Inspired by the indolopyridoquinazoline scaffold of natural products evodiamine and rutaecarpine, novel triple G4 and Top1/2 ligands were rationally designed and synthesized. Systematic structure–activity relationshi...Inspired by the indolopyridoquinazoline scaffold of natural products evodiamine and rutaecarpine, novel triple G4 and Top1/2 ligands were rationally designed and synthesized. Systematic structure–activity relationship(SAR) studies led to the discovery of compound 15g, which effectively induced and stabilized G4 and inhibited Top1/2 with potent antitumor activity. Compound 15g represents a valuable chemical tool or lead compound for antitumor drug discovery. This proof-of-concept study also validated the feasibility of using planar natural products scaffold as templates to design new G4 ligands.展开更多
Countries must have strong early warning,detection,and response capabilities in the face of the risks and challenges posed by major infectious diseases and bioterrorism threats.Vaccination is one of the most effective...Countries must have strong early warning,detection,and response capabilities in the face of the risks and challenges posed by major infectious diseases and bioterrorism threats.Vaccination is one of the most effective means for countries to maintain biosecurity and respond to bioterrorism attacks.Microneedles are emerging as a potential vaccine delivery method with minimal pain,no bleeding,and the ability to be self-administered,doing away with the need for professional health care workers.This last advantage,particularly if combined with room temperature preservation,could have an important role in improving national biosecurity through large-scale,rapid deployment of a biological vaccine.In this review,we summarized the research status of microneedles,including the types,materials,and production technologies of microneedles.Recent progress regarding microneedles in the field of biosecurity is introduced and challenges in its future application are discussed.展开更多
基金supported by the National Natural Science Foundation of China (Nos. 22077138 to S. Wu, 81725020 to C. Sheng81872742 to G. Dong)+1 种基金the National Key Research and Development Program of China (No. 2020YFA0509200 to C. Sheng)Shanghai Rising-Star Program (No. 22QA1411300 to S. Wu)。
文摘Inspired by the indolopyridoquinazoline scaffold of natural products evodiamine and rutaecarpine, novel triple G4 and Top1/2 ligands were rationally designed and synthesized. Systematic structure–activity relationship(SAR) studies led to the discovery of compound 15g, which effectively induced and stabilized G4 and inhibited Top1/2 with potent antitumor activity. Compound 15g represents a valuable chemical tool or lead compound for antitumor drug discovery. This proof-of-concept study also validated the feasibility of using planar natural products scaffold as templates to design new G4 ligands.
文摘Countries must have strong early warning,detection,and response capabilities in the face of the risks and challenges posed by major infectious diseases and bioterrorism threats.Vaccination is one of the most effective means for countries to maintain biosecurity and respond to bioterrorism attacks.Microneedles are emerging as a potential vaccine delivery method with minimal pain,no bleeding,and the ability to be self-administered,doing away with the need for professional health care workers.This last advantage,particularly if combined with room temperature preservation,could have an important role in improving national biosecurity through large-scale,rapid deployment of a biological vaccine.In this review,we summarized the research status of microneedles,including the types,materials,and production technologies of microneedles.Recent progress regarding microneedles in the field of biosecurity is introduced and challenges in its future application are discussed.
