Results 131 to 140 of about 11,341 (256)

TRIM31–LOX‐1 Axis: A Novel Therapeutic Frontier in Atherosclerosis

iNew Medicine, EarlyView.
ABSTRACT Atherosclerosis, driven by a vicious cycle of lipid accumulation and chronic inflammation, underlies most cardiovascular diseases. Macrophages exacerbate this process by internalizing oxidized low‐density lipoprotein (oxLDL), forming foam cells, and releasing inflammatory mediators. A recent study published in Circulation identified the TRIM31–
Qian Zhang, Cheng Xue Qin
wiley   +1 more source

A region-confined PROTAC nanoplatform for spatiotemporally tunable protein degradation and enhanced cancer therapy

Nature Communications
The antitumor performance of PROteolysis-TArgeting Chimeras (PROTACs) is limited by its insufficient tumor specificity and poor pharmacokinetics. These disadvantages are further compounded by tumor heterogeneity, especially the presence of cancer stem ...
Jing Gao, Xingyu Jiang, Shumin Lei, Wenhao Cheng, Yi Lai, Min Li, Lei Yang, Peifeng Liu, Xiao-hua Chen, Min Huang, Haijun Yu, Huixiong Xu, Zhiai Xu   +12 more
doaj   +1 more source

PROTACs in cancer immunotherapy: a minireview

Biochemical Society Transactions
The discovery of immune checkpoint blockade as a therapeutic strategy to induce immunogenic cancer cell elimination has shown great success in the treatment of various cancers. However, limited response rates highlight the need for further development in this field. Promising new preclinical developments include the discoveries of proteolysis-targeting
Köckenberger J. E., Cardenas Alcoser E. S., Chang E. T., Gutkind J. S., Ferguson F. M.   +4 more
openaire   +2 more sources

SUMOylation regulates tumorigenesis and progression: Molecular mechanisms and therapeutic applications

Interdisciplinary Medicine, EarlyView.
SUMOylation, a dynamic post‐translational modification, acts as a master regulator at the heart of tumor malignancy. Our work delineates how the SUMOylation cycle—mediated by E1/E2/E3 enzymes and reversed by SENPs—orchestrates multiple hallmarks of cancer. The central pathway converges on three critical pathological axes: 1.
Yimao Wu, Zichang Chen, Yinting Hu, Gokhan Zengin, Qian Zhang, Meng‐Yao Li, Wenlong Sun   +6 more
wiley   +1 more source

Bladder-cancer-associated mutations in RXRA activate peroxisome proliferator-activated receptors to drive urothelial proliferation [PDF]

, 2017
RXRA regulates transcription as part of a heterodimer with 14 other nuclear receptors, including the peroxisome proliferator-activated receptors (PPARs).
Arora, Vivek K, Bolzenius, Jennifer, Bowman, Gregory R, Chu, Clarence E, Halstead, Angela M, Kapadia, Chiraag D, Schriefer, Andrew, Wartman, Lukas D   +7 more
core   +2 more sources

Smart Integration of Structural Biology and Medicinal Chemistry to Unlock Target‐Driven Drug Discovery

Medicinal Research Reviews, EarlyView.
ABSTRACT To enhance drug discovery efforts, medicinal chemists should evaluate, filter, and utilize relevant structural information about target proteins. Acquiring and interpreting protein structures is crucial for elucidating ligand‐receptor interactions and addressing ADME‐related considerations, making it an essential aspect of medicinal chemistry.
Matteo Rossi Sebastiano, Giulia Apprato, Serena Francisco, Giuseppe Ermondi, Giulia Caron   +4 more
wiley   +1 more source

Multi‐Targeting Ligands as Prospective Therapeutics for Alzheimer's Disease, a Prevalent Neurodegenerative Disorder: Mechanistic Insights, Emerging Targets and Drug Discovery Campaigns

Medicinal Research Reviews, EarlyView.
ABSTRACT Alzheimer's disease (AD) is a debilitating neurodegenerative condition characterized by progressive cognitive impairment, memory deterioration, and neuronal dysfunction. Its complex pathophysiology involves multiple interlinked processes, including amyloid‐β (Aβ) aggregation, tau hyperphosphorylation, oxidative stress, neuroinflammation ...
Amandeep Thakur, Mandeep Rana, Sakshi Vanjani, Kei‐Chi Liou, Rajeev Taliyan, Kunal Nepali, Chih‐Hao Yang   +6 more
wiley   +1 more source

Dual-Action-Only PROTACs

Journal of the American Chemical Society
Proteolysis targeting chimera (PROTAC)-based degraders are highly potent pseudocatalytic drugs, but on-target off-site homing could yield undesirable consequences. We report here a generalizable AND-logic gated PROTAC, where the concurrent presence of two different disease-relevant endogenous stimuli liberates an active protein degrader. We design Dual-
Ranit Dutta, Anirudh Devarajan, Amelia Talluri, Ritam Das, S. Thayumanavan   +4 more
openaire   +2 more sources

AlphaFold2‐Guided Cyclic Peptide Stabilizer Design to Target Protein–Protein Interactions

Proteins: Structure, Function, and Bioinformatics, EarlyView.
ABSTRACT The control and modulation of protein–protein interactions (PPIs) is of central importance for the majority of biological processes and most biomedical applications. Stabilization of PPIs, besides inhibition, is of growing pharmaceutical interest.
Niklas Halbwedl, Martin Zacharias
wiley   +1 more source

Effects of bioinsecticide exposure route on aphids and their natural enemies in oilseed rape

Pest Management Science, EarlyView.
Fatty acids, silicone polymers and surfactants reduced aphid numbers but caused natural enemy mortality under direct exposure, while minimal residual activity suggests potential for targeted, compatible use in integrated pest management. Abstract BACKGROUND Myzus persicae Sulzer and Brevicoryne brassicae L.
Aimee J. Tonks, Tom W. Pope, Simon Cooper, Joe M. Roberts   +3 more
wiley   +1 more source