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Rewinkel J Enthoven M Golstein I van der Rijst M Scholten A van Tilborg M de Weys D Wisse J Hamersma H 《Bioorganic & medicinal chemistry》2008,16(6):2753-2763
Recently, a new class (often referred to as SPRMs: