Results 31 to 40 of about 827,025 (271)

Photopharmacology of Proteolysis-Targeting Chimeras: A New Frontier for Drug Discovery

Frontiers in Chemistry, 2021
Photopharmacology is an emerging field that uses light to precisely control drug activity. This strategy promises to improve drug specificity for reducing off-target effects.
Shenxin Zeng, Shenxin Zeng, Hongjie Zhang, Hongjie Zhang, Zhengrong Shen, Zhengrong Shen, Wenhai Huang, Wenhai Huang   +7 more
doaj   +1 more source

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   +2 more sources

Overcoming the therapeutic limitations of EZH2 inhibitors in Burkitt’s lymphoma: a comprehensive study on the combined effects of MS1943 and Ibrutinib

Frontiers in Oncology, 2023
Enhancer of zeste homolog 2 (EZH2) and Bruton’s tyrosine kinase (BTK) are both key factors involved in the development and progression of hematological malignancies.
Yurim Jeong, Se Been Kim, Chae-Eun Yang, Min Seo Yu, Wan-Su Choi, Wan-Su Choi, Youngwoo Jeon, Jung-Yeon Lim   +7 more
doaj   +1 more source

Proteolysis-targeting chimeras in drug development: A safety perspective [PDF]

, 2020
Proteolysis‐targeting chimeras are a new drug modality that exploits the endogenous ubiquitin proteasome system to degrade a protein of interest for therapeutic benefit.
Pachl, Fiona, Boyd, Helen, Dahl, Goran, Andrew X. Zhang, Coen, Muireann, Newham, Pete, Goran Dahl, Moreau, Kevin, Castaldi, M Paola, Helen Boyd, Clay Scott, Fiona Pachl, M. Paola Castaldi, Zhang, Andrew X, Scott, Clay, Kevin Moreau, Muireann Coen, Pete Newham   +17 more
core   +1 more source

Discovery of Selective Proteolysis-Targeting Chimera Degraders Targeting PTP1B as Long-Term Hypoglycemic Agents

PTP1B, a promising target for insulin sensitizers in type 2 diabetes treatment, can be effectively degraded using proteolysis-targeting chimera (PROTAC). This approach offers potential for long-acting antidiabetic agents.
Yuqi Ying (14434974), Shaobing Cheng (10094194), Ziwei Zhang (2029975), Zhifang Cai (785093), Zunhua Yang (544464), Yulin Feng (117705), Pei Hu (1489597), Jian Xiong (531582), Jiamin Wu (1987333), Yuanying Fang (544463), Qing Zeng (494174), Huilan Li (7489379)   +11 more
core   +4 more sources

Newly Emerging Strategies in Antiviral Drug Discovery: Dedicated to Prof. Dr. Erik De Clercq on Occasion of His 80th Anniversary

Molecules, 2022
Viral infections pose a persistent threat to human health. The relentless epidemic of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become a global health problem, with millions of infections and fatalities so far.
Shujing Xu, Dang Ding, Xujie Zhang, Lin Sun, Dongwei Kang, Boshi Huang, Xinyong Liu, Peng Zhan   +7 more
doaj   +1 more source

Proteolysis Targeting Chimeras (PROTACs)

ACS Pharmacology and Translational Science, 2022
Targeted protein degradation (TPD) is a promising therapeutic modality to modulate protein levels and its application promises to reduce the "undruggable"proteome. Among TPD strategies, Proteolysis TArgeting Chimera (PROTAC) technology has shown a tremendous potential with attractive advantages when compared to the inhibition of the same target.
Ruffilli, Camilla, Roth, Sascha, Rodrigo, Monica, Boyd, Helen, Zelcer, Noam, Moreau, Kevin   +5 more
openaire   +1 more source

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Molecular Cancer, 2022
AbstractProteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits target protein and E3 ubiquitin ligase together to trigger proteasomal degradation of target protein by the ubiquitin-proteasome system. PROTAC has emerged as a promising
Xinyi Li, Wenchen Pu, Qingquan Zheng, Min Ai, Song Chen, Yong Peng   +5 more
openaire   +3 more sources

Proteolysis Targeting Chimera Degraders of the METTL3–14 m6A‑RNA Methyltransferase [PDF]

JACS Au
Francesco Errani, Annalisa Invernizzi, Marcin Herok, Elena Bochenkova, Fiona Stamm, Ivan Corbeski, Valeria Romanucci, Giovanni Di Fabio, František Zálešák, Amedeo Caflisch   +9 more
doaj   +2 more sources

Radiotherapy-Triggered Proteolysis Targeting Chimera Prodrug Activation in Tumors

, 2022
Proteolysis targeting chimera (PROTAC) is an emerging protein degradation strategy, which shows excellent advantages in targeting those so-called “undruggable” proteins.
Yujie Li (294983), Jinghong Li (219583), Chunrong Yang (294274), Yujie Li, Qiankun Ni, Yuchen Yang, Chunrong Yang, Jinghong Li, Yuchen Yang (21709), Qiankun Ni (8574846)   +9 more
core   +1 more source