Results 81 to 90 of about 14,786 (290)

Nanotherapies for Atherosclerosis: Targeting, Catalysis, and Energy Transduction

Advanced Healthcare Materials, EarlyView.
Atherosclerosis management is hindered by poor drug targeting and plaque heterogeneity. Nanotechnology overcomes these barriers via three core strategies: (1) target‐engineered nanocarriers that achieve lesion‐specific precision via ligand modification, biomimetic camouflage, stimuli‐responsive release, and self‐propelling nanomotors; (2) catalytic ...
Yuqi Yang, Jingguo Qu, Tonghuan Xiao, Xinyang Han, Michael Tin‐Cheung Ying   +4 more
wiley   +1 more source

Towards the targeted protein degradation of CK2: design and synthesis of CAM4066-based PROTACs

Beilstein Journal of Organic Chemistry
Human protein kinase CK2 is a constitutively active serine/threonine kinase implicated in numerous cancers. Although ATP-competitive inhibitors such as CX-4945 show therapeutic potential, they are limited by off-target effects and incomplete or transient
Sophie Day-Riley, Sona Krajcovicova, Aryaman Raj Sokhal, Jan L. Venne, Paul Brear, Marko Hyvönen, Benjamin C. Whitehurst, Jason S. Carroll, David R. Spring   +8 more
doaj   +1 more source

Structure-guided design of peptides as tools to probe the protein-protein interaction between Cullin-2 and Elongin BC substrate adaptor in Cullin RING E3 ubiquitin ligases [PDF]

, 2017
Cullin RING E3 ubiquitin ligases (CRLs) are large dynamic multi-subunit complexes that control the fate of many proteins in cells. CRLs constitute attractive drug targets for the development of small-molecule inhibitors and chemical inducers of protein ...
Arkin, Arkin, Bulatov, Cardote, Cardote, Chan, Chen, Chen, Chène, Cromm, Dias, Fischer, Frost, Gadd, Galdeano, Knauth, Lai, Morreale, Nevola, Nguyen, Petroski, Rebollo, Scott, Van Molle, Vranken, Williamson   +25 more
core   +2 more sources

Natural Products Inspired Scaffold Diversification Leads to Unnatural Molecular Warhead and Covalent Strategy to Modulating Protein Function through Electrophilic Bromine Transfer

Advanced Science, EarlyView.
We report a new thiolate‐reactive α,α‐gem‐dibromo lactam warhead that activates transcription factor Nrf2 and demonstrates anti‐inflammatory activities, which have implications in cancer, neurodegeneration, and cardiovascular diseases. RNA‐seq illuminated detailed transcriptional profiles, and chemical reactions with cysteine‐containing compounds ...
Beau R. Brummel, Sofia Kokkaliari, Qiwen Gao, Jinjing Chen, Larissa Costa de Almeida, Srinivasarao Tenneti, Derek A. Leas, Eli Levit, Lewis S. Alexander, Khalil A. Abboud, Pingrong Wei, Michael D. Cameron, James R. Rocca, Ranjala Ratnayake, Donna D. Zhang, Hendrik Luesch, Robert W. Huigens III   +16 more
wiley   +1 more source

Overcoming Cancer Drug Resistance Utilizing PROTAC Technology

Frontiers in Cell and Developmental Biology, 2022
Cancer drug resistance presents a major barrier to continued successful treatment of malignancies. Current therapies inhibiting proteins indicated in cancer progression are consistently found to lose efficacy as a result of acquired drug resistance ...
Matthew R. Burke, Alexis R. Smith, Guangrong Zheng   +2 more
doaj   +1 more source

PROTACs in the Management of Prostate Cancer

Molecules, 2023
Cancer treatments with targeted therapy have gained immense interest due to their low levels of toxicity and high selectivity. Proteolysis-Targeting Chimeras (PROTACs) have drawn special attention in the development of cancer therapeutics owing to their unique mechanism of action, their ability to target undruggable proteins, and their focused target ...
Poornachandra Yedla, Ahmed O. Babalghith, Vindhya Vasini Andra, Riyaz Syed   +3 more
openaire   +3 more sources

Fibrates Inhibit PLTP‐induced M2 Macrophage Infiltration and Increase the Sensitivity of Hepatocellular Carcinoma to ICIs

Advanced Science, EarlyView.
Phospholipid transfer protein(PLTP) plays a critical role in forming a complex with kinase A (AURKA) and P65. This interaction facilitates phosphorylation of P65 at Ser536, leading to the activation of the NF‐κB signaling pathway. Ultimately, this leads to the upregulation of downstream cytokines, including IL‐6, IL‐8, and CSF‐1, which promotes M2 ...
Xinyue Liang, Yaning Li, Jianxun Cai, Lisi Luo, Pengfei Yang, Yutong Chen, Jiancong Zhou, Yan Zeng, Jiaping Yu, Weiyu Zhang, Wenzheng Pang, Yufang Li, Chunhua Wen, Jian Li, Linjuan Zeng   +14 more
wiley   +1 more source

Inflammasome priming in sterile inflammatory disease [PDF]

, 2017
The inflammasome is a cytoplasmic protein complex that processes interleukins (IL)-1β and IL-18, and drives a form of cell death known as pyroptosis. Oligomerization of this complex is actually the second step of activation, and a priming step must occur
Bryant, Clare E., Carroll, Richard G., Galván-Peña, Silvia, Masters, Seth L., Mills, Evanna L., Olden, Robin, Patel, Meghana N., Triantafilou, Kathy, Triantafilou, Martha, Wolf, Amaya I.   +9 more
core   +2 more sources

Targeting Lactate and Lactylation in Cancer Metabolism and Immunotherapy

Advanced Science, EarlyView.
Lactate, once deemed a metabolic waste, emerges as a central regulator of cancer progression. This review elucidates how lactate and its epigenetic derivative, protein lactylation, orchestrate tumor metabolism, immune suppression, and therapeutic resistance.
Jiajing Gong, Yuhang Xie, Zhijie Weng, Yongzhi Wu, Longjiang Li, Bo Li   +5 more
wiley   +1 more source

Fusion Molecules Between the STAT5b Inhibitor Stafib-2-CR and a Cereblon Ligand. [PDF]

ChemistryOpen
The design and synthesis of fusion molecules between the selective STAT5b inhibitor Stafib‐2‐CR and a ligand of the E3 ubiquitin ligase cereblon is reported. Activity analysis in fluorescence polarization assays and isothermal titration calorimetry indicated that the chosen attachment point for the linker is well‐suited to retain activity of the fusion
Münzel T, Seidenstücker KC, Protzel C, Berg A, Berg T.   +4 more
europepmc   +2 more sources