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Biological and Medicinal Chemistry

Working Paper

Cereblon versus VHL: Hijacking E3 Ligases Against Each Other Using PROTACs

Miriam Girardini, Chiara Maniaci, Scott J. Hughes, Andrea Testa, Alessio Ciulli

Version 2 posted 19 February 2019

1,755

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Biological and Medicinal Chemistry

Working Paper

Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer

Hidetomo Yokoo, Norihito Shibata, Miyako Naganuma, Kiyonaga Fujii, Takahito Ito, Kosuke Aritake, Mikihiko Naito, Yosuke Demizu

Version 1 posted 05 October 2020

533

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Biological and Medicinal Chemistry

Working Paper

Efficient targeted degradation via reversible and irreversible covalent PROTACs

Ronen Gabizon, Amit Shraga, Paul Gehrtz, Ella Livnah, Yamit Shorer, Neta Gurwicz, Liat Avram, Tamar Unger, Hila Aharoni, Shira Albeck, Alexander Brandis, Ziv Shulman, Ben- Zion Katz, Yair Herishanu, Nir London

Version 2 posted 17 March 2020

2,500

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Biological and Medicinal Chemistry

Working Paper

Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs

Christian Steinebach, Izidor Sosič, Aleša Bricelj, Arunima Murgai, Luca Bischof, Yuen Lam Dora Ng, Christopher Heim, Samuel Maiwald, Matic Proj, Rabea Voget, Felix Feller, Janez Košmrlj, Annika Schmidt, Patricia Lemnitzer, Finn K. Hansen, Michael Gütschow, Jan Krönke, Marcus D. Hartmann

Version 1 posted 21 April 2023

1,637

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1

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Biological and Medicinal Chemistry

Working Paper

Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity

Victoria Klein, Adam Bond, Conner Craigon, R. Scott Lokey, Alessio Ciulli

Version 1 posted 05 July 2021

2,282

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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

4,472

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1

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Biological and Medicinal Chemistry

Working Paper

PROTAC degraders of the METTL3-14 m6A-RNA methyltransferase

Francesco Errani, Annalisa Invernizzi, Marcin Herok, Elena Bochenkova, Fiona Stamm, Ivan Corbeski, Valeria Romanucci, Giovanni Di Fabio, František Zálešák, Amedeo Caflisch

Version 2 posted 06 February 2024

760

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Biological and Medicinal Chemistry

Working Paper

Leveraging dual-ligase recruitment to enhance degradation via a heterotrivalent PROTAC

Adam G. Bond, Miquel Muñoz i Ordoño, Celia M. Bisbach, Conner Craigon, Nikolai Makukhin, Elizabeth A. Caine, Manjula Nagala, Marjeta Urh, Georg E. Winter, Kristin M. Riching, Alessio Ciulli

Version 1 posted 21 August 2024

2,263

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Biological and Medicinal Chemistry

Working Paper

Hijacking the MDM2 E3 Ligase with novel BRD4-Targeting PROTACs in Pancreatic Cancer Cells

Mihaela Ficu, Dan Niculescu-Duvaz, Mohammed Aljarah, Christopher S. Kershaw, Caroline J. Springer

Version 1 posted 09 August 2024

360

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Biological and Medicinal Chemistry

Working Paper

A Reliable and Sustainable Multicomponent Access to Protein Degraders

Irene Preet Bhela, Alice Ranza, Marta Serafini, Tracey PIRALI

Version 2 posted 25 October 2021

1,636

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20 results in Protacs in Keywords: Protacs

Cereblon versus VHL: Hijacking E3 Ligases Against Each Other Using PROTACs

Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer

Efficient targeted degradation via reversible and irreversible covalent PROTACs

Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs

Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity

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

PROTAC degraders of the METTL3-14 m6A-RNA methyltransferase

Leveraging dual-ligase recruitment to enhance degradation via a heterotrivalent PROTAC

Hijacking the MDM2 E3 Ligase with novel BRD4-Targeting PROTACs in Pancreatic Cancer Cells

A Reliable and Sustainable Multicomponent Access to Protein Degraders

20 results in Keywords: Protacs