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From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9

Whitney L. Petrilli, Gregory Adam, Roman S. Erdmann, Pravien Abeywickrema, Viju Agnani, Xi Ai, Jen Baysarowich, Noel Byrne, John Caldwell, Wonsuk Chang, Edward DiNunzio, Zhe Feng, Rachel Ford, Sookhee Ha, Yongcheng Huang, Brian Hubbard, Jennifer M. Johnston, Michael Kavana, Jean-Marie Lisnock, Rui Liang, Jun Lu, Zhijian Lu, Juncai Meng, Peter Orth, Oksana Palyha, Gopal Parthasarathy, Scott P. Salowe, Sujata Sharma, Jennifer Shipman, Stephen Soisson, Alison Strack, Hyewon Youm, Kake Zhao, Debbie Zinc, Hratch Zokian, George Addona, Karen Akinsanya, James R. Tata, Yusheng Xiong, Jason E. Imbriglio

Version 1 posted 09 July 2019

1,055

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Biological and Medicinal Chemistry

Working Paper

Targeted Protein Degradation via a Covalent Reversible Degrader Based on Bardoxolone

Bingqi Tong, Mai Luo, Yi Xie, Jessica Spradlin, John A. Tallarico, Jeffrey M. McKenna, Markus Schirle, Thomas J. Maimone, Daniel Nomura

Version 1 posted 02 April 2020

2,778

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2

Citations

Biological and Medicinal Chemistry

Working Paper

A Mathematical Model for Covalent Proteolysis Targeting Chimeras: Thermodynamics and Kinetics underlying Catalytic Efficiency

Charu Chaudhry

Version 1 posted 26 November 2021

1,594

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3

Citations

Biological and Medicinal Chemistry

Working Paper

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity

Satomi Imaide, Kristin M. Riching, Nikolai Makukhin, Vesna Vetma, Claire Whitworth, Scott J. Hughes, Nicole Trainor, Sarah D. Mahan, Nancy Murphy, Angus Cowan, Kwok-Ho Chan, Conner Craigon, Andrea Testa, Chiara Maniaci, Marjeta Urh, Danette L. Daniels, Alessio Ciulli

Version 2 posted 20 October 2021

4,430

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Biological and Medicinal Chemistry

Working Paper

Lysosome Targeting Chimeras (LYTACs) That Engage a Liver-Specific Asialoglycoprotein Receptor for Targeted Protein Degradation

Green Ahn, Steven Banik, Caitlyn L. Miller, Nicholas Riley, Jennifer R. Cochran, Carolyn Bertozzi

Version 1 posted 30 July 2020

3,380

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5

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Biological and Medicinal Chemistry

Working Paper

PDTAC: Targeted photodegradation of GPX4 triggers Ferroptosis and potent antitumor immunity

Sijin Liu, Xi Zhao, Sufang Shui, Biao Wang, Yingxian Cui, Tairan Yuwen, Suwei Dong, Guoquan Liu

Version 1 posted 31 May 2022

424

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Biological and Medicinal Chemistry

Working Paper

Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable and Blood Brain Barrier Penetrant Prote-olysis Targeting Chimera Degrader of Leucine Rich Repeat Kinase 2

Xingui Liu, Alexia Kalogeropulou, Sofia Domingos, Nikolai Makukhin, Raja Nirujogi, Francois Singh, Natalia Shpiro, Anton Saalfrank, Esther Sammler, Ian Ganley, Rui Moreira, Dario Alessi, Alessio Ciulli

Version 2 posted 13 July 2022

4,328

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1

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Analytical Chemistry

Working Paper

Proximity Biosensor Assay for PROTAC Ternary Complex Analysis

Irene Ponzo, Alice Solda, Charlotte Crowe, Goran Dahl, Stefan Geschwindner, Alessio Ciulli, Ulrich Rant

Version 1 posted 06 March 2024

1,299

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Biological and Medicinal Chemistry

Review

Molecular glues: The adhesive connecting targeted protein degradation to the clinic

Janet M. Sasso, Rumiana Tenchov, DaSheng Wang, Linda S. Johnson, Xinmei Wang, Qiongqiong Angela Zhou

Version 1 posted 16 June 2022

4,015

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Theoretical and Computational Chemistry

Working Paper

Lenalidomide stabilizes protein-protein complexes by turning labile intermolecular H-bonds into robust interactions

Marina Miñarro-Lleonar, Andrea Bertran-Mostazo, Jorge Duro, Xavier Barril, Jordi Juárez-Jiménez

Version 2 posted 07 October 2022

313

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Refine Search

25 results in Targeted Protein Degradation in Keywords: Targeted Protein Degradation

From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9

Targeted Protein Degradation via a Covalent Reversible Degrader Based on Bardoxolone

A Mathematical Model for Covalent Proteolysis Targeting Chimeras: Thermodynamics and Kinetics underlying Catalytic Efficiency

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity

Lysosome Targeting Chimeras (LYTACs) That Engage a Liver-Specific Asialoglycoprotein Receptor for Targeted Protein Degradation

PDTAC: Targeted photodegradation of GPX4 triggers Ferroptosis and potent antitumor immunity

Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable and Blood Brain Barrier Penetrant Prote-olysis Targeting Chimera Degrader of Leucine Rich Repeat Kinase 2

Proximity Biosensor Assay for PROTAC Ternary Complex Analysis

Molecular glues: The adhesive connecting targeted protein degradation to the clinic

Lenalidomide stabilizes protein-protein complexes by turning labile intermolecular H-bonds into robust interactions

25 results in Keywords: Targeted Protein Degradation