ cells with an antibody-drug conjugate for the treatment of colon cancer

Melissa R. Junttila, Weiguang Mao, Xi Wang, +16

Science Translational Medicine

Tumor BiologyCsc MarkerDrug TargetingMedicineAntibody-drug Conjugate +12

A Novel Anti-CD22 Anthracycline-Based Antibody–Drug Conjugate (ADC) That Overcomes Resistance to Auristatin-Based ADCs

Shang‐Fan Yu, Bing Zheng, MaryAnn Go, +10

Clinical Cancer Research

Solid-Phase Synthesis of 2-Aminothiazoles

Patrick C. Kearney, Mónica Fernández, John A. Flygare

The Journal of Organic Chemistry

Materials ScienceCombinatorial ChemistryMolecular SciencesSolid-phase SynthesisEngineering +10