Results 21 to 30 of about 419,478 (257)
Targeting Protein Kinases Degradation by PROTACs [PDF]
Frontiers in Chemistry, 2021 Kinase dysregulation is greatly associated with cell proliferation, migration and survival, indicating the importance of kinases as therapeutic targets for anticancer drug development. However, traditional kinase inhibitors binding to catalytic or allosteric sites are associated with significant challenges.
Fei Yu +3 more
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Targeted protein degradation: mechanisms, strategies and application
Signal Transduction and Targeted Therapy, 2022 Traditional drug discovery mainly focuses on direct regulation of protein activity. The development and application of protein activity modulators, particularly inhibitors, has been the mainstream in drug development.
Lin Zhao +4 more
doaj +1 more source
Central Nervous System Targeted Protein Degraders
Biomolecules, 2023 Diseases of the central nervous system, which once occupied a large component of the pharmaceutical industry research and development portfolio, have for many years played a smaller part in major pharma pipelines—primarily due to the well cited challenges in target validation, valid translational models, and clinical trial design.
Bedwyr ab Ion Thomas +3 more
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Targeting DUBs to degrade oncogenic proteins [PDF]
British Journal of Cancer, 2020 Targeted protein degradation has emerged as a strategy in cancer therapy. Yang et al. discovered that HBX19818, an inhibitor of the deubiquitinase (DUB) USP10, leads to the dual degradation of spleen tyrosine kinase (SYK) and FLT3, resulting in death of AML cells.
Cremer, Anjali, Stegmaier, Kimberly
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Targeted Protein Degradation through E2 Recruitment
ACS Chemical Biology, 2022 AbstractTargeted protein degradation (TPD) with Proteolysis Targeting Chimeras (PROTACs), heterobifunctional compounds consisting of protein targeting ligands linked to recruiters of E3 ubiquitin ligases, has arisen as a powerful therapeutic modality to induce the proximity of target proteins with E3 ligases to ubiquitinate and degrade specific ...
Nafsika Forte +6 more
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PROTAC’ing oncoproteins: targeted protein degradation for cancer therapy
Molecular Cancer, 2023 Molecularly targeted cancer therapies substantially improve patient outcomes, although the durability of their effectiveness can be limited. Resistance to these therapies is often related to adaptive changes in the target oncoprotein which reduce binding
Jeremy M. Kelm +6 more
doaj +1 more source
N-Terminal-Based Targeted, Inducible Protein Degradation in Escherichia coli. [PDF]
PLoS ONE, 2016 Dynamically altering protein concentration is a central activity in synthetic biology. While many tools are available to modulate protein concentration by altering protein synthesis rate, methods for decreasing protein concentration by inactivation or ...
Karthik Sekar +3 more
doaj +1 more source
Targeted Protein Degradation Tools: Overview and Future Perspectives
Biology, 2020 Targeted protein inactivation (TPI) is an elegant approach to investigate protein function and its role in the cellular landscape, overcoming limitations of genetic perturbation strategies.
Yuri Prozzillo +6 more
doaj +1 more source
Protein-Targeted Degradation Agents Based on Natural Products
Pharmaceuticals, 2022 Natural products are an important source of drug lead compounds, and natural products with significant biological activity are constantly being discovered and used in clinical practice.
Yan Li +4 more
doaj +1 more source
Targeted Protein Degradation for Agricultural Applications: Rationale, Challenges, and Outlook [PDF]
ACS Bio & Med Chem AuDenis Fourches +4 more
doaj +2 more sources