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The most important new information since the previous Report is as follows: Our estimate for the output gap in the coming year has been revised upwards because the growth rate for mainland GDP is now projected to be somewhat higher see Chart 1 ; . This upward revision is primarily due to higher mainland investment and increased public consumption. Employment has been somewhat higher than previously projected. The krone has appreciated, but high export prices are curbing the negative effects on profitability in the export industries.
FIG. 6. Steady-state fluorescence emission spectra of Xyl I as a function of pepstatin A. Protein fluorescence was excited at 295 nm, and emission was monitored from 300 400 nm at 25 Titration was performed by the addition of different concentrations of the inhibitor to a fixed concentration of enzyme. Xyl I 2 M ; was dissolved in sodium phosphate buffer, 0.05 M, pH 6.0, and the concentrations of pepstatin A used were 0 M f ; , 0.72 M ; , 0.1.44 M OE ; , 2.16 M ; , 3.6 M ; , 4.32 M E ; , 5 5.8 M ; , 6.5 M , ; . The curve in the inset represents the best fit of the fluorescence quenching data of Xyl I at 340 nm max ; as a function of pepstatin A concentration.
3. Report on the World Planning Schools Congress WPSC ; 2001 Mike Hibbard: ACSP representative, reported on the upcoming conference. In addition to the details regarding co-sponsoring organizations, dates, and submission deadlines, Mike observed that having a plenary session of Thursday, Nov. 2 with Prad Laquian as the keynote speaker, was a major accomplishment for the GPEIG group. Tongji University organizing committee: Profs. Wu Zhiqiang, Wang Bowei, and Tang Zilai were present to offer clarifications about the conference. 3.a. ; Comments from ACSP president-elect Wim Wiewel. 4. Action items Election for a new Co-Chair with two-year term Nov. 2000-Nov. 2002 ; : Johanna Looye, University of Cincinnati, was elected Co-Chair for the term Nov. 2000- Nov. 2002. The position of "Co-Chair elect" was created and Nihal Pereira, Ball State University, was elected as Co-Chair for the term Nov. 2001- Nov. 2003. Secretariat offered thanks to Ruth Yabes for her tireless service. GPEIG Online Newsletter: The newsletter is to be published twice a year, in the fall after the ACSP conference and in the spring after the abstract submissions for the upcoming conference. It has been planned to encourage papers for the conference and member communications. It was agreed that each Co-Chair is responsible for two issues of the newsletter during his her term. A call for contributions will be announced on the listserv 4 to 6 weeks in advance of its publication. WPSC 2001 panel and roundtable topics and volunteer organizers: The need to be more organized was mentioned, as well as the importance of having all proposals in on deadline. In an effort to be proactive in encouraging and organizing the submission of papers, panels, and roundtables, the group discussed several topics for potential sessions. There was also a discussion of the difference between roundtables and panels. Farokh Afshar: Roundtable with representation from different world regions to discuss pedagogy, with emphasis on the importance of different perspectives and the different issues in planning and how to prepare students to face them. Salah El Shakhs: Roundtable on the governance of mega-cities. Bish Sanyal: Panel or roundtable on the relationship between economic performance and political systems as it is mediated by planning. Elizabeth Sweet: Gender issues in transitioning economies. Nihal Pereira: How planning has changed in South and Southeast Asia European and colonial influences and changes afterward ; . Tridib Bannerjee: Comparative planning systems, with a focus on planning itself. Hemalata Dandekar: Panel session. Different regions, roles of the states, and faces of privatization. Keith Pezolli: Trans -border environmental problems. Sam Cassella, president-elect of AICP, mentioned plans to create a globalization task force to improve responsiveness of AICP to international and global issues. ACSP 2001 panel and roundtable topics and volunteer organizers. To be done on listserv. Faculty and Ph.D. mentoring program volunteers for committee ; : Salah El-Shakhs mentioned that ACSP is already in charge of this, and feels there is no need to get involved. Gill Lim mentioned it is good to nurture people in this area, but need more incentives to do this, e.g. best dissertation in planning. The new leaders are to discuss mentoring, which at this time was referred to as a good idea, but one with insufficient interest to pursue at the current time. Governance principles and by-laws volunteers for committee ; : The need for GPEIG's own by-laws was brought up. John Browder volunteered to prepare the first draft. Al Nuur Ibrahim volunteered to assist. Gill Lim brought up the importance of maintaining continuity and of being aware of our beginnings as a group. He cited the 1997 report by the National Commission on Global Education, which included a good report on Global Education. There was also the outline of major issues to deal with in JPER published in 1993. The need for continuity was mentioned e.g., Paul Niebank and Himi Jamal, who no longer come ; . Farokh volunteered to prepare a piece for the newsletter that would summarize our institutional history. He planned for it to include benchmark events and decisions, and 1-2 short documents for circulation. 5. Discussion items GPEIG webpage and member directory discussion postponed ; . Hema Dandekar proposed to change the name of the track to "International Development Planning." The motion was passed. Hema will contact ACSP Conference Chair to formally change the track name. The need for one additional member for the secretariat was suggested. No decisions were made; and email will be sent to the group to discuss and decide. Logistical issues for the conference were discussed, including: Airfare for Chicago-Shanghai is estimated at 0 lowest ; by NW Airlines. There were inquiries regarding the possibility of a group rate. It was mentioned that AESOP has done this in the past. Hotel: 4 stars 0-0, 3 stars - for hotels, see brochure ; . Visas: 2 kinds for visa information, see embassy website ; : 1 ; Travel visa tourist ; , .00, 5 days to process for stay up to 30 days. 2 ; Business visa, .00, 2 weeks to process, allows for a longer stay Connections to Latin America. Bill Siembieda reported on ACSP interactions with two Latin American planning organizations: ANPUR, Brazilian organization, with participation from Chile and Argentina; and Association of Latin American Schools of Planning, which includes Mexico, Venezuela and Argentina, with a total of 8-9 schools. It was proposed that our group interact with these organizations in order to nurture more global discussion and build trust among us.
