PROTACs selectively degrade the target protein through the ubiquitin鈥損roteasome system, which describes a different mode of action compared to conventional small-molecule inhibitors or even antibodies. Among different cancer types, prostate cancer (PC) is the most prevalent non-cutaneous cancer ...
PROTACs in the Management of Prostate Cancer Cancer treatments with targeted therapy have gained immense interest due to their low levels of toxicity and high selectivity. Proteolysis-Targeting Chimer... P Yedla,AO Babalghith,VV Andra,... - 《Molecules》 被引量: 0发表: 2023年 ...
which recruits the SCFβ−TrCPE3 ligase to degrade methionine aminopeptidase-2 (MetAp-2) [14]. In 2003, Sakamoto et al. developed PROTACs that can degrade estrogen receptor-alpha (ERα) or androgen receptor (AR) in breast cancer and prostate cancer, respectively [15]. However, these PROTA...
Advances and perspectives of proteolysis targeting chimeras (PROTACs) in drug discovery. Bioorg Chem. 2022;125:105848. https://doi.org/10.1016/j.bioorg.2022.105848 Bhatia S, Singh M, Singh T, Singh V. Scrutinizing the therapeutic potential of PROTACs in the management of Alzheimer’s disease. ...
(PROTACs) provide an alternative way to modulate protein homeostasis for cancer therapy; however, the always-on bioactivity of existing PROTACs potentially leads to uncontrollable protein degradation at non-target sites, limiting their in vivo therapeutic efficacy. We herein report a semiconducting ...
Numerous illnesses, including cancer, metabolic problems, and neurological diseases, have been linked to ubiquitination abnormalities. By creating a chimeric molecule called a proteolysis-targeting chimera, it is possible to control the balance between the creation and breakdown of proteins in the ...
The androgen receptor is a major driver of prostate cancer and inhibition of its transcriptional activity using competitive antagonists, such as enzalutamide remains a frontline therapy for prostate cancer management. However, the majori... S Jemilat,A Shanique,RR Willard,... - 《Communications Biol...
PROTAC; prostate cancer; androgen receptor; mutation; resistance1. Introduction Targeted therapies work to treat cancer by impeding certain proteins that promote tumor growth and metastasis throughout the body. These therapies have made significant strides in the treatment of cancer over the past few ...