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1.
Acta Pharmaceutica Sinica ; (12): 1385-1397, 2010.
Article Dans Anglais | WPRIM | ID: wpr-353360

Résumé

To obtain higher potency and specificity, a series of 7-alkoxy analogues of illudalic acid was synthesized on the base of structure-activity relationship (SAR). All of these compounds exhibited submicromolar inhibition of the enzyme when tested against human leukocyte common antigen-related phosphatase (LAR) (for example, for 15e, IC50 = 180 nmol x L(-1)). They represent the most potent small-molecule inhibitors of LAR so far. These analogues also display excellent selectivity for LAR over other protein tyrosine phosphatases (PTPs) except for the highly homologous PTPsigma. The compound 15f is of 120-fold selectivity for LAR versus PTP-1B inhibition. The development of potent enzyme-specific inhibitors is so important that they may serve both as tools to study the role of LAR and as therapeutic agents for treatment of type II diabetes.


Sujets)
Coumarines , Chimie , Pharmacologie , Antienzymes , Chimie , Pharmacologie , Concentration inhibitrice 50 , Structure moléculaire , Receptor-Like Protein Tyrosine Phosphatases, Class 2 , Relation structure-activité
2.
Chinese Acupuncture & Moxibustion ; (12): 845-848, 2007.
Article Dans Chinois | WPRIM | ID: wpr-262070

Résumé

Comrade ZHU Lian is a main founder of Institute of Acupuncture and Moxibustion, China Academy of Chinese Medical Sciences, and she is the first to learn TCM for a physician of western medicine. The present paper looks back the works of comrade ZHU in acupuncture and moxibustion cause. Her main contributions are learning acupuncture and moxibustion medicine, popularizing acupuncture and moxibustion therapy; being concerned acupuncture and moxibustion cause, establishing organization of acupuncture and moxibustion research, more early conducting international exchanges of acupuncture and moxibustion; paying attention to clinical practice, proposing scientific research of acupuncture and moxibustion; writing New Acupuncture and Moxibustion Science, passing on later generations.


Sujets)
Acupuncture , Chine , Histoire du 20ème siècle
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