Currently,cancer is the most rapidly growing life-threatening disease after cardiovascular in the world,posing a major threat to human life.Telomerase promotes tumorigenesis and development in most cancers and dyskeri...Currently,cancer is the most rapidly growing life-threatening disease after cardiovascular in the world,posing a major threat to human life.Telomerase promotes tumorigenesis and development in most cancers and dyskerin plays a crucial role in telomere maintenance.Cancer molecules are being developed continuously as a result of continuous research.A series of novel anticancer agents have been developed using telomerase inhibitors with improved specificity and pharmacokinetics.As medicinal chemistry advances,heterocyclic-based drugs find increasing applications,including anticancer agents.These properties have led to the development of five-membered aromatic rings of oxadiazoles.In order to enhance their anticancer activity,oxadiazole scaffolds can be modified.In this review,we discuss the functions and mechanism of action of the telomerase enzyme.The paper also summarizes the interaction between 1,3,4-oxadiazole inhibitors and telomerase enzymes.展开更多
First cationic 6-quinolyl substituted dithiaporphyrin was synthesized using Skraup quinoline methodology from thiaporphyrin bearing 4-acetamidophenyl prepared by condensation reaction of aromatic aldehyde with pyrrole.
Objective This study aimed to investigate the expression and significance of PIN2/TERF1 interacting, telomerase inhibitor 1(Pin X1) and human telomerase reverse transcriptase(h TERT) in basal cell carcinoma(BCC). Meth...Objective This study aimed to investigate the expression and significance of PIN2/TERF1 interacting, telomerase inhibitor 1(Pin X1) and human telomerase reverse transcriptase(h TERT) in basal cell carcinoma(BCC). Methods Real-time polymerase chain reaction and immunohistochemistry were performed to quantify the m RNA expressions and integrated optical density(IOD), respectively, of Pin X1 and h TERT in BCC specimens(n = 30), as well as in normal skin specimens(n = 15). Results The m RNA expression level and IOD of Pin X1 in the BCC samples were both significantly lower than those in the control specimens(P < 0.05). Conversely, the m RNA expression level and IOD of h TERT in BCC were both significantly higher than that in the control samples(P < 0.05). The correlation between the expression levels of Pin X1 and h TERT showed no statistical significance(P > 0.05). Conclusion Downregulation of Pin X1 and upregulation of h TERT expression may be associated with the activation and maintenance of telomerases in the induction of BCC.展开更多
文摘Currently,cancer is the most rapidly growing life-threatening disease after cardiovascular in the world,posing a major threat to human life.Telomerase promotes tumorigenesis and development in most cancers and dyskerin plays a crucial role in telomere maintenance.Cancer molecules are being developed continuously as a result of continuous research.A series of novel anticancer agents have been developed using telomerase inhibitors with improved specificity and pharmacokinetics.As medicinal chemistry advances,heterocyclic-based drugs find increasing applications,including anticancer agents.These properties have led to the development of five-membered aromatic rings of oxadiazoles.In order to enhance their anticancer activity,oxadiazole scaffolds can be modified.In this review,we discuss the functions and mechanism of action of the telomerase enzyme.The paper also summarizes the interaction between 1,3,4-oxadiazole inhibitors and telomerase enzymes.
文摘First cationic 6-quinolyl substituted dithiaporphyrin was synthesized using Skraup quinoline methodology from thiaporphyrin bearing 4-acetamidophenyl prepared by condensation reaction of aromatic aldehyde with pyrrole.
文摘Objective This study aimed to investigate the expression and significance of PIN2/TERF1 interacting, telomerase inhibitor 1(Pin X1) and human telomerase reverse transcriptase(h TERT) in basal cell carcinoma(BCC). Methods Real-time polymerase chain reaction and immunohistochemistry were performed to quantify the m RNA expressions and integrated optical density(IOD), respectively, of Pin X1 and h TERT in BCC specimens(n = 30), as well as in normal skin specimens(n = 15). Results The m RNA expression level and IOD of Pin X1 in the BCC samples were both significantly lower than those in the control specimens(P < 0.05). Conversely, the m RNA expression level and IOD of h TERT in BCC were both significantly higher than that in the control samples(P < 0.05). The correlation between the expression levels of Pin X1 and h TERT showed no statistical significance(P > 0.05). Conclusion Downregulation of Pin X1 and upregulation of h TERT expression may be associated with the activation and maintenance of telomerases in the induction of BCC.
