Results 51 to 60 of about 827,025 (271)

Proteolysis targeting chimeras (PROTACs) for epigenetics research

Current Opinion in Chemical Biology, 2020
Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules and allow selective protein degradation by addressing the natural ubiquitin proteasome system. As this new strategy of chemically induced protein degradation can serve as a biological tool and provides new possibilities for drug discovery, it has been applied to a variety of ...
Anja Vogelmann, Dina Robaa, Wolfgang Sippl, Manfred Jung   +3 more
openaire   +3 more sources

Proteolysis Targeting Chimera (PROTAC) for Macrophage Migration Inhibitory Factor (MIF) Has Anti‐Proliferative Activity in Lung Cancer Cells [PDF]

, 2021
Macrophage migration inhibitory factor (MIF) is involved in protein-protein interactions that play key roles in inflammation and cancer. Current strategies to develop small molecule modulators of MIF functions are mainly restricted to the MIF tautomerase
Shanshan Song, Wim J. Quax, Poelarends, Gerrit; id_orcid, Xiao, Zhangping, Melgert, Barbro, Gerrit J. Poelarends, Barbro N. Melgert, van der Wouden, Petra, Zhangping Xiao, Chen, Deng; id_orcid, Dekker, Frank Jacobus; id_orcid, Song, Shanshan, Xiao, Zhangping; id_orcid, Melgert, Barbro; id_orcid, Quax, Wim, Poelarends, Gerrit, Deng Chen, Petra E. van der Wouden, Frank J. Dekker, van Merkerk, Ronald, Quax, Wim; id_orcid, Cool, Robbert, Robbert H. Cool, Dekker, Frank Jacobus, Ronald van Merkerk, Chen, Deng   +25 more
core   +2 more sources

Targeted degradation of LRG1 to attenuate renal fibrosis

Asian Journal of Pharmaceutical Sciences
Leucine-rich α-2 glycoprotein 1 (LRG1), a secreted glycoprotein, has been identified as significantly upregulated in renal fibrosis, potentially exacerbating the condition by enhancing TGF-β-Smad3-dependent signaling pathways.
Linyao Fan, Yingqiu Qi, Xi Yang, Yarui Xu, Yana Zhang, Longdi Wang, Anying Zhu, Lirong Zhang, Jian Song, Shengnan Du, Guangjun Nie, Huan Min   +11 more
doaj   +1 more source

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery [PDF]

Cell, 2020
New biological tools provide new techniques to probe fundamental biological processes. Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which are capable of modulating protein concentrations at a post-translational level by co-opting the ubiquitin-proteasome system. We describe the PROTAC technology and its application
George M, Burslem, Craig M, Crews
openaire   +2 more sources

Recent advances in the molecular design and applications of proteolysis targeting chimera-based multi-specific antiviral modality [PDF]

, 2023
Viral infections represent a major threat to human health and the global economy; however, most of the currently available antiviral drugs are not fully effective in restricting viral replication and selecting for drug-resistant variants.
Shujing Xu, Xinyong Liu, Luis Menéndez-Arias, Yang Zhou, Nerea López-Carrobles, Peng Zhan, Dang Ding   +6 more
core   +1 more source

Leveraging Dual-Ligase Recruitment to Enhance Protein Degradation via a Heterotrivalent Proteolysis Targeting Chimera. [PDF]

J Am Chem Soc
Proteolysis targeting chimera (PROTAC) degraders are typically bifunctional with one E3 ligase ligand connected to one target protein ligand via a linker.
Bond AG, Muñoz I Ordoño M, Bisbach CM, Craigon C, Makukhin N, Caine EA, Nagala M, Urh M, Winter GE, Riching KM, Ciulli A.   +10 more
europepmc   +2 more sources

Targeting Protein Kinases Degradation by PROTACs

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.
Fei Yu, Ming Cai, Liang Shao, Jihong Zhang   +3 more
doaj   +1 more source

Nucleic Acid-driven Protein Degradation: Frontiers of Lysosomal Targeted Degradation Technology

Shengwu huaxue yu shengwu wuli jinzhan
Distinct from the complementary inhibition mechanism through binding to the target with three-dimensional conformation of small molecule inhibitors, targeted protein degradation technology takes tremendous advantage of endogenous protein degradation ...
YIN Han, LI Yu, FAN Yu-Chuan, GUO Shuai, HUANG Yuan-Yu, LI Yong, WENG Yu-Hua   +6 more
doaj   +1 more source

Engineering peptides into antibodies—opportunities and strategies for therapeutic innovation

FEBS Letters, EarlyView.
Peptides and antibodies occupy complementary therapeutic niches. Peptides recognize difficult targets in a compact format, while antibodies add specificity, long half‐life, and effector functions. This review examines strategies that merge both modalities—peptide grafting into loops, terminal and Fc fusions, and bioconjugation—highlighting how ...
Jinling Wang, Ruslana Romaniuk, Hristo L. Svilenov   +2 more
wiley   +1 more source

The ubiquitin system in normal and infected germinal center B cells

FEBS Letters, EarlyView.
The ubiquitin system plays a central role in germinal center (GC) B cells, influencing differentiation to long‐lived memory B cells. Oncogenic gammaherpesviruses gain access to memory B cells by establishing latency in GC B cells. Mapping ubiquitin mechanisms in normal and infected GC B cells will define specific molecular circuits in B cells germane ...
Destiny Davis, Lesly Mejia, Emily K Moser   +2 more
wiley   +1 more source