Our Science

OUR SCIENCE

Scientific Publications

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

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VIEW CONGRESS PRESENTATIONS

Discovery of oral PROTAC LRRK2 degraders as potential treatments for neurodegenerative disorders

Journal/Conference: Michael J. Fox Foundation 2024 Parkinson’s Disease Therapeutics Conference

Author: Angela Cacace, PhD

Date: October 17, 2024

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