Our Science

Scientific Publications

[Scientific publications page will use a blog style list and post detail templates. When a user visits the scientific publications page, they will see a list view of links they can click on. We’d recommend on initial page load; the latest 10 publications be shown on the page. The page will include both paginations to access older publications and a filter. The filter could be setup to filter by year, tag, or key word.

To support SEO, we’d recommend instead of each publication linking directly to a PDF, there should be a detail post page that could support a summary or abstract and an image or two from the publication and a link to view the full PDF.]

[Additional Publications formatting forthcoming]


· 2021

o [button] Angela Cacace, Ph.D. PROTAC Discovery Engine: Harnessing the power of oral blood brain barrier penetrant degraders and new E3 ligases. Protein Society Meeting. July 2021 – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/Angela-Cacace-Protein-Society-July-2021_2021-08-06-014908_ebim.pdf

o [button] Angela Cacace, Ph.D. Heterobifunctional Degrader Molecules that lead to the clearance of Pathologic Proteins in Neurodegeneration. Alzheimer’s Association International Conference. July 2021. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/Angela-Cacace-AAIC-July-2021_2021-08-06-014821_rskj.pdf

o [button] Larry Snyder, Ph.D. Discovery of ARV-110, a first in class androgen receptor degrading PROTAC® for the treatment of men with metastatic castration resistant prostate cancer. American Association for Cancer Research Annual Meeting. April 2021 – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/AACR21_ARV110_Structure_Disclosure_2021-08-06-014658_jiuz.pdf

o [button] Larry Snyder, Ph.D. The Discovery of ARV-471, an Orally Bioavailable Estrogen Receptor Degrading PROTAC® for the Treatment of Patients with Breast Cancer. American Association for Cancer Research Annual Meeting. April 2021. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/AACR21_ARV471_Structure_Disclosure_2021-08-06-014540_nkje.pdf

o [button] Ian Taylor, Ph.D. Arvinas PROTAC® Discovery Engine: How Arvinas’ Platform Targets Disease-Causing Proteins in Oncology and Beyond. North American Protein Degradation Congress. February 2021. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/Ian-Taylor-Feb-2021_2021-08-06-014424_iiau.pdf

· 2020

o [button] John Houston, Ph.D. The Promise of PROTAC® Protein Degraders: What’s Next for Arvinas’ Pipeline & Platform. Targeted Protein Degradation Summit. October 2020. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/2020-TPD-Summit_John-H-Presentation_Final-10.13.2020-V2.pdf

· 2019

o [button] 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. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/Cacace_TPD-10-24-2019_final.pdf

o [button] Ian Taylor, Ph.D. Moving PROTAC® Protein Degraders from the Laboratory to the Clinic. Targeted Protein Degradation Summit Boston. October 23, 2019. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/Targeted-Protein-Degradation-Summit-October-2019_FINAL.pdf

o [button] 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. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/Arvinas_AAIC_190718b.pdf

o [button] Neklesa, T. et al. ARV-110: An Oral Androgen Receptor PROTAC Degrader for Prostate Cancer. 2019 GU ASCO. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/AR-GUASCO-2-11-2019.pdf

· 2018

o [button] Flanagan, J. et al. ARV-471, an Oral Estrogen Receptor PROTAC™ Protein Degrader for Breast Cancer. 2018 SABCS. De


o [button] Neklesa, T. et al. An Oral Androgen Receptor PROTAC Degrader for Prostate Cancer. 2018 GU ASCO. February 2018. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/AR-GUASCO2018-final.pdf

o [button] Burslem, G., et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chemical Biology. January 2018. – https://www.cell.com/cell-chemical-biology/fulltext/S2451-9456(17)30353-7

o [button] Bondeson, D., et al. Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead. Cell Chemical Biology. January 2018. – https://www.cell.com/cell-chemical-biology/fulltext/S2451-9456(17)30354-9

