排序方式: 共有22条查询结果,搜索用时 638 毫秒
1.
David R. Bauman Alan Whitehead Lisa C. Contino Jisong Cui Margarita Garcia-Calvo Xin Gu Nancy Kevin Xiuying Ma Lee-yuh Pai Kashmira Shah Xiaolan Shen Sloan Stribling Hratch J. Zokian Joe Metzger Diane E. Shevell Sherman T. Waddell 《Bioorganic & medicinal chemistry letters》2013,23(12):3650-3653
In an effort to understand the origin of blood-pressure lowering effects observed in recent clinical trials with 11β-HSD1 inhibitors, we examined a set of 11β-HSD1 inhibitors in a series of relevant in vitro and in vivo assays. Select 11β-HSD1 inhibitors reduced blood pressure in our preclinical models but most or all of the blood pressure lowering may be mediated by a 11β-HSD1 independent pathway. 相似文献
2.
Eleanor Burnett Tenneth Dalipanda Divi Ogaoga Jenny Gaiofa Gregory Jilini Alison Halpin Vance Dietz Kashmira Date Eric Mintz Terri Hyde Kathleen Wannemuehler Catherine Yen 《PLoS neglected tropical diseases》2016,10(8)
BackgroundIn response to a 2011 cholera outbreak in Papua New Guinea, the Government of the Solomon Islands initiated a cholera prevention program which included cholera disease prevention and treatment messaging, community meetings, and a pre-emptive cholera vaccination campaign targeting 11,000 children aged 1–15 years in selected communities in Choiseul and Western Provinces.ConclusionsThis pre-emptive OCV campaign in a cholera-naïve community provided a unique opportunity to assess household-level knowledge, attitudes, and practices regarding diarrhea, cholera, and water, sanitation, and hygiene (WASH). Our findings suggest that education provided during the vaccination campaign may have reinforced earlier mass messaging about cholera and diarrheal disease in vaccinated communities. 相似文献
3.
Verma Urja Kashmira Khaire Suresh Balakrishnan Gowri Kumari Uggini 《In vitro cellular & developmental biology. Animal》2018,54(10):756-769
Chick embryonic cells can be used to develop an easy and economical in vitro model for conducting studies on the disease muscle dystrophy (MD). For this, the limb myoblasts from 11th day chick embryo were isolated and cultured. To this muscle cell culture, anti-dystroglycan antibody (IIH6) was added so as to target the α-dystroglycan and disrupt the connection between the cytoskeletal proteins and the extracellular matrix (which is a characteristic feature of MD). Cells were allowed to differentiate further and the morphometrics and mRNA expression were studied. The IIH6-treated muscle cells displayed changes in morphometry, contractibility, and also atrophy was observed when compared to the control cultures. Concomitant gene expression studies showed an upregulation in TGF-β expression, while the muscle sculpture genes MYOD1, MYF5, LAMA2 and MYOG were downregulated resembling the MD in vivo. This simple and cost-effective method can be useful in studies to further understand the disease mechanism and also in conducting initial studies on effect of novel pharmacological agents. 相似文献
4.
5.
Doherty GA Yang GX Borges E Tong S McCauley ED Treonz KM Van Riper G Pacholok S Si Q Koo GC Shah K Mumford RA Hagmann WK 《Bioorganic & medicinal chemistry letters》2003,13(11):1891-1895
A series of isonicotinoyl-(L)-aminophenylalanine derivatives was prepared and evaluated as VLA-4 antagonists. These compounds exhibit subnanomolar binding affinity to VLA-4 and significant off-rates. The interplay between off-rate, protein binding and pharmacokinetics is discussed. 相似文献
6.
