Results 71 to 80 of about 13,195 (282)

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

Novel Design Strategies to Enhance the Efficiency of Proteolysis Targeting Chimeras

ACS Pharmacology & Translational Science, 2022
Despite the success of drug discovery over the past decades, many potential drug targets still remain intractable for small molecule modulation. The development of proteolysis targeting chimeras (PROTACs) that trigger degradation of the target proteins provides a conceptually novel approach to address drug targets that remained previously elusive ...
Chunlong Zhao, Frank J. Dekker
openaire   +3 more sources

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies [PDF]

Journal of Hematology & Oncology, 2020
AbstractProteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI). PROTACs are potentially superior to conventional small molecule inhibitors (SMIs) because of their unique mechanism of action (MOA, i.e., degrading POI in a sub-stoichiometric ...
Yonghan He, Sajid Khan, Zhiguang Huo, Dongwen Lv, Xuan Zhang, Xingui Liu, Yaxia Yuan, Robert Hromas, Mingjiang Xu, Guangrong Zheng, Daohong Zhou   +10 more
openaire   +3 more sources

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

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, Antonio Delgado, Bernat Crosas   +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, Youngjun Lee, Young Mee Jung, Ju Hyun Park, Hyuk Sang Yoo, Jongmin Park   +5 more
doaj   +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

Extracellular Vesicles Modulation by an Adiponectin Receptor Agonist Provides Cardioprotection for Myocardial Ischemic Injury

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, Wing Yan Chung, Serena M. Pulente, Yubin Lei, Khang Nguyen, Eddie Tam, Nadya M. Morrow, Ilka Lorenzen‐Schmidt, Fengxia Xiao, Augusto Zani, Dylan Burger, Hye Kyoung Sung, Erin E. Mulvihill, Gary Sweeney   +13 more
wiley   +1 more source

Proteolysis targeting chimeras in non-small cell lung cancer

Cancer Treatment Reviews, 2023
Non-small cell lung cancer (NSCLC) has very poor prognosis in advanced stages. Discovery and application of therapies targeting specific oncogenic driver mutations has greatly improved overall survival. However, targeted therapies are limited in their efficacy due to resistance mutations that may arise with long term use. Proteolysis targeting Chimeras
Garo Hagopian, Christopher Grant, Misako Nagasaka   +2 more
openaire   +2 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