Undruggable targets typically refer to a class of therapeutic targets that are difficult to target through conventional methods or have not yet been targeted,but are of great clinical significance.According to statist...Undruggable targets typically refer to a class of therapeutic targets that are difficult to target through conventional methods or have not yet been targeted,but are of great clinical significance.According to statistics,over 80%of disease-related pathogenic proteins cannot be targeted by current conventional treatment methods.In recent years,with the advancement of basic research and new technologies,the development of various new technologies and mechanisms has brought new perspectives to overcome challenging drug targets.Among them,targeted protein degradation technology is a breakthrough drug development strategy for challenging drug targets.This technology can specifically identify target proteins and directly degrade pathogenic target proteins by utilizing the inherent protein degradation pathways within cells.This new form of drug development includes various types such as proteolysis targeting chimera(PROTAC),molecular glue,lysosome-targeting Chimaera(LYTAC),autophagosometethering compound(ATTEC),autophagy-targeting chimera(AUTAC),autophagy-targeting chimera(AUTOTAC),degrader-antibody conjugate(DAC).This article systematically summarizes the application of targeted protein degradation technology in the development of degraders for challenging drug targets.Finally,the article looks forward to the future development direction and application prospects of targeted protein degradation technology.展开更多
2019年2月5日,中科院生物物理研究所姬广聚课题组与清华大学药学院饶燏课题组及北京大学张秀琴课题组合作在《Cell discovery》期刊在线发表了题为“A Chemical Approach for Global ProteinKnockdown from Mice to Non-human Primates...2019年2月5日,中科院生物物理研究所姬广聚课题组与清华大学药学院饶燏课题组及北京大学张秀琴课题组合作在《Cell discovery》期刊在线发表了题为“A Chemical Approach for Global ProteinKnockdown from Mice to Non-human Primates”的研究成果。展开更多
基金supported by the National Natural Science Foundation of China(U22A20328 and 22074043)Science and Technology Commission of Shanghai Municipality(20430711800 and23ZR1475000)Lingang Laboratory(LG-QS-202206-04)。
基金supported by the National Key R&D Program of China(2021YFA1300200,2021YFA1302100 and 2020YFE0202200)the National Natural Science Foundation of China(82125034,82330115)。
文摘Undruggable targets typically refer to a class of therapeutic targets that are difficult to target through conventional methods or have not yet been targeted,but are of great clinical significance.According to statistics,over 80%of disease-related pathogenic proteins cannot be targeted by current conventional treatment methods.In recent years,with the advancement of basic research and new technologies,the development of various new technologies and mechanisms has brought new perspectives to overcome challenging drug targets.Among them,targeted protein degradation technology is a breakthrough drug development strategy for challenging drug targets.This technology can specifically identify target proteins and directly degrade pathogenic target proteins by utilizing the inherent protein degradation pathways within cells.This new form of drug development includes various types such as proteolysis targeting chimera(PROTAC),molecular glue,lysosome-targeting Chimaera(LYTAC),autophagosometethering compound(ATTEC),autophagy-targeting chimera(AUTAC),autophagy-targeting chimera(AUTOTAC),degrader-antibody conjugate(DAC).This article systematically summarizes the application of targeted protein degradation technology in the development of degraders for challenging drug targets.Finally,the article looks forward to the future development direction and application prospects of targeted protein degradation technology.
文摘2019年2月5日,中科院生物物理研究所姬广聚课题组与清华大学药学院饶燏课题组及北京大学张秀琴课题组合作在《Cell discovery》期刊在线发表了题为“A Chemical Approach for Global ProteinKnockdown from Mice to Non-human Primates”的研究成果。