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MEDI 381 Pyrido[1, 2-a]pyrimidin-4-ones as potent CXCR3 antagonists Jason Duquette1, Xiaohui Du1, Johann Chan2, Bryan Lemon1, Tassie Collins1, George Tonn1, Julio Medina1, and Xiaoqi Chen1. 1 ; Amgen Inc, 1120 Veterans Blvd, South San Francisco, CA 94080, duquette amgen , 2 ; Amgen Inc, Thousand Oaks, CA 91320 Pyrido-[1, 2-a]pyrimidine-4-ones were found to be a potent series of CXCR3 antagonists. However, compounds in this series displayed PXR mediated CYP-induction. In this presentation we describe the optimization that lead to the discovery of a potent CXCR3 antagonist with reduced PXR activity. Some observations on the relationship between lipophilicity and PXR activation will be presented. Furthermore, the synthetic routes that enabled the exploration of the SAR of this series will be highlighted along with the biological data. These efforts lead to the identification of compound 1 as a potent CXCR3 antagonist with good in vitro and in vivo pharmacokinetic properties.
The following authors or their immediate family members have indicated a financial interest. No conflict exists for drugs or devices in a study if they are not being evaluated as part of the investigation. Acted as a consultant within the last 2 years: Mark G. Kris, Aventis Pharmaceuticals, Bristol-Myers Squibb, GlaxoSmithKline, Merck and Company, MGI Pharma Inc, Pfizer Inc. Received more than , 000 a year from a company for either of the last 2 years: Mark G. Kris, Aventis Pharmaceuticals, Bristol-Myers Squibb, GlaxoSmithKline, Merck and Company, MGI Pharma Inc, Pfizer Inc and formoterol.
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Chemicals--Sodium pentobarbitone Sagatal ; was obtained from Rhone Merieux Harlow, Middlesex, UK ; . Antibodies were obtained from Autogen Bioclear UK Ltd. Wiltshire, UK ; . All other chemicals were purchased from Sigma. Animals--All experiments were undertaken in accordance with criteria outlined in a license granted under the Animals Scientific Procedures ; Act 1986 and approved by the Animal Ethics Committee of the University of Liverpool. Transgenic mice in which both the P1 and P2 genes were deleted GstP1 P2 and wild type GstP1 P2 mouse lines, on a 129 MF1 background, were generated and maintained as reported previously 26 ; . Determination of JNK Activity--JNK activity was determined using a stress-activated protein kinase JNK assay kit from New England Biolabs according to the manufacturer's instructions. Briefly, the kinase reaction was performed in the presence of excess ATP and was optimized for both time 30 min ; and protein concentration 1 mg of liver extract 0.6 mg of lung extract ; . Reactions without tissue extract were used as negative controls. Samples were electrophoresed on 12% polyacrylamide gels, and c-Jun phosphorylation was selectively measured using a phospho-c-Jun antibody, which specifically measures JNKcatalyzed phosphorylation of c-Jun at Ser-63. Phospho-c-Jun band volumes were quantified by band densitometry arbitrary units ; using UVISoftTM software UVITech UK ; and compared with that of the c-Jun protein band, which was visualized by staining the nitrocellulose membrane with Ponceau Red. Electrophoretic Mobility Shift Analysis--AP-1 DNA binding activity was determined by electrophoretic mobility shift analysis using a radiolabeled AP-1 consensus oligonucleotide. The double-stranded oligonucleotide containing the consensus AP-1 binding site underlined ; consisted of the following sequence: 5 -GCGTTGATGAGTCAGCCGGAA-3 . The double-stranded oligonucleotide containing a mutant AP-1 binding site underlined ; consisted of the following sequence: 5 -CGCTTGAGCTGTCAGCCGGAA-3 . Mouse hepatic or lung nuclear protein extractions were carried out as described previously 28 ; . Nuclear extracts 10 g ; from wild type or null mice n 4 ; were incubated with 35 fmol of [ -32P]ATP-labeled oligonucleotides for 20 min at room temperature in a final reaction volume of 10 l. Binding buffer contained 4% Ficoll, 20 mM HEPES pH 7.5 ; , 35 mM NaCl, 60 mM KCl, 0.01% Nonidet P-40, 2 mM dithiothreitol, and 0.5 g of poly dI-dC ; . For antibody supershift experiments, nuclear extracts pooled samples from null mice ; were incubated with 1 l of the corresponding antibody solution. DNA protein complexes were separated by electrophoresis on 5% polyacrylamide, 0.5 Tris borate EDTA gels, dried, and analyzed by autoradiography at 80 C with Kodak Biomax film Eastman Kodak Co. ; . AP-1 band volumes were quantified as described above. Determination of Nrf2 Nuclear Translocation--Hepatic Nrf2 nuclear translocation was determined by Western immunoblot analysis. Briefly, nuclear extracts 25 g ; were separated by electrophoresis on 7.5% SDS-polyacrylamide gels Bio-Rad ; and subsequently transferred to nitrocellulose membranes Sigma ; . After incubation in blocking buffer 10% fat-free milk in Tris-buffered saline pH 7.6 ; containing 0.15% Tween 20 ; for 1 h, the membrane was incubated with anti-Nrf2 antibody 1: 2000 in Tris-buffered saline Tween 20 containing 2% milk ; for 1 h. Following multiple washes with Tris-buffered saline Tween 20, the secondary antibody was added peroxidase-conjugated goat antirabbit IgG, 1: 2000 in Tris-buffered saline Tween 20 containing 2 and fortovase.
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