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Design principles for optogenetic-based targeted protein degradation [PDF]

Synthetic and Systems Biotechnology
Precise regulation of protein abundance is essential for understanding dynamic cellular processes and for advancing therapeutic development. However, existing approaches lack the spatiotemporal resolution required to these cellular processes.
Yunyue Chen, Siyifei Wang, Leiying Xie, Luhao Zhang, Min Zhu, Yingke Xu   +5 more
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De novo designed protein guiding targeted protein degradation [PDF]

Nature Communications
Targeted protein degradation is a powerful tool for biological research, cell therapy, and synthetic biology. However, conventional methods often depend on pre-fused degrons or chemical degraders, limiting their wider applications.
Zhendong Li, Gan Qiao, Xianghe Wang, Ming Wang, Jinyu Cheng, Guipeng Hu, Xiaomin Li, Jing Wu, Jia Liu, Cong Gao, Liming Liu   +10 more
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Targeted protein degradation: species, diseases and efficient utilization [PDF]

Journal of Translational Medicine
Background Targeted protein degradation (TPD) is a novel protein modulation strategy distinct from traditional inhibitors. Its core mechanism involves labeling proteins of interest to initiate endogenous protein clearance pathways, mainly including the ...
Tian Yue, Jian He, Jun Hou
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Targeted protein degradation in Escherichia coli using CLIPPERs [PDF]

EMBO Reports
New, universal tools for targeted protein degradation in bacteria can help to accelerate protein function studies and antimicrobial research. We describe a new method for degrading bacterial proteins using plasmid-encoded degrader peptides which deliver ...
Matylda Anna Izert-Nowakowska, Maria Magdalena Klimecka, Anna Antosiewicz, Karol Wróblewski, Jakub Józef Kowalski, Katarzyna Justyna Bandyra, Tomasz Góral, Sebastian Kmiecik, Remigiusz Adam Serwa, Maria Wiktoria Górna   +9 more
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Cellular parameters shaping pathways of targeted protein degradation [PDF]

Communications Biology
In recent years the development of proteolysis-targeting chimeras (PROTACs) has enhanced the field of ubiquitin signalling through advancing therapeutic targeted protein degradation (TPD) strategies and generating tools to explore the ubiquitin landscape.
Annabel Cardno, Bryony Kennedy, Catherine Lindon   +2 more
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Targeted protein degradation with small molecules for cancer immunotherapy [PDF]

Asian Journal of Pharmaceutical Sciences
Immunotherapy has transformed cancer treatment, marked by the approval of numerous antibody-based drugs. However, the limitations of antibodies in pharmacokinetics including long half-lives, limited oral bioavailability and immunogenicity, have prompted ...
Zichao Yang, Jianwei Xu, Xixiang Yang, Jianjun Chen   +3 more
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From PROTAC to TPD: Advances and Opportunities in Targeted Protein Degradation

Pharmaceuticals
PROTAC is a rapidly developing engineering technology for targeted protein degradation using the ubiquitin–proteasome system, which has promising applications for inflammatory diseases, neurodegenerative diseases, and malignant tumors. This paper gives a
Siqi Wang, Fuchu He, Chunyan Tian, Aihua Sun   +3 more
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Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2

Nature Communications, 2023
The Src homology 2 (SH2) domain recognizes phosphotyrosine (pY) post translational modifications in partner proteins to trigger downstream signaling. Drug discovery efforts targeting the SH2 domains have long been stymied by the poor drug-like properties
Sarath Ramachandran, Nikolai Makukhin, Kevin Haubrich, Manjula Nagala, Beth Forrester, Dylan M. Lynch, Ryan Casement, Andrea Testa, Elvira Bruno, Rosaria Gitto, Alessio Ciulli   +10 more
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A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo

Nature Communications, 2022
Protein degraders are an emerging drug modality; however, their properties lie beyond typical drug-like space. Here the authors report optimisation via structure-based exit vector and linker design towards the VHL-recruiting PROTAC ACBI2, an orally ...
Christiane Kofink, Nicole Trainor, Barbara Mair, Simon Wöhrle, Melanie Wurm, Nikolai Mischerikow, Michael J. Roy, Gerd Bader, Peter Greb, Géraldine Garavel, Emelyne Diers, Ross McLennan, Claire Whitworth, Vesna Vetma, Klaus Rumpel, Maximilian Scharnweber, Julian E. Fuchs, Thomas Gerstberger, Yunhai Cui, Gabriela Gremel, Paolo Chetta, Stefan Hopf, Nicole Budano, Joerg Rinnenthal, Gerhard Gmaschitz, Moriz Mayer, Manfred Koegl, Alessio Ciulli, Harald Weinstabl, William Farnaby   +29 more
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Systems-Wide Dissection of Organic Acid Assimilation in Pseudomonas aeruginosa Reveals a Novel Path To Underground Metabolism

mBio, 2022
The human pathogen Pseudomonas aeruginosa (Pa) is one of the most frequent and severe causes of nosocomial infection. This organism is also a major cause of airway infections in people with cystic fibrosis (CF). Pa is known to have a remarkable metabolic
Stephen K. Dolan, Andre Wijaya, Michael Kohlstedt, Lars Gläser, Paul Brear, Rafael Silva-Rocha, Christoph Wittmann, Martin Welch   +7 more
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