Journal: Current Cancer Therapy Reviews
Guest editor(s):Dr. LEA Hassan
Co-Guest Editor(s):

Introduction

argeted Protein Degradation is gaining momentum in cancer therapy, it facilitate targeting undruggable proteins, it overcome cancer resistance and avoid undesirable side effects. Thus small molecules degraders have emerged as novel therapeutic strategy. Targeted protein degradation (TPD), the process of eliminating a protein of interest hold a great promise for the development of cancer therapy. The main focus of TPD is development of heterobifunctional small molecules degraders, including proteolysis-targeting chimeras (PROTACs), which contains two linked moieties with one binding the protein of interest and the other binding an E3 ligase, the formation of that complex results in polyubiquitination of the protein of interest and its subsequent degradation by the 26S proteasome. In the realm of cancer therapy, a profound evolution has ushered in sophisticated strategies the encompass both traditional protein degradation and antibody drug conjugate for targeted delivery of degraders

Keywords

Hetrobifuntional Degraders, protein degrading, Small molecules , Molecular glue, undraggable targets, PROTAC

Sub-topics