Results 71 to 80 of about 13,155 (273)
The Potential of Proteolytic Chimeras as Pharmacological Tools and Therapeutic Agents
Molecules, 2020 The induction of protein degradation in a highly selective and efficient way by means of druggable molecules is known as targeted protein degradation (TPD).
Bernat Coll-Martínez +2 more
doaj +1 more source
Discovery of E3 Ligase Ligands for Target Protein Degradation
Molecules, 2022 Target protein degradation has emerged as a promising strategy for the discovery of novel therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a cellular ubiquitin-dependent proteolysis system for the efficient ...
Jaeseok Lee +5 more
doaj +1 more source
The epigenetic control of E-box and Myc-dependent chromatin modifications regulate the licensing of lamin B2 origin during cell cycle [PDF]
, 2012 Recent genome-wide mapping of the mammalian replication origins has suggested the role of transcriptional regulatory elements in origin activation. However, the nature of chromatin modifications associated with such trans-factors or epigenetic marks ...
Kumar, V, Singh, AK, Swarnalatha, M
core +1 more source
Advanced Healthcare Materials, EarlyView.This study demonstrates that ALY688, a drug mimicking the heart‐protective hormone adiponectin, reduces myocardial ischemia injury. ALY688 increases the production of extracellular vesicles, which carry protective cargo including adiponectin itself.
Jialing Tang +13 more
wiley +1 more source
Towards engineering hormone-binding globulins as drug delivery agents. [PDF]
, 2014 The treatment of many diseases such as cancer requires the use of drugs that can cause severe side effects. Off-target toxicity can often be reduced simply by directing the drugs specifically to sites of diseases.
Chan, Wee Lee, Read, Randy J, Zhou, Aiwu
core +3 more sources
PROteolysis TArgeting Chimeras (PROTACs) — Past, present and future
Drug Discovery Today: Technologies, 2019 The majority of currently used therapeutics are small molecule-based and utilize occupancy-driven pharmacology as the mode of action (MOA), in which the protein function is modulated via temporary inhibition. New modalities that operate using alternative MOAs are essential for tapping into the "undruggable" proteome.
Mariell Pettersson, Craig M. Crews
openaire +2 more sources
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 +14 more
wiley +1 more source
CD36-mediated endocytosis of proteolysis-targeting chimeras
CellPassive diffusion does not explain why many drugs are too large and/or too polar for rule-breaking membrane penetration, such as proteolysis-targeting chimeras (PROTACs, generally of a molecular weight > 800 Da). Here, using biotinylated chemical-probe-based target fishing and genetic knockdown/knockin approaches, we discovered that the membrane ...
Zhengyu Wang +17 more
openaire +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 +5 more
wiley +1 more source
Advanced Science, 2021 DNA‐binding proteins, including transcription factors (TFs), play essential roles in various cellular processes and pathogenesis of diseases, deeming to be potential therapeutic targets.
Jingwei Shao +9 more
doaj +1 more source