Science
Scientific Publications
- November, 2017
- April, 2017Targeting the MDM2–p53 Protein–Protein Interaction for New Cancer Therapy: Progress and Challenges. Cold Spring Harbor Perspectives in Medicine.
View - April, 2017A Network of Substrates of the E3 Ubiquitin Ligases MDM2 and HUWE1 Control Apoptosis Independently of p53. http://stke.sciencemag.org/.
View - March, 2017Discovery of 4‑((3′R,4′S,5′R)‑6″-Chloro-4′-(3-chloro-2-fluorophenyl)-1′-ethyl-2″-oxodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indoline]-5′-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development. Journal of Medicinal Chemistry.
View - October, 2016Reactivation of p53 by MDM2 Inhibitor MI-77301 for the Treatment of Endocrine-Resistant Breast Cancer. Molecular Cancer Therapeutics.
View - August, 2016Therapeutic Inhibition of the MDM2–p53 Interaction Prevents Recurrence of Adenoid Cystic Carcinomas. Clinical Cancer Research.
View - March, 2016
- February, 2016TNFa-Mediated Cytotoxic Responses to IAP Inhibition Are Limited by the p38a MAPK Pathway. Cancer Cell.
View - January, 2016MDM2 Inhibition Sensitizes Prostate Cancer Cells to Androgen Ablation and Radiotherapy in a p53-Dependent Manner. Neoplasia.
View - March, 2015Elucidation of Acquired Resistance to Bcl-2 and MDM2 Inhibitors in Acute Leukemia In Vitro and In Vivo. Clinical Cancer Research.
View - August, 2014SAR405838: An Optimized Inhibitor of MDM2–p53 Interaction That Induces Complete and Durable Tumor Regression. Cancer Research.
View - June, 2014BM-1197: A Novel and Specific Bcl-2/Bcl-xL Inhibitor Inducing Complete and Long-Lasting Tumor Regression In Vivo. PLOS One.
View - January, 2014Smac Mimetics and Innate Immune Stimuli Synergize to Promote Tumor Death. Nature Biotechnology.
View - May, 2013A Network of Substrates of the E3 Ubiquitin Ligases MDM2 and HUWE1 Control Apoptosis Independently of p53. Science Signaling.
View - May, 2013Diastereomeric Spirooxindoles as Highly Potent and Efficacious MDM2 Inhibitors. Journal of the American Chemical Society.
View - February, 2013
- July, 2012Structure-Based Design of Potent Bcl-2/Bcl-xL Inhibitors with Strong In Vivo Antitumor Activity. Journal of Medicinal Chemistry.
View - March, 2012Design of Bcl-2 and Bcl-xL Inhibitors with Subnanomolar Binding Affinities Based upon a New Scaffold. Journal of Medicinal Chemistry.
View - May, 2011Potent Bivalent Smac Mimetics: Effect of the Linker on Binding to Inhibitor of Apoptosis Proteins (IAPs) and Anticancer Activity. Journal of Medicinal Chemistry.
View - September, 2010Non-Peptidic and Potent Small-Molecule Inhibitors of cIAP-1/2 and XIAP Proteins. Journal of Medicinal Chemistry.
View - September, 2010
- April, 2010Cyclopeptide Smac Mimetics as Antagonists of IAP Proteins. Bioorganic & Medicinal Chemistry Letters.
View - November, 2009Potent and Orally Active Small-Molecule Inhibitors of the MDM2-p53 Interaction. Journal of Medicinal Chemistry.
View - July, 2008Interaction of a Cyclic, Bivalent Smac Mimetic with the X-Linked Inhibitor of Apoptosis Protein. Biochemistry.
View - September, 2007Small Molecule Inhibitors of the MDM2-p53 Interaction Discovered by Ensemble-Based Receptor Models. Journal of the American Chemical Society.
View - June, 2007Therapeutic Window for Melanoma Treatment Provided by Selective Effects of the Proteasome on Bcl-2 Proteins. Cell Death and Differentiation.
View - April, 2007Pyrogallol-Based Molecules as Potent Inhibitors of the Antiapoptotic Bcl-2 Proteins. Journal of Medicinal Chemistry.
View - October, 2006Structure-Based Design of Potent Small-Molecule Inhibitors of Anti-Apoptotic Bcl-2 Proteins. Journal of Medicinal Chemistry.
View - September, 2006
- June, 2005Structure-Based Design of Potent Non-Peptide MDM2 Inhibitors. Journal of the American Chemical Society.
View - June, 2005Bcl-2 Acts in a Proangiogenic Signaling Pathway through Nuclear, Factor-KB and CXC Chemokines. Cancer Research .
View - January, 2005Gossypol Acts Directly on the Mitochondria to Overcome Bcl-2- and Bcl-XL-Mediated Apoptosis Resistance. Molecular Cancer Therapeutics.
View - November, 2004Breast Cancer Cells Can Evade Apoptosis-Mediated Selective Killing by a Novel Small Molecule Inhibitor of Bcl-2. American Association for Cancer Research .
View - July, 2004Development and Optimization of a Binding Assay for the XIAP BIR3 Domain Using Fluorescence Polarization. Analytical Biochemistry.
View - January, 2001Discovery of Small-Molecule Inhibitors of Bcl-2 through Structure-Based Computer Screening. Journal of Medicinal Chemistry.
View - Note: This is a select list of our scientific publications.