Results 11 to 20 of about 823,777 (226)

Proteolysis-targeting chimera (PROTAC) nanomedicines toward cancer treatment: From synthesis to therapeutic delivery [PDF]

Biomaterials
Proteolysis-targeting chimera (PROTAC) has emerged as a groundbreaking therapeutic strategy by hijacking the endogenous ubiquitin proteasome system (UPS) for targeted protein degradation. These heterobifunctional molecules recruit E3 ligases to recognize
Fuwu Zhang, Xiaoyuan Chen, Xiao Zhang
exaly   +3 more sources

Rational Design and Optimization of a Potent IDO1 Proteolysis Targeting Chimera (PROTAC). [PDF]

J Med Chem
Indoleamine 2,3-dioxygenase 1 (IDO1) is an immunosuppressive protein that inhibits antitumor immunity through both tryptophan metabolism and nonenzymatic functions.
Monsen PJ, Bommi PV, Grigorescu AA, Lauing KL, Mao Y, Berardi P, Zhai L, Ojo O, Penco-Campillo M, Koch T, Egozi M, Jha S, Dunne SF, Jiang H, Song G, Zhang F, Kregel S, Vaziri-Gohar A, Fanning SW, Sanchez-Gomez P, Allen JM, Yamini B, Lukas RV, Wainwright DA, Schiltz GE.   +24 more
europepmc   +6 more sources

Potential application of proteolysis targeting chimera (PROTAC) modification technology in natural products for their targeted protein degradation

Food Science and Human Wellness, 2022
There are numerous evaluations of natural products, of which majority are food bioactives, performed up to date for their various health beneficial activities via targeting specific proteins.
Guliang Yang, Haiyan Zhong, Xinxin Xia, Zhiwen Qi, Chengzhang Wang, Shiming Li   +5 more
doaj   +2 more sources

Natural product-based PROteolysis TArgeting Chimeras (PROTACs)

Natural Product Reports, 2022
Covering: upto 2022 Natural products have an embedded recognition of protein surfaces. They possess this property as they are produced by biosynthetic enzymes and are substrates for one or more enzymes in the biosynthetic pathway. The inherent advantages,
Liu, Miaomiao, Quinn, Ronald J, Martyn, Alexander P   +2 more
core   +6 more sources

Recent Advances in Optically Controlled PROTAC

Bioengineering, 2023
Proteolysis-targeting chimera (PROTAC) technology is a groundbreaking therapeutic approach with significant clinical potential for degrading disease-inducing proteins within targeted cells.
Muzi Ouyang, Ying Feng, Hui Chen, Yanping Liu, Chunyan Tan, Ying Tan   +5 more
doaj   +2 more sources

Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity [PDF]

Nature Communications, 2020
Senolytics have the potential to extend healthspan by selectively killing senescent cells (SCs), but senolytics that target Bcl-xl may cause platelet toxicity.
Yonghan He, Xuan Zhang, Jianhui Chang, Ha-Neui Kim, Peiyi Zhang, Yingying Wang, Sajid Khan, Xingui Liu, Xin Zhang, Dongwen Lv, Lin Song, Wen Li, Dinesh Thummuri, Yaxia Yuan, Janet S. Wiegand, Yuma T. Ortiz, Vivekananda Budamagunta, Jennifer H. Elisseeff, Judith Campisi, Maria Almeida, Guangrong Zheng, Daohong Zhou   +21 more
doaj   +2 more sources

Specific proteolysis mediated by a p97-directed proteolysis-targeting chimera (p97-PROTAC) [PDF]

eLife
The p97 protein is a member of the AAA+ family of ATPases. This protein is encoded by the VCP gene. It is a mechanoenzyme that uses energy from ATP hydrolysis to promote protein unfolding and segregation actively.
Constanza Salinas-Rebolledo, Javier Blesa, Guillermo Valenzuela-Nieto, David Schwefel, Natalia López-González del Rey, Maxs Méndez-Ruette, Janine Burkhalter, Elizabeth Carrazana, Francisca Díaz-Tejeda, Ignacio Arias Catalán, Claudio Cappelli Leon, Natalia Salvadores, Luis Federico Bátiz, Ronald Jara, José A Obeso, Pedro Chana-Cuevas, Gopal P Sapkota, Alejandro Rojas-Fernandez   +17 more
doaj   +2 more sources

PTGES3 proteolysis using the liposomal peptide-PROTAC approach

Biology Direct
Background Hepatocellular carcinoma (HCC) is the leading cause of cancer-related deaths worldwide, and the lack of effective biomarkers for early detection leads to poor therapeutic outcomes.
Shiwei Liu, Fukang Yuan, Hui Dong, Jiaqi Zhang, Xinyu Mao, Yangsui Liu, Huansong Li   +6 more
doaj   +2 more sources

Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer. [PDF]

J Med Chem, 2023
We report the discovery of ARD-2051 as a potent and orally efficacious androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM and Dmax >90% in inducing AR protein degradation in both the LNCaP and VCaP ...
Han X, Zhao L, Xiang W, Miao B, Qin C, Wang M, Xu T, McEachern D, Lu J, Wang Y, Metwally H, Yang CY, Kirchhoff PD, Wang L, Matvekas A, Takyi-Williams J, Wen B, Sun D, Ator M, Mckean R, Wang S.   +20 more
europepmc   +2 more sources

PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes

, 2020
We have identified a proteolysis targeting chimera (PROTAC) of class I HDACs 1, 2 and 3. The most active degrader consists of a benzamide HDAC inhibitor, an alkyl linker, and the von Hippel-Lindau E3 ligand.
Shaun Michael Cowley (9088397), James KS Norris (9088391), Grace E Adams (9088385), Joshua P Smalley (9088382), James T Hodgkinson (9088400), Christopher J Millard (9088388), Yun Song (2183038), John WR Schwabe (9088394)   +7 more
core   +6 more sources