Results 11 to 20 of about 714,957 (298)

Gluing Proteins for Targeted Degradation [PDF]

Cancer Cell, 2021
Targeted protein degradation is an emerging technology for drug development. An article published in Nature reported a novel mechanism of targeted protein degradation triggered by small-molecule-induced polymerization of the oncogenic transcription factor BCL6.
Mikihiko, Naito, Shigeo, Murata
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Targeting proteins for degradation [PDF]

Nature Chemical Biology, 2009
Protein degradation plays a central role in many cellular functions. Misfolded and damaged proteins are removed from the cell to avoid toxicity. The concentrations of regulatory proteins are adjusted by degradation at the appropriate time. Both foreign and native proteins are digested into small peptides as part of the adaptive immune response.
Erin K, Schrader, Kristine G, Harstad, Andreas, Matouschek   +2 more
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A TRIM21-based method for targeted protein degradation [PDF]

Acta Biochimica et Biophysica Sinica
Hu Weikang, Qiu Xiang, Yang Yun, Wu Yaoyao, Wang Chengcheng, Hu Ronggui, Li Chuanyin   +6 more
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Proteolysis-Targeting Chimeras (PROTACs) in Cancer Therapy: Present and Future

Molecules, 2022
The PROteolysis TArgeting Chimeras (PROTACs) is an innovative technique for the selective degradation of target proteins via the ubiquitin–proteasome system.
Rui Li, Miao Liu, Zhenya Yang, Jiao Li, Yuxin Gao, Ruirong Tan   +5 more
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Chemical-Mediated Targeted Protein Degradation in Neurodegenerative Diseases

Life, 2021
Neurodegenerative diseases, including Alzheimer’s disease, Huntington’s disease, and Parkinson’s disease, are a class of diseases that lead to dysfunction of cognition and mobility.
Soonsil Hyun, Dongyun Shin
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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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Modular Assembled Targeting Chimera Enables Multimodal Targeted Protein Degradation [PDF]

JACS Au
Wentao Zhu, Wenqian Zhang, Yinmiao Wang, Jian Chen, Fang Xu, Jiyan Pang   +5 more
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Erioflorin stabilizes the tumor suppressor Pdcd4 by inhibiting its interaction with the E3-ligase β-TrCP1 [PDF]

, 2012
Loss of the tumor suppressor Pdcd4 was reported for various tumor entities and proposed as a prognostic marker in tumorigenesis. We previously characterized decreased Pdcd4 protein stability in response to mitogenic stimuli, which resulted from p70S6K1 ...
Bajer, Magdalena M., Blees, Johanna, Bokesch, Heidi R., Brüne, Bernhard, Colburn, Nancy H., Gustafson, Kirk R., Henrich, Curtis J., McMahon, James B., Milke, Larissa, Rübsamen, Daniela, Schmid, Tobias, Schulz, Kathrin   +11 more
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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, Ming Cai, Liang Shao, Jihong Zhang   +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, Jia Zhao, Kunhong Zhong, Aiping Tong, Da Jia   +4 more
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