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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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
The Arvinas PROTAC® Discovery Engine: PROTAC® Biophysical Characterization Fuels The Discovery Of Target And E3 Ligase Ligands For Optimized PROTAC® Degrader Molecules
Journal/Conference: American Chemical Society (ACS) Spring 2023
Author: Alicia Harbin
March 28, 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