Results 21 to 30 of about 7,774 (200)

Proteolysis Targeting Chimera Loaded Extracellular Vesicles for Developing Triple Negative Breast Cancer Treatment [PDF]

Journal of Extracellular Vesicles
Proteolysis targeting chimeras (PROTACs) represent an emerging targeted cancer therapy approach. However, their poor cell penetration and instability in vivo pose daunting challenges for wide‐spread clinical usage.
Nina Erwin, Umasankar De, Yufeng Xiao, Lei Wang, Chandra K. Maharjan, Xiaoshu Pan, Ding Zuo, Nikee Awasthee, Guangrong Zheng, Daiqing Liao, Weizhou Zhang, Mei He   +11 more
doaj   +2 more sources

Proteolysis targeting chimera (PROTAC)-driven antibody internalization of oncogenic cell surface receptors [PDF]

Communications Biology
Antibody-drug conjugates (ADCs) are increasingly used in clinic for multiple indications and may improve upon the activity of parental antibodies by delivering cytotoxic payloads into target cells.
Ezequiel J. Tolosa, Lin Yang, Jennifer Ayers-Ringler, Shinichiro Suzuki, Jayapal Reddy Mallareddy, Janet Schaefer-Klein, Mitesh Borad, Farhad Kosari, Amarnath Natarajan, Aaron S. Mansfield   +9 more
doaj   +2 more sources

Effect of esomeprazole on the pharmacokinetics of vepdegestrant, a PROteolysis TArgeting Chimera oestrogen receptor degrader, in healthy participants. [PDF]

Br J Clin Pharmacol
Aims The aim of this study is to evaluate the effects of multiple doses of esomeprazole, a strong proton pump inhibitor and acid‐reducing agent, on the pharmacokinetics and safety of vepdegestrant, a PROteolysis TArgeting Chimera oestrogen receptor degrader.
Tran L, Chen N, Winton JA, Matschke KT, Goodman SP, Lee KC, Zhang Y, Tan W.   +7 more
europepmc   +2 more sources

Promising Proteolysis-Targeting Chimera for Mutant p53-R175H [PDF]

ACS Omega
Xinzhe Zhuang, Yidan Guo, Xiaozi Sun, Jie Chen, Songbo Xie, Fengtang Yang, Jingrui Li   +6 more
doaj   +2 more sources

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

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   +1 more source

Research advances in targeted protein degradation technologies [PDF]

Yixue xinzhi zazhi
Targeted protein degradation (TPD) technologies leverage the body’s innate protein degradation systems to selectively eliminate protein of interest (POI).
PI Chuan, HAO Xuanrun, XIAO Haiting, LUO Xing, ZHANG Qixiong   +4 more
doaj   +1 more source

Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy

Journal of Hematology & Oncology, 2020
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently ...
Xin Li, Yongcheng Song
doaj   +1 more source

Proteolysis-targeting chimera against BCL-XL destroys tumor-infiltrating regulatory T cells

Nature Communications, 2021
Targeting regulatory T cells (Treg) represents a therapeutic option to abrogate tumor-associated immune suppression. Here the authors show that pharmacological degradation of BCL-XL preferentially induces apoptosis of tumor-infiltrating Treg, promoting ...
Ryan Kolb, Umasankar De, Sajid Khan, Yuewan Luo, Myung-Chul Kim, Haijun Yu, Chaoyan Wu, Jiao Mo, Xin Zhang, Peiyi Zhang, Xuan Zhang, Nicholas Borcherding, Daniel Koppel, Yang-Xin Fu, Song Guo Zheng, Dorina Avram, Guangrong Zheng, Daohong Zhou, Weizhou Zhang   +18 more
doaj   +1 more source

Development of KEAP1-targeting PROTAC and its antioxidant properties: In vitro and in vivo

Redox Biology, 2023
Oxidative stress due to abnormal accumulation of reactive oxygen species (ROS) is an initiator of a large number of human diseases, and thus, the elimination and prevention of excessive ROS are important aspects of preventing the development of such ...
Se Yong Park, Raju Gurung, Jung Ho Hwang, Ju-Hee Kang, Hyun Jin Jung, Alam Zeb, Jong-Ik Hwang, Sung Jean Park, Han-Joo Maeng, Dongyun Shin, Seung Hyun Oh   +10 more
doaj   +1 more source

Targeted degradation of LRG1 to attenuate renal fibrosis

Asian Journal of Pharmaceutical Sciences
Leucine-rich α-2 glycoprotein 1 (LRG1), a secreted glycoprotein, has been identified as significantly upregulated in renal fibrosis, potentially exacerbating the condition by enhancing TGF-β-Smad3-dependent signaling pathways.
Linyao Fan, Yingqiu Qi, Xi Yang, Yarui Xu, Yana Zhang, Longdi Wang, Anying Zhu, Lirong Zhang, Jian Song, Shengnan Du, Guangjun Nie, Huan Min   +11 more
doaj   +1 more source