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21.
Snyder LB Meng Z Mate R D'Andrea SV Marinier A Quesnelle CA Gill P DenBleyker KL Fung-Tomc JC Frosco M Martel A Barrett JF Bronson JJ 《Bioorganic & medicinal chemistry letters》2004,14(18):4735-4739
A series of potential antimicrobial derivatives possessing bioisosteric replacements for the central oxazolidinone ring found in oxazolidinone antibacterials have been prepared. The design concept involved replacement of the requisite sp(3)-hybridized stereogenic center found at the 5-position of the oxazolidinone with a nitrogen atom. The synthesis and antibacterial activity of three such ring systems, the benzisoxazolinones, pyrroles, and isoxazolinones is described. 相似文献
22.
Nantermet PG Barrow JC Newton CL Pellicore JM Young M Lewis SD Lucas BJ Krueger JA McMasters DR Yan Y Kuo LC Vacca JP Selnick HG 《Bioorganic & medicinal chemistry letters》2003,13(16):2781-2784
A series of potent and selective proline- and pyrazinone-based macrocyclic thrombin inhibitors is described. Detailed SAR studies led to the incorporation of specific functional groups in the tether that enhanced functional activity against thrombin and provided exquisite selectivity against trypsin and tPA. X-ray crystallography and molecular modeling studies revealed the inhibitor-enzyme interactions responsible for this selectivity. 相似文献
23.
CXCR4 and CCR5 Genetic Polymorphisms in Long-Term Nonprogressive Human Immunodeficiency Virus Infection: Lack of Association with Mutations other than CCR5-Δ32
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Oren J. Cohen Stefania Paolucci Steven M. Bende MaryBeth Daucher Hiroyuki Moriuchi Masako Moriuchi Claudia Cicala Richard T. Davey Jr. Barbara Baird Anthony S. Fauci 《Journal of virology》1998,72(7):6215-6217
Polymorphisms in the coding sequences of CCR5 and CXCR4 were studied in a group of human immunodeficiency virus (HIV)-infected long-term nonprogressors. Two different point mutations were found in the CXCR4 coding sequence. One of these CXCR4 mutations was silent, and each was unique to two nonprogressors. The well-described 32-bp deletion within the CCR5 coding sequence (CCR5-Δ32) was found in 4 of 13 nonprogressors, and 12 different point mutations were found scattered over the CCR5 coding sequence from 8 nonprogressors. Most of the mutations created either silent or conservative changes in the predicted amino acid sequence: only one of these mutations was found in more than a single nonprogressor. All nonsilent mutations were tested in an HIV envelope-dependent fusion assay, and all functioned comparably to wild-type controls. Polymorphisms in the CXCR4 and CCR5 coding sequences other than CCR5-Δ32 do not appear to play a dominant mechanistic role in nonprogression among HIV-infected individuals. 相似文献
24.
Elvio Pinto Bosetti Yngve Grahn Rodrigo Scalise Horodyski Paula Mendlowicz Mauller Pierre Breuer Carolina Zabini 《Pal?ontologische Zeitschrift》2011,85(1):49-65
An earliest Givetian “Lilliput Effect” at Sítio Wolff and São Bento in the Paraná Basin occurred after an extinction event, possibly related to the latest Eifelian KA?ÁK Event. The Malvinokaffric fauna was reduced from 65 genera before the extinction event to eight genera after the event. However, the abundance of the individual taxa is high. The size reduction of the surviving taxa was up to 90%. The palynomorphs during the extinction and post-extinction (“Lilliput Effect”) events are scarce. Normal palynomorph abundance and diversity is restored later in the early Givetian immediately after the post-extinction event. The relictual fauna in the beds with the “Lilliput Effect” at Sítio Wolff and São Bento constitute the last survivors of the classical Malvinokaffric shelly fauna in the Paraná Basin, and are at these sites mixed with immigrants and alien elements (e.g. orthoconic nautiloids). 相似文献
25.
Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1)
Nantermet PG Barrow JC Lundell GF Pellicore JM Rittle KE Young M Freidinger RM Connolly TM Condra C Karczewski J Bednar RA Gaul SL Gould RJ Prendergast K Selnick HG 《Bioorganic & medicinal chemistry letters》2002,12(3):319-323
The synthesis and biological evaluation of a series of nonpeptidic small molecule antagonists of the human platelet thrombin receptor (PAR-1) are described. Optimization of the 5-amino-3-arylisoxazole lead resulted in an approximate 100-fold increase in potency. The most potent of these compounds (54) inhibits platelet activation with IC(50)s of 90 nM against the thrombin receptor agonist peptide (TRAP) and 510 nM against thrombin as the agonist. Further, antagonist 54 fully blocks platelet aggregation stimulated by 1 nM thrombin for 10 min. 相似文献
26.
