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Isolation and structure of antagonists of chemokine receptor (CCR5)   总被引:2,自引:0,他引:2  
Human CCR5 is a G-coupled receptor that binds to the envelope protein gp120 and CD4 and mediates the HIV-1 viral entry into the cells. The blockade of this binding by a small molecule receptor antagonist could lead to a new mode of action agent for HIV-1 and AIDS. Screening of natural product extracts led to the identification of anibamine (1), a novel pyridine quaternary alkaloid as a TFA salt, from Aniba sp.; ophiobolin C from fermentation extracts of fungi Mollisia sp.; and 19,20-epoxycytochalasin Q from Xylaria sp. Formation of the TFA salt of anibamine is plausibly an artifact of the isolation. The identity of the natural counterion is unknown. Anibamine.TFA competed for the binding of 125I-gp120 to human CCR5 with an IC50 of 1 microM. Ophiobolin C and 19,20-epoxycytochalasin Q exhibited binding IC50) values of 40 and 60 microM, respectively.  相似文献   
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OBJECTIVE: To measure communication loads on clinical staff in an acute clinical setting, and to describe the pattern of informal and formal communication events, Australia. DESIGN: Observational study. SETTING: Two emergency departments, one rural and one urban, in New South Wales hospitals, between June and July 1999. PARTICIPANTS: Twelve clinical staff members, comprising six nurses and six doctors. MAIN OUTCOME MEASURES: Time involved in communication; number of communication events, interruptions, and overlapping communications; choice of communication channel; purpose of communication. RESULTS: 35 hours and 13 minutes were observed, and 1286 distinct communication events were identified, representing 36.5 events per person per hour (95% CI, 34.5-38.5). A third of communication events (30.6%) were classified as interruptions, giving a rate of 11.15 interruptions per hour for all subjects; 10% of communication time involved two or more concurrent conversations; and 12.7% of all events involved formal information sources such as patients' medical records. Face-to-face conversation accounted for 82%. While medical staff asked for information slightly less frequently than nursing staff (25.4% v 30.9%), they received information much less frequently (6.6% v 16.2%). CONCLUSION: Our results support the need for communication training in emergency departments and other similar workplaces. The combination of interruptions and multiple concurrent tasks may produce clinical errors by disrupting memory processes. About 90% of the information transactions observed involved interpersonal exchanges rather than interaction with formal information sources. This may put a low upper limit on the potential for improving information processes by introducing electronic medical records.  相似文献   
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Jayasuriya JP 《Anaesthesia》2000,55(2):201-202
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