· 2017

o [button] Flanagan, J., et al. Identification of Oral Estrogen Receptor PROTAC Degraders for Breast Cancer. San Antonio Breast Cancer Symposium. December 2017. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/2017-SABCS-poster.pdf

o [button] 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. – https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.7b00635

o [button] B Sun, et al. BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells. Leukemia. June 2017. – https://www.nature.com/articles/leu2017207?foxtrotcallback=true

o [button] 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. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/AACR-BRD4-flow-IHC-poster-2017-final.pdf

o [button] Neklesa, T., et al. An Oral Androgen Receptor PROTAC Degrader for Prostate Cancer. AACR 2017. April 2017. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/AR-AACR-final.pdf

o [button] Neklesa, T., et al. An Oral Androgen Receptor PROTAC Degrader for Prostate Cancer. 2017 GU ASCO. February 2017. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/AR-GU-ASCO-02-15-2017.pdf

o [button] 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. – https://www.nature.com/articles/leu2016393

· 2016

o [button] Flanagan, J. Targeted and Selective Degradation of ERa by PROTACs. San Antonio Breast Cancer Symposium. December 2016. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/2016-SABCS-Presentation.pdf

o [button] 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. – https://ash.confex.com/ash/2016/webprogram/Paper91378.html

o [button] 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. – https://ash.confex.com/ash/2016/webprogram/Paper96013.html

o [button] 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. – https://ash.confex.com/ash/2016/webprogram/Paper95952.html

o [button] Coleman, K. BET PROTACs Are More Broadly Effective Than BET Inhibitors. 2016 EORTC-NCI-AACR Symposium. November 2016. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/EORTC-2016-BRD4-Talk_Final-1.pdf

o [button] Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proceedings of the National Academy of Sciences of the United States of America (PNAS). vol. 113 no. 26, June 2016. doi: 10.1073/pnas.1521738113 – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/PNAS-2016-Raina.pdf

o [button] 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. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/AACR-2016-BRD4-Poster.pdf

o [button] 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. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/Yimin-Qian-San-Diego-251st-ACS-Meeting-March-2016.pdf

o [button] Winkler J. PROTAC BRD4 Degraders Allow a More Effective Therapeutic Strategy than BRD4 Inhibitors. 14th International Congress on Targeted Anticancer Therapies (TAT). March 2016. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/Arvinas-TAT-Talk-2016.pdf

· 2015

o [button] 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. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/ASH-2015-Poster.pdf

o [button] 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. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/2015-AACR-NCI-EORTC-Poster.pdf

o [button] Neklesa TK, et al. ARV-330: PROTAC Androgen Receptor Degrader for Prostate Cancer. 22nd Annual Prostate Cancer Foundation (PCF) Scientific Retreat. October 2015. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/PCF-Poster-ARV-330.pdf

o [button] Lu J, et al. “Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4”. Cell Chemical Biology. vol. 22 no. 6, 18 June 2015. doi: 10.1016/j.chembiol.2015.05.009 – https://www.sciencedirect.com/science/article/pii/S1074552115001933?via%3Dihub

o [button] Crew A, et al. Targeted Protein Degradation of Pathological Proteins. Cambridge Healthtech Institute, Discovery on Target Meeting. June 2015. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/Disovery-on-Target-Boston-2015-Andy-Crew.pdf

o [button] 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. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/ASCO-2015-Poster-1.pdf

o [button] Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. American Association for Cancer Research (AACR) Annual Meeting. April 2015. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/AACR-2015-BRD4-Poster.pdf

o [button] Jin M, et al. Targeted Degradation of the Androgen Receptor in Prostate Cancer. American Association for Cancer Research (AACR) Annual Meeting. April 2015. – https://s3.us-east-1.amazonaws.com/arvinas-assets.investeddigital.com/scientific-publications/AACR-2015-PROTAC-Poster.pdf

The agents listed below are currently under investigation. Their safety and effectiveness have not yet been established.

The list below contains scientific publications and presentations related to PROTAC® science and our discovery compounds.

To view publications related to our clinical-stage agents please click button below 

To see congress posters and presentations related to our clinical-stage assets click button below 

Journal/Conference: Dana Farber Cancer Institute
Author: Miklós Békés
December 15, 2022


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