Santella RM Gammon M Terry M Senie R Shen J Kennedy D Agrawal M Faraglia B Zhang F 《Mutation research》2005,592(1-2):29-35
It is well established that the initiating event in chemical carcinogenesis is the binding of reactive carcinogens to DNA. Thus, a number of analytic methods have been developed for determining levels of carcinogen-DNA adducts in humans as a marker of individual exposure and, potentially, of risk for cancer development. We have developed monoclonal and polyclonal antibodies to carcinogen-DNA adducts and highly sensitive ELISA and immunohistochemical assays for determining levels of adducts in human tissues. These methods have been combined with genotyping and phenotyping methods for DNA repair to study gene-environment interactions in cancer risk. Recent studies on breast cancer have utilized two large biorepositories. The first is blood and tumor tissues collected as part of the Long Island Breast Cancer Study Project, a population-based case-control study of environmental risk factors. The second is the Metropolitan New York Registry of Breast Cancer Families, one of six sites funded by the National Cancer Institute as a part of the Breast Cooperative Family Registry (CFR). Analysis of samples from these two studies have demonstrated the utility of measurement of DNA adducts as biomarkers of exposure and that DNA repair capacity, measured by genotyping or phenotyping, can influence risk. 相似文献
27.
Maxwell RA Welch WH Horodyski FM Schegg KM Schooley DA 《The Journal of biological chemistry》2002,277(24):21882-21890
The gene sequence of Manduca sexta juvenile hormone diol kinase (JHDK) codes for an enzyme that has 59% sequence identity to Drosophila melanogaster sarcoplasmic calcium-binding protein-2 (dSCP2). JHDK and dSCP2 are similar to G-proteins with three conserved sequence elements involved in purine nucleotide binding. Both proteins contain two pairs of EF-hand motifs. Characterization and partial purification of the D. melanogaster homolog of M. sexta JHDK from adult D. melanogaster gave material with JHDK activity. This activity has an experimental pI and molecular mass that are nearly identical to those of dSCP2. Moreover, D. melanogaster phosphotransferase activity has very similar chromatographic retention in three systems compared with M. sexta JHDK. Substrate docking to three-dimensional models of JHDK has shown that the three conserved nucleotide-binding elements surround the putative substrate-binding site and align with conserved sequence elements of p21(Ras) and adenylate kinase. D. melanogaster dSCP2 is a homolog of M. sexta JHDK, and these proteins constitute a novel kinase family that binds nucleotides using the scaffold of an SCP (Protein Data Bank code ). 相似文献
28.
Bryan P. Conrad Matthew Rappé MaryBeth Horodyski Kevin W. Farmer Peter A. Indelicato 《Cell and tissue banking》2013,14(3):359-366
One major concern regarding soft tissue allograft use in surgical procedures is the risk of disease transmission. Current techniques of tissue sterilization, such as irradiation have been shown to adversely affect the mechanical properties of soft tissues. Grafts processed using Biocleanse processing (a proprietary technique developed by Regeneration Technologies to sterilize human tissues) will have better biomechanical characteristics than tissues that have been irradiated. Fifteen pairs of cadaveric Achilles tendon allografts were obtained and separated into three groups of 10 each. Three treatment groups were: Biocleanse, Irradiated, and Control (untreated). Each specimen was tested to determine the biomechanical properties of the tissue. Specimens were cyclically preloaded and then loaded to failure in tension. During testing, load, displacement, and optical strain data were captured. Following testing, the cross sectional area of the tendons was determined. Tendons in the control group were found to have a higher extrinsic stiffness (slope of the load–deformation curve, p = .005), have a higher ultimate stress (force/cross sectional area, p = .006) and higher ultimate failure load (p = .003) than irradiated grafts. Biocleanse grafts were also found to be stiffer than irradiated grafts (p = .014) yet were not found to be statistically different from either irradiated or non-irradiated grafts in terms of load to failure. Biocleanse processing seems to be a viable alternative to irradiation for Achilles tendon allografts sterilization in terms of their biomechanical properties. 相似文献
29.
Joseph G. Wasser Daniel C. Herman MaryBeth Horodyski Jason L. Zaremski Brady Tripp Phillip Page Kevin R. Vincent Heather K. Vincent 《Trials》2017,18(1):630