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Light-Activatable Photochemically Targeting Chimeras (PHOTACs) Enable the Optical Control of Targeted Protein Degradation of HDAC6

Silas Wurnig, Maria Hanl, Thomas Geiger, Shiyang Zhai, Ina Dressel, Dominika Pieńkowska, Radosław Nowak, Finn Kristian Hansen

Version 1 posted 09 December 2024

268

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Biological and Medicinal Chemistry

Working Paper

Heterobifunctional Molecules Induce Dephosphorylation of Kinases - a Proof of Concept Study

Sayumi Yamazoe, Steve Staben

Version 1 posted 31 July 2019

1,188

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Biological and Medicinal Chemistry

Working Paper

HaloTag-Targeted Sirtuin Rearranging Ligand (SirReal) for the Development of Proteolysis Targeting Chimeras (PROTACs) Against the Lysine Deacetylase Sirtuin 2 (Sirt2)

Matthias Schiedel, Attila Lehotzky, Sándor Szunyogh, Judit Oláh, Sören Hammelmann, Nathalie Wössner, Dina Robaa, Oliver Einsle, Wolfgang Sippl, Judit Ovádi, Manfred Jung

Version 1 posted 27 May 2020

556

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Biological and Medicinal Chemistry

Working Paper

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

1,094

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Biological and Medicinal Chemistry

Working Paper

Targeted Degradation of Oncogenic KRASG12C by VHL-recruiting PROTACs

Michael J. Bond, Ling Chu, Dhanusha A. Nalawansha, Ke Li, Craig Crews

Version 1 posted 10 April 2020

3,736

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Biological and Medicinal Chemistry

Working Paper

A Caged E3 Ligase Ligand for PROTAC-Mediated Protein Degradation with Light

Cyrille Kounde, Maria M. Shchepinova, Edward Tate

Version 2 posted 23 December 2019

1,238

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Biological and Medicinal Chemistry

Working Paper

Rational Design and Synthesis of Novel Dual Protacs for Simultaneous Degradation of EGFR and PARP

Mengzhu Zheng, Junfeng Huo, Xiaoxia Gu, Canrong Wu, Qingzhe Zhang, Wang Wang, Yang Liu, Yu Liu, Xuechen Zhou, Lixia Chen, Yirong Zhou, Hua Li

Version 1 posted 18 February 2021

971

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Biological and Medicinal Chemistry

Working Paper

From Inhibition to Degradation: Targeting the Anti-apoptotic Protein Myeloid Cell Leukemia 1(MCL1)

James Papatzimas, Evgueni Gorobets, Ranjan Maity, Mir Ishruna Muniyat, Justin L. MacCallum, Paola Neri, Nizar J. Bahlis, Darren Derksen

Version 1 posted 15 February 2019

1,451

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1

Citations

Biological and Medicinal Chemistry

Working Paper

A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo

Christiane Kofink, Nicole Trainor, Barbara Mair, Simon Wöhrle, Melanie Wurm, Nikolai Mischerikow, Gerd Bader, Klaus Rumpel, Thomas Gerstberger, Yunhai Cui, Peter Greb, Geraldine Garavel, Maximilian Scharnweber, Julian Fuchs, Gabriela Gremel, Paolo Chette, Stefan Hopf, Nicole Budano, Jörg Rinnenthal, Gerhard Gmaschitz, Emelyne Diers, Ross McLennan, Michael Roy, Claire Whitworth, Vesna Vetma, Moriz Mayer, Manfred Koegl, Alessio Ciulli, Harald Weinstabl, William Farnaby

Version 1 posted 01 February 2022

6,037

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4

Citations

Biological and Medicinal Chemistry

Working Paper

Self-Assembly of Proteolysis Targeting Chimeras Via Reversible Bioorthogonal Reactions

Weijun Gui, Sarah Giardina, Madeline Balzarini, Francis Barany, Thomas Kodadek

Version 1 posted 15 September 2022

1,791

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49 results in protac in Keywords: protac

Light-Activatable Photochemically Targeting Chimeras (PHOTACs) Enable the Optical Control of Targeted Protein Degradation of HDAC6

Heterobifunctional Molecules Induce Dephosphorylation of Kinases - a Proof of Concept Study

HaloTag-Targeted Sirtuin Rearranging Ligand (SirReal) for the Development of Proteolysis Targeting Chimeras (PROTACs) Against the Lysine Deacetylase Sirtuin 2 (Sirt2)

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

Targeted Degradation of Oncogenic KRASG12C by VHL-recruiting PROTACs

A Caged E3 Ligase Ligand for PROTAC-Mediated Protein Degradation with Light

Rational Design and Synthesis of Novel Dual Protacs for Simultaneous Degradation of EGFR and PARP

From Inhibition to Degradation: Targeting the Anti-apoptotic Protein Myeloid Cell Leukemia 1(MCL1)

A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo

Self-Assembly of Proteolysis Targeting Chimeras Via Reversible Bioorthogonal Reactions

49 results in Keywords: protac