DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance

Autor: Martin Schröder, Martin Renatus, Xiaoyou Liang, Fabian Meili, Thomas Zoller, Sandrine Ferrand, Francois Gauter, Xiaoyan Li, Frederic Sigoillot, Scott Gleim, Therese-Marie Stachyra, Jason R. Thomas, Damien Begue, Maryam Khoshouei, Peggy Lefeuvre, Rita Andraos-Rey, BoYee Chung, Renate Ma, Benika Pinch, Andreas Hofmann, Markus Schirle, Niko Schmiedeberg, Patricia Imbach, Delphine Gorses, Keith Calkins, Beatrice Bauer-Probst, Magdalena Maschlej, Matt Niederst, Rob Maher, Martin Henault, John Alford, Erik Ahrne, Luca Tordella, Greg Hollingworth, Nicolas H. Thomä, Anna Vulpetti, Thomas Radimerski, Philipp Holzer, Seth Carbonneau, Claudio R. Thoma

Publikováno v: Nature Communications, Vol 15, Iss 1, Pp 1-19 (2024)

Abstract Targeted protein degradation (TPD) mediates protein level through small molecule induced redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal degradation. TPD has recently emerged as a key modality in drug d

Externí odkaz: https://doaj.org/article/8f2eff537f564b01931321a688bb396a

Reinstating targeted protein degradation with DCAF1 PROTACs in CRBN PROTAC resistant settings

Autor: Martin Schröder, Martin Renatus, Xiaoyou Liang, Fabian Meili, Thomas Zoller, Sandrine Ferrand, Francois Gauter, Xiaoyan Li, Fred Sigoillot, Scott Gleim, Marie-Therese Stachyra, Jason Thomas, Damien Begue, Peggy Lefeuvre, Rita Andraos-Rey, BoYee Chung, Renate Ma, Seth Carbonneau, Benika Pinch, Andreas Hofmann, Markus Schirle, Niko Schmiedberg, Patricia Imbach, Delphine Gorses, Keith Calkins, Bea Bauer-Probst, Magdalena Maschlej, Matt Niederst, Rob Maher, Martin Henault, John Alford, Erik Ahrne, Greg Hollingworth, Nicolas H. Thomä, Anna Vulpetti, Thomas Radimerski, Philipp Holzer, Claudio R. Thoma

Targeted protein degradation (TPD) of neo-substrates with proteolysis targeting chimeras (PROTACs) or molecular glues has emerged as a key modality in exploring new biology as well as designing new drug candidates where catalytic inhibition is neithe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b962ac1012caadf747a15217539d973e
https://doi.org/10.1101/2023.04.09.536153

Author Correction: DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance.

Autor: Schröder, Martin, Renatus, Martin, Liang, Xiaoyou, Meili, Fabian, Zoller, Thomas, Ferrand, Sandrine, Gauter, Francois, Li, Xiaoyan, Sigoillot, Frederic, Gleim, Scott, Stachyra, Therese-Marie, Thomas, Jason R., Begue, Damien, Khoshouei, Maryam, Lefeuvre, Peggy, Andraos-Rey, Rita, Chung, BoYee, Ma, Renate, Pinch, Benika, Hofmann, Andreas

Publikováno v: Nature Communications; 8/19/2024, Vol. 15 Issue 1, p1-5, 5p

A proteomic study of myeloproliferative neoplasms using reverse-phase protein arrays.

Autor: Tognon, Raquel^1,2 (AUTHOR), Almeida-e-Silva, Danillo C.³ (AUTHOR), Andraos-Rey, Rita⁴ (AUTHOR), Ristov, Mitko⁴ (AUTHOR), Ambrósio, Luciana¹ (AUTHOR), de Almeida, Felipe Campos¹ (AUTHOR), de Souza Nunes, Natália¹ (AUTHOR), Xisto Souto, Elizabeth⁵ (AUTHOR), de Lourdes Perobelli, Leila⁵ (AUTHOR), Simões, Belinda Pinto⁶ (AUTHOR), Alexander Guthy, Daniel⁴ (AUTHOR), Radimerski, Thomas⁴ (AUTHOR), Attié de Castro, Fabíola¹ (AUTHOR)

Publikováno v: Leukemia & Lymphoma. Dec2020, Vol. 61 Issue 13, p3052-3065. 14p.

A conditional inducible JAK2V617F transgenic mouse model reveals myeloproliferative disease that is reversible upon switching off transgene expression.

Autor: Chapeau EA; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Mandon E; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Gill J; Friedrich Miescher Institute for Biomedical Research, Basel, Switzerland., Romanet V; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Ebel N; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Powajbo V; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Andraos-Rey R; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Qian Z; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Kininis M; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Zumstein-Mecker S; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Ito M; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Hynes NE; Friedrich Miescher Institute for Biomedical Research, Basel, Switzerland., Tiedt R; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Hofmann F; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Eshkind L; Institute for Translational Immunology and Research Center for Immunotherapy, University Medical Center, Johannes Gutenberg University, Mainz, Germany., Bockamp E; Institute for Translational Immunology and Research Center for Immunotherapy, University Medical Center, Johannes Gutenberg University, Mainz, Germany., Kinzel B; Chemical Biology and Therapeutics, Novartis Institutes for BioMedical Research, Basel, Switzerland., Mueller M; Chemical Biology and Therapeutics, Novartis Institutes for BioMedical Research, Basel, Switzerland., Murakami M; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Baffert F; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland., Radimerski T; Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland.

Publikováno v: PloS one [PLoS One] 2019 Oct 10; Vol. 14 (10), pp. e0221635. Date of Electronic Publication: 2019 Oct 10 (Print Publication: 2019).