Conventional small-molecule drugs (SMDs) are compounds characterized by low molecular weight, high cell permeability, and high selectivity. In clinical translation, SMDs are regarded as good candidates for oral drug formulation. SMD inhibitors play an important role in cancer treatment; however, resistance and low effectiveness have been major bottlenecks in clinical application. Generally, only 20% of cell proteins can potentially be targeted and have been developed as SMDs; thus, some types of tumor targets are considered "undruggable." Among these are transcription factors (TFs), an important class of proteins that regulate the occurrence, formation, and development of tumors. It is difficult for SMDs and macromolecular drugs to identify bioactive sites in TFs and hence for use as pharmacological inhibitors in targeting TF proteins. For this reason, technologies that enable targeted protein degradation, such as proteolysis-targeting chimera or molecular glues, could serve as a potential tool to solve these conundrums.
第一作者机构：[1]Wuhan Univ, Zhongnan Hosp, Dept Gynecol Oncol, Wuhan, Peoples R China
共同第一作者：
通讯作者：
通讯机构：[8]Harvard Med Sch, Brigham & Womens Hosp, Dept Pathol, Boston, MA 02115 USA[*1]Department of Pathology, Brigham and Women’s Hospital, Harvard Medical School, Boston, MA 02115, USA.
推荐引用方式(GB/T 7714)：
Dai Mengyuan,Radhakrishnan Sridhar,Li Rui,et al.Targeted Protein Degradation: An Important Tool for Drug Discovery for "Undruggable" Tumor Transcription Factors[J].TECHNOLOGY IN CANCER RESEARCH & TREATMENT.2022,21:doi:10.1177/15330338221095950.
APA：
Dai, Mengyuan,Radhakrishnan, Sridhar,Li, Rui,Tan, Ruirong,Yan, Kuo...&Liu, Miao.(2022).Targeted Protein Degradation: An Important Tool for Drug Discovery for "Undruggable" Tumor Transcription Factors.TECHNOLOGY IN CANCER RESEARCH & TREATMENT,21,
MLA：
Dai, Mengyuan,et al."Targeted Protein Degradation: An Important Tool for Drug Discovery for "Undruggable" Tumor Transcription Factors".TECHNOLOGY IN CANCER RESEARCH & TREATMENT 21.(2022)
