Some novel peptide dendrimers bearing four amino acids, GD and RGD peptides on their surface were synthesized from tetrakis[（carboxyethoxy）methyl]-methane using DCC method.
THE Chinese knot is a decorative handicraft that is intricately woven with one single colored rope.Knot tying in China harks back to ancient times.Before Chinese writing appeared,people tied knots to make records of t...THE Chinese knot is a decorative handicraft that is intricately woven with one single colored rope.Knot tying in China harks back to ancient times.Before Chinese writing appeared,people tied knots to make records of their lives.The size and shape indicated the significance and nature of an event.展开更多
Targeted protein degradation(TPD)represented by proteolysis targeting chimeras(PROTACs)marks a significant stride in drug discovery.A plethora of innovative technologies inspired by PROTAC have not only revolutionized...Targeted protein degradation(TPD)represented by proteolysis targeting chimeras(PROTACs)marks a significant stride in drug discovery.A plethora of innovative technologies inspired by PROTAC have not only revolutionized the landscape of TPD but have the potential to unlock functionalities beyond degradation.Non-small-molecule-based approaches play an irreplaceable role in this field.A wide variety of agents spanning a broad chemical spectrum,including peptides,nucleic acids,antibodies,and even vaccines,which not only prove instrumental in overcoming the constraints of conventional small molecule entities but also provided rapidly renewing paradigms.Herein we summarize the burgeoning non-small molecule technological platforms inspired by PROTACs,including three major trajectories,to provide insights for the design strategies based on novel paradigms.展开更多
Undruggable proteins are a class of proteins that are often characterized by large,complex structures or functions that are diffcult to interfere with using conventional drug design strategies.Targeting such undruggab...Undruggable proteins are a class of proteins that are often characterized by large,complex structures or functions that are diffcult to interfere with using conventional drug design strategies.Targeting such undruggable targets has been considered also a great opportunity for treatment of human diseases and has attracted substantial efforts in the field of medicine.Therefore,in this review,we focus on the recent development of drug discovery targeting"undruggable"proteins and their application in clinic.To make this review well organized,we discuss the design strategies targeting the undruggable proteins,including covalent regulation,allosteric inhibition,protein-protein/DNA interaction inhibition,targeted proteins regulation,nucleic acid-based approach,immunotherapy and others.展开更多
AbstracBteclin-1 is the firstly-identified mammalian protein of the autophagy machinery,which functions as a molecular scaffold for the assembly of PI3KC3(class II phosphatidylinositol 3 kinase)complex,thus controllin...AbstracBteclin-1 is the firstly-identified mammalian protein of the autophagy machinery,which functions as a molecular scaffold for the assembly of PI3KC3(class II phosphatidylinositol 3 kinase)complex,thus controlling autophagy induction and other cellular trafficking events.Notably,there is mounting evidence establishing the implications of Beclin-1 in diverse tumorigenesis processes,including tumor suppression and progression as well as resistance to cancer therapeutics and CSC(cancer stem-like cell)maintenance.More importantly,Beclin-1 has been confirmed as a potential target for the treatment of multiple cancers.In this review,we provide a comprehensive survey of the structure,functions,and regulations of Beclin-1,and we discuss recent advances in understanding the controversial roles of Beclin-1 in oncology.Moreover,we focus on summarizing the targeted Beclin-1-regulating strategies in cancer therapy,providing novel insights into a promising strategy for regulating Beclin-1 to improvecancer therapeutics in thefuture.展开更多
PRINTING is one of the four greatest inventions of ancient China.For millennia its mastery made China the sole country in the world able to produce copies of texts in great numbers and so build the largest repository ...PRINTING is one of the four greatest inventions of ancient China.For millennia its mastery made China the sole country in the world able to produce copies of texts in great numbers and so build the largest repository of books.Freed from time-consuming hand copying,the spread of culture and knowledge accelerated,ushering world civilization onto a new stage.展开更多
THE earliest Chinese characters,according to archaeological fi ndings,date back to the Yangshao Culture of the Neolithic Age,about 5,000 to 7,000 years ago.A writing system came into being in the Shang Dynasty(ca.17th...THE earliest Chinese characters,according to archaeological fi ndings,date back to the Yangshao Culture of the Neolithic Age,about 5,000 to 7,000 years ago.A writing system came into being in the Shang Dynasty(ca.17th-11th centuries BC).An immense cache of animal bones展开更多
基金the financial support of the National Natural Science Foundation of China （Project No. 20472055）.
