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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

Development of Triantennary N-Acetylgalactosamine Conjugates as Degraders for Extracellular Proteins

Yaxian Zhou, peng teng, Weiping Tang

Version 1 posted 19 August 2020

790

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Biological and Medicinal Chemistry

Working Paper

PHOTACs Enable Optical Control of Protein Degradation

Martin Reynders, Bryan Matsuura, Marleen Bérouti, Daniele Simoneschi, Antonio Marzio, Michele Pagano, Dirk Trauner

Version 2 posted 31 May 2019

3,270

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5

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Organic Chemistry

Working Paper

Bifunctional Small Molecules That Mediate the Degradation of Extracellular Proteins

David Caianiello, Mengwen Zhang, Jason Ray, Jake Swartzel, Emily Branham, Egor Chirkin, Venkata Sabbasani, Angela Gong, David Mcdonald, Viswanathan Muthusamy, David Spiegel

Version 2 posted 04 August 2020

2,447

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1

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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

3,382

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5

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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

2,781

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2

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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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Biological and Medicinal Chemistry

Working Paper

Lysosome Targeting Chimeras (LYTACs) for the Degradation of Secreted and Membrane Proteins

Steven Banik, Kayvon Pedram, Simon Wisnovsky, Nicholas Riley, Carolyn Bertozzi

Version 2 posted 20 November 2019

11,381

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5

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Theoretical and Computational Chemistry

Working Paper

In Silico Modeling and Scoring of PROTAC-Mediated Ternary Complex Poses

Junzhuo Liao, Xueqing Nie, Ilona Unarta, Spencer Ericksen, Weiping Tang

Version 3 posted 20 December 2021

1,909

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Biological and Medicinal Chemistry

Working Paper

Selection of DNA-encoded Chemical Libraries for Compounds that can Induce Protein Ubiquitination

Cen Huang, Xingyuan Liu, Xinyuan Wu, Ling Meng, Xiaojie Lu, Xiaoyu Li

Version 1 posted 12 February 2024

782

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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

Development of Triantennary N-Acetylgalactosamine Conjugates as Degraders for Extracellular Proteins

PHOTACs Enable Optical Control of Protein Degradation

Bifunctional Small Molecules That Mediate the Degradation of Extracellular Proteins

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

Targeted Protein Degradation via a Covalent Reversible Degrader Based on Bardoxolone

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

Lysosome Targeting Chimeras (LYTACs) for the Degradation of Secreted and Membrane Proteins

In Silico Modeling and Scoring of PROTAC-Mediated Ternary Complex Poses

Selection of DNA-encoded Chemical Libraries for Compounds that can Induce Protein Ubiquitination

25 results in Keywords: Targeted protein degradation