Our Science

OUR SCIENCE

Scientific Publications

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

New therapies on the horizon: Targeted protein degradation in neuroscience

Journal/Conference: Cell Chemical Biology

Author: James A. Gregory, Christopher M. Hickey, Juan Chavez, and Angela M. Cacace

September 19, 2024

Development of potent, orally bioavailable PROTAC® LRRK2 degrader molecules as potential disease modifying therapeutics for neurodegeneration

Journal/Conference: Biennial International LRRK2 Meeting

Author: Kaela Kelly, PhD

June 21, 2024

Development of potent, orally bioavailable, and highly selective LRRK2 PROTAC® degrader molecules as potential disease modifying therapeutics for Parkinson’s disease

Journal/Conference: International Congress of Parkinson’s Disease and Movement Disorders

Author: Jere Meredith Jr., Kaela Kelly, Val Guss, Adrianna DeSantis, Lida Kimmel, Sierra Soletsky, Dianne Bryce, Rashaun Wilson, John Corradi, Stefanie Keenan, Greg Cadelina, Jennifer Pizzano, Juan Chavez, Steve Sparks, Angela M. Cacace

March 8, 2024

Plate-based screening approaches and mechanistic insights to inform optimization of PROTAC® degraders for the treatment of neurodegenerative disease

Journal/Conference: SLAS2024 International Conference and Exhibition

Author: D. Revell, L. Soto, D. Rogoz, B. Shebl, G. Naumann, Y-T. Jeong, D. Nickischer, N. Cockroft, A. Hendricson, R. Kyne, S. Sparks, Adams, N., J. Meredith, J. Corradi, J. Landro, L. Snyder, M. Berlin, A. Cacace
Arvinas Operations, Inc., New Haven, CT

February 5, 2024

PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models

Journal/Conference: J Med Chem

Author: Michael Berlin*, Jennifer Cantley, Mark Bookbinder, Elizabeth Bortolon, Fabio Broccatelli, Greg Cadelina, Emily W. Chan, Huifen Chen, Xin Chen, Yunxing Cheng, Tommy K. Cheung, Kim Davenport, Dean DiNicola, Debbie Gordon, Brian D. Hamman, Alicia Harbin, Roy Haskell, Mingtao He, Alison J. Hole, Thomas Januario, Philip S. Kerry, Stefan G. Koenig, Limei Li, Mark Merchant, Inmaculada Pérez-Dorado, Jennifer Pizzano, Connor Quinn, Christopher M. Rose, Emma Rousseau, Leofal Soto, Leanna R. Staben, Hongming Sun, Qingping Tian, Jing Wang, Weifeng Wang, Crystal S. Ye, Xiaofen Ye, Penghong Zhang, Yuhui Zhou, Robert Yauch and Peter S. Dragovich*

January 5, 2024

Co-Opting The E3 Ligase KLHDC2 For Targeted Protein Degradation By Small Molecules

Journal/Conference: Nature Structural & Molecular Biology

Author: Christopher M. Hickey, Katherine M. Digianantonio, Kurt Zimmermann, Alicia Harbin, Connor Quinn, Avani Patel, Peter Gareiss, Amanda Chapman, Bernadette Tiberi, Jennifer Dobrodziej, John Corradi, Angela M. Cacace, David R. Langley & Miklós Békés

January 4, 2024

Physicochemical Property Determinants Of Oral Absorption For PROTAC® Protein Degraders

Journal/Conference: Journal of Medicinal Chemistry

Author: Keith R. Hornberger and Erika M. V. Araujo

June 6, 2023

Small Molecule PROTAC® Hijacking And Structural Characterization Of An E3 Ligase, KLHDC2, For Targeted Protein Degradation

Journal/Conference: Cold Spring Harbor Ubiquitin Meeting

Author: Katie Digianantonio

April 25, 2023

Oral PROTAC® Degrader Molecules To Selectively Clear Proteins In Neurodegenerative Diseases

Journal/Conference: Keystone Symposia: Autophagy and Neurodegeneration

Author: Angela Cacace

March 29, 2023

KRAS-Targeted PROTAC® Degraders Are Broadly Efficacious Against KRAS Dependent Tumor Models

Journal/Conference: Targeting RAS Conference (AACR Special Conference)

Author: Katie Smith

March 8, 2023

High Throughput Screening Techniques To Inform On Compound Liability And Solubility To Advance The PROTAC® Platform

Journal/Conference: Society of Laboratory Automation and Screening

Author: Dustin Revell, et al.

February 25, 2023

Structural Insights Into PROTAC®-Induced Proximity

Journal/Conference: New England Structural Biology Association (NESBA)

Author: Katie Digianantonio

January 25, 2023

Orally Administered PROTAC® Molecules Selectively Clear Pathologic Proteins In CNS & Muscle

Journal/Conference: Society of Neuroscience 2022 Meeting

Author: Angela Cacace, Ph.D.

November 12, 2022

PROTAC® Targeted Protein Degraders: The Past Is Prologue. Nature Reviews Drug Discovery

Journal/Conference: Nature Reviews Drug Discovery

Author: Miklós Békés, et al.

January 18, 2022