文摘Some novel peptide dendrimers bearing four amino acids, GD and RGD peptides on their surface were synthesized from tetrakis[（carboxyethoxy）methyl]-methane using DCC method.
文摘THE Chinese knot is a decorative handicraft that is intricately woven with one single colored rope.Knot tying in China harks back to ancient times.Before Chinese writing appeared,people tied knots to make records of their lives.The size and shape indicated the significance and nature of an event.
基金supported by grants from the National Natural Science Foundation of China(22177084,82273559,82103757 and 82073473)the China Postdoctoral Science Foundation(2022M722283)+2 种基金PostDoctor Research Project,West China Hospital,Sichuan University(2023HXBH076,China)Sichuan Natural Science Foundation Project(2023NSFSC1554,China)the 1.3.5 Project for Disciplines of Excellence,West China Hospital,Sichuan University(ZYJC21036,China).
文摘Targeted protein degradation(TPD)represented by proteolysis targeting chimeras(PROTACs)marks a significant stride in drug discovery.A plethora of innovative technologies inspired by PROTAC have not only revolutionized the landscape of TPD but have the potential to unlock functionalities beyond degradation.Non-small-molecule-based approaches play an irreplaceable role in this field.A wide variety of agents spanning a broad chemical spectrum,including peptides,nucleic acids,antibodies,and even vaccines,which not only prove instrumental in overcoming the constraints of conventional small molecule entities but also provided rapidly renewing paradigms.Herein we summarize the burgeoning non-small molecule technological platforms inspired by PROTACs,including three major trajectories,to provide insights for the design strategies based on novel paradigms.
基金The study was supported by the Fundamental Research Funds for the National Natural Science Foundation of China(Nos.82104376,82073998,22177084,and 82104373)the Xinglin Scholar Research Premotion Project of Chengdu University of TCM,the Open Research Fund of Chengdu University of Traditional Chinese Medicine State Key Laboratory of Characteristic Chinese Medicine Resources in Southwest China,the Fundamental Research Funds of Science&Technology Department of Sichuan Province(Nos.2022NSFSC0626,2023NSFSC1108)the Postdoctoral Research Project of Sichuan Province.
文摘Undruggable proteins are a class of proteins that are often characterized by large,complex structures or functions that are diffcult to interfere with using conventional drug design strategies.Targeting such undruggable targets has been considered also a great opportunity for treatment of human diseases and has attracted substantial efforts in the field of medicine.Therefore,in this review,we focus on the recent development of drug discovery targeting"undruggable"proteins and their application in clinic.To make this review well organized,we discuss the design strategies targeting the undruggable proteins,including covalent regulation,allosteric inhibition,protein-protein/DNA interaction inhibition,targeted proteins regulation,nucleic acid-based approach,immunotherapy and others.
基金supported by the National Natural Science Foundation of China(Grant Nos.22177084 and 82173666)Sichuan Science and Technology Program(Grant No.2022YFQ0054,China)the Open Research Fund of Chengdu University of Traditional Chinese Medicine State Key Laboratory of Characteristic Chinese Medicine Resources in Southwest China.
文摘AbstracBteclin-1 is the firstly-identified mammalian protein of the autophagy machinery,which functions as a molecular scaffold for the assembly of PI3KC3(class II phosphatidylinositol 3 kinase)complex,thus controlling autophagy induction and other cellular trafficking events.Notably,there is mounting evidence establishing the implications of Beclin-1 in diverse tumorigenesis processes,including tumor suppression and progression as well as resistance to cancer therapeutics and CSC(cancer stem-like cell)maintenance.More importantly,Beclin-1 has been confirmed as a potential target for the treatment of multiple cancers.In this review,we provide a comprehensive survey of the structure,functions,and regulations of Beclin-1,and we discuss recent advances in understanding the controversial roles of Beclin-1 in oncology.Moreover,we focus on summarizing the targeted Beclin-1-regulating strategies in cancer therapy,providing novel insights into a promising strategy for regulating Beclin-1 to improvecancer therapeutics in thefuture.
文摘PRINTING is one of the four greatest inventions of ancient China.For millennia its mastery made China the sole country in the world able to produce copies of texts in great numbers and so build the largest repository of books.Freed from time-consuming hand copying,the spread of culture and knowledge accelerated,ushering world civilization onto a new stage.
文摘THE earliest Chinese characters,according to archaeological fi ndings,date back to the Yangshao Culture of the Neolithic Age,about 5,000 to 7,000 years ago.A writing system came into being in the Shang Dynasty(ca.17th-11th centuries BC).An immense cache of animal bones
