Heterobifunctional proteolysis-targeting chimeras (PROTACs) offer a promising cancer treatment avenue by efficiently degrading unwanted cellular proteins. A recent study from Zhang et al. demonstrated the successful utilization of the N-end rule in PROTAC design, allowing for a modular degradation rate tailored to the oncogenic driver BCR-ABL.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.tibs.2023.10.001 | DOI Listing |
Pharmacol Rep
December 2024
Lukasiewicz Research Network - PORT Polish Center for Technology Development, ul. Stabłowicka 147, 54-066, Wroclaw, Poland.
The hypothalamic-pituitary-adrenal (HPA) axis plays a central role in governing stress-related disorders such as major depressive disorder (MDD), anxiety, and post-traumatic stress disorder. Chronic stress or early life trauma, known risk factors of disease, alter HPA axis activity and pattern of glucocorticoid (GC) secretion. These changes have consequences for physiological processes controlled by glucocorticoid receptor (GR) signaling, such as immune response and metabolism.
View Article and Find Full Text PDFMetab Brain Dis
August 2024
Department of Pharmacy Shri G.S. Institute of Technology and Science, Indore, 452003, Madhya Pradesh, India.
The mainstay behind Alzheimer's disease (AD) remains unknown due to the elusive pathophysiology of the disease. Beta-amyloid and phosphorylated Tau is still widely incorporated in various research studies while studying AD. However, they are not sufficient.
View Article and Find Full Text PDFEBioMedicine
June 2024
Department of Urology, The First Affiliated Hospital, Xi'an Jiaotong University, #277 Yanta West Road, Xi'an, China. Electronic address:
Background: Finding the oncogene, which was able to inhibit tumor cells intrinsically and improve the immune answers, will be the future direction for renal cancer combined treatment. Following patient sample analysis and signaling pathway examination, we propose p21-activated kinase 4 (PAK4) as a potential target drug for kidney cancer. PAK4 exhibits high expression levels in patient samples and plays a regulatory role in the immune microenvironment.
View Article and Find Full Text PDFFront Mol Neurosci
April 2024
LifeArc, Accelerator Building, Open Innovation Campus, Stevenage, United Kingdom.
Targeted protein degradation (TPD) is a rapidly expanding field, with various PROTACs (proteolysis-targeting chimeras) in clinical trials and molecular glues such as immunomodulatory imide drugs (IMiDs) already well established in the treatment of certain blood cancers. Many current approaches are focused on oncology targets, leaving numerous potential applications underexplored. Targeting proteins for degradation offers a novel therapeutic route for targets whose inhibition remains challenging, such as protein aggregates in neurodegenerative diseases.
View Article and Find Full Text PDFTrends Biochem Sci
January 2024
School of Life Science and Technology, ShanghaiTech University, Shanghai, 201210, China. Electronic address:
Heterobifunctional proteolysis-targeting chimeras (PROTACs) offer a promising cancer treatment avenue by efficiently degrading unwanted cellular proteins. A recent study from Zhang et al. demonstrated the successful utilization of the N-end rule in PROTAC design, allowing for a modular degradation rate tailored to the oncogenic driver BCR-ABL.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!