Camacho RE Wnek R Shah K Zaller DM O'Reilly RJ Collins N Fitzgerald-Bocarsly P Koo GC 《Cellular immunology》2004,232(1-2):86-95
A HLA-DR1 transgenic mouse (NOD/scid-DR1) was derived by breeding the existing B10.M/J-[Tg]DR1 mouse with the NOD/scid mouse. The intention was to enhance engraftment of human T cells by providing human class II elements in the tissues. Thymus and spleen fragments from adult NOD/scid-DR1 mice were transplanted under the syngeneic kidney capsules, followed by injection of human cord blood mononuclear cells (CBMNC) into transplanted tissues. FACS analyses showed that human T and B cells were consistently detected in the peripheral blood and spleen, of the chimeric mice. An average of 20% of human cells was found in the spleen and the engrafted thymus/spleen tissues. Furthermore, human cells from these tissues could proliferate with anti-human CD3 antibody and these mice could generate humoral and cellular responses to allogeneic human cells. Cytokines, such as IL-10, GMCSF, IFN-gamma, and TNF-alpha were also detected in the supernatants of the cultured human cells from the chimeric mice, when they were stimulated with allogeneic cells. Therefore, a novel mouse model with functional circulating human T and B cells was established that would facilitate the exploration of vaccine, the disease processes of autoimmunity, HIV infection, and human cancer. 相似文献
7.
Bao J Miao S Kayser F Kotliar AJ Baker RK Doss GA Felix JP Bugianesi RM Slaughter RS Kaczorowski GJ Garcia ML Ha SN Castonguay L Koo GC Shah K Springer MS Staruch MJ Parsons WH Rupprecht KM 《Bioorganic & medicinal chemistry letters》2005,15(2):447-451
Kv1.3, the voltage-gated potassium channel in human T cells, represents a new target for treating immunosuppression and autoimmune diseases. Correolide (1), a pentacyclic natural product, is a potent and selective Kv1.3 channel blocker. Simplification of correolide via removal of its E-ring generates enone 4, whose modification produced a new series of tetracyclic Kv1.3 blockers. The structure-activity relationship for this class of compounds in two functional assays, Rb_Kv and human T cell proliferation, is presented herein. The most potent analog 43 is 15-fold more potent than correolide as inhibitor of human T cell proliferation. 相似文献
8.
Rajapandian Kanagaraj Miguel B. Araujo Rathin Barman Priya Davidar Rahul De Dinesh K. Digal G. V. Gopi A. J. T. Johnsingh Kashmira Kakati Stephanie Kramer‐Schadt Babu R. Lamichhane Salvador Lyngdoh M. D. Madhusudan Muneer Ul Islam Najar Jyotirmayee Parida Narendra M. B. Pradhan Jean‐Philippe Puyravaud R. Raghunath P. P. Abdul Rahim K. Muthamizh Selvan Naresh Subedi Antonio Trabucco Swati Udayraj Thorsten Wiegand Amirtharaj C. Williams Surendra P. Goyal 《Diversity & distributions》2019,25(5):822-838
9.
Miao S Bao J Garcia ML Goulet JL Hong XJ Kaczorowski GJ Kayser F Koo GC Kotliar A Schmalhofer WA Shah K Sinclair PJ Slaughter RS Springer MS Staruch MJ Tsou NN Wong F Parsons WH Rupprecht KM 《Bioorganic & medicinal chemistry letters》2003,13(6):1161-1164
The voltage-gated potassium channel, Kv1.3, is present in human T-lymphocytes. Blockade of Kv1.3 results in T-cell depolarization, inhibition of T-cell activation, and attenuation of immune responses in vivo. A class of benzamide Kv1.3 channel inhibitors has been identified. The structure-activity relationship within this class of compounds in two functional assays, Rb_Kv and T-cell proliferation, is presented. In in vitro assays, trans isomers display moderate selectivity for binding to Kv1.3 over other Kv1.x channels present in human brain. 相似文献
10.
Aster SD Graham DW Kharbanda D Patel G Ponpipom M Santorelli GM Szymonifka MJ Mundt SS Shah K Springer MS Thieringer R Hermanowski-Vosatka A Wright SD Xiao J Zokian H Balkovec JM 《Bioorganic & medicinal chemistry letters》2008,18(9):2799-2804
3-Aryl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). They are active in both in vitro and an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented. 相似文献