Scientific Publications

Angela Cacace, Ph.D. Discovery of Brain Penetrant PROTAC® Degrader Molecules That Target Pathologic Tau and alpha‐Synuclein Protein Species. Targeted Protein Degradation Summit Boston. October 24, 2019.

Angela Cacace, Ph.D. A New Therapeutic Strategy for Tauopathies: Discovery of Highly Potent Brain Penetrant Tau PROTAC® Degrader Molecules. Alzheimer's Association International Conference® Presentation, Los Angeles, CA. July 18, 2019.

Neklesa, T. et al. ARV-110: An Oral Androgen Receptor PROTAC Degrader for Prostate Cancer. 2019 GU ASCO.

Flanagan, J. et al. ARV-471, an Oral Estrogen Receptor PROTAC™ Protein Degrader for Breast Cancer. 2018 SABCS. December 2018.

Neklesa, T. et al. An Oral Androgen Receptor PROTAC Degrader for Prostate Cancer. 2018 GU ASCO. February 2018.

Burslem, G., et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chemical Biology. January 2018.

Bondeson, D., et al. Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead. Cell Chemical Biology. January 2018.

Flanagan, J., et al.. Identification of Oral Estrogen Receptor PROTAC Degraders for Breast Cancer. San Antonio Breast Cancer Symposium. December 2017.

Crew, A., et al.. Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1. Journal of Medicinal Chemistry. July 2017.

B Sun, et al.. BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells. Leukemia. June 2017.

Gough, S., et al.. IHC and Flow Cytometry Quantifies BRD4 Levels in Surrogate Tissues After Ex-vivo and In-vivo Dosing with BRD4 Degrading PROTAC. AACR 2017. April 2017.

Neklesa, T., et al.. An Oral Androgen Receptor PROTAC Degrader for Prostate Cancer. AACR 2017. April 2017.

Neklesa, T., et al.. An Oral Androgen Receptor PROTAC Degrader for Prostate Cancer. 2017 GU ASCO. February 2017.

D T Saenz, et al.. Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary(s) AML cells. Leukemia. February 2017.

Flanagan, J. Targeted and Selective Degradation of ERa by PROTACs. San Antonio Breast Cancer Symposium. December 2016.

Sujan Piya, Ph.D. 748 BRD4 Proteolysis Targeting Chimera (PROTAC) ARV-825, Causes Sustained Degradation of BRD4 and Modulation of Chemokine Receptors, Cell Adhesion and Metabolic Targets in Leukemia Resulting in Profound Anti-Leukemic Effects. ASH 58th Annual Meeting & Exposition. December 2016.

Baohua Sun, MD, PhD. 1058 Novel BET Protein Proteolysis Targeting Chimeras (BETP-PROTACs) Exert Potent Single Agent and Synergistic Activity with Ibrutinib and Venetoclax Against Human Mantle Cell Lymphoma Cells. ASH 58th Annual Meeting & Exposition. December 2016.

Dyana T Saenz, Ph.D. 747 Superior Lethal Activity of Novel BET Protein Proteolysis Targeting Chimera (BETP-PROTACs) Versus Betp Bromodomain Inhibitor (BETi) Against Post-Myeloproliferative Neoplasm (MPN) Secondary(s) AML Cells. ASH 58th Annual Meeting & Exposition. December 2016.

Coleman, K. BET PROTACs Are More Broadly Effective Than BET Inhibitors. 2016 EORTC-NCI-AACR Symposium. November 2016.

Raina, K et al. BRD4 Degradation by PROTACs Represents a More Effective Therapeutic Strategy than BRD4 Inhibitors in Ovarian Cancer. American Association for Cancer Research (AACR) Annual Meeting. April 2016.

Qian Y, et al. Hijacking Ubiquitin E3 Ligases Using PROTAC Technology to Effectively Degrade BRD4 and Achieve Anti-tumor Efficacy. 251st American Chemical Society National Meeting. March 2016.

Winkler J. PROTAC BRD4 Degraders Allow a More Effective Therapeutic Strategy than BRD4 Inhibitors. 14th International Congress on Targeted Anticancer Therapies (TAT). March 2016.

Lu J, et al. BRD4 Degradation by PROTACs Represents a More Effective Therapeutic Strategy than BRD4 Inhibitors in DLBCL. 57th American Society of Hematology (ASH) Annual Meeting & Exposition. December 2015.

Neklesa TK, et al. ARV-330: An Androgen Receptor PROTAC Degrader for Prostate Cancer. AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics. November 2015.

Neklesa TK, et al. ARV-330: PROTAC Androgen Receptor Degrader for Prostate Cancer. 22nd Annual Prostate Cancer Foundation (PCF) Scientific Retreat. October 2015.

Crew A, et al. Targeted Protein Degradation of Pathological Proteins. Cambridge Healthtech Institute, Discovery on Target Meeting. June 2015.

Coleman K, et al. BRD4 Degraders Produce Long-Lasting Loss of BRD4 Protein and Robust Efficacy in Burkitt’s Lymphoma, Multiple Myeloma and Prostate Cancer cells. American Society of Clinical Oncology (ASCO) Annual Meeting. May 2015.

Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. American Association for Cancer Research (AACR) Annual Meeting. April 2015.

Jin M, et al. Targeted Degradation of the Androgen Receptor in Prostate Cancer. American Association for Cancer Research (AACR) Annual Meeting. April 2015.