Tag: PROTAC

Application of PROTACs in target identification and validation

Announcing a new publication for Acta Materia Medica journal. Proteolysis targeting chimeras (PROTACs), as a novel therapeutic drug model, has received widespread attention from academia and the pharmaceutical industry. PROTAC technology has led researchers to focus on developing chemical biology tool properties due to the unique operating mechanism and protein dynamic regulatory properties. In recent […]

PROTACs targeting epigenetic proteins

Announcing a new publication for Acta Materia Medica journal.  The field of epigenetics pertains to alterations in gene function that are inherited without changes in the DNA sequence, including histone modifications, post-translational modifications of amino acids, and covalent modifications of DNA bases. These alteration pathways modulate the transformation of genotypes into specific phenotypes. Epigenetics plays […]

Recent advances in the molecular design and applications of proteolysis targeting chimera-based multi-specific antiviral modality

Announcing a new publication for Acta Materia Medica journal. Viral infections represent a major threat to human health and the global economy; however, most of the currently available antiviral drugs are not fully effective in restricting viral replication and selecting for drug-resistant variants. Targeted protein degradation technologies are promising strategies to avoid or delay the […]

MDM2-BCL-X L PROTACs enable degradation of BCL-X L and stabilization of p53

Announcing a new publication for Acta Materia Medica journal. Inhibition or degradation of the anti-apoptotic protein BCL-XL is a viable strategy for cancer treatment. Despite the recent development of PROTACs for degradation of BCL-XL, the choice of E3 ligase has been restricted to VHL and CRBN. The authors of this article report the development of MDM2-BCL-XL PROTACs […]

PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective

Announcing a new review article publication for Acta Materia Medica journal.  Mouse double minute 2 (MDM2) is an oncogenic E3 ligase that effectively degrades the tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt MDM2-p53 binding have been discovered and developed. Given that MDM2 and p53 form an auto-regulatory loop, in […]

PROTAC Technology for the Treatment of Alzheimer’s Disease: Advances and Perspectives

Announcing a new review article publication for Acta Materia Medica journal. Although PROTAC technology is preferable to oligonucleotides and antibodies for the treatment of neurodegenerative diseases, many limitations, such as their pharmacokinetic properties, tissue distribution, and cell permeability, must be addressed. The authors of this article review recent advances in PROTAC technology, as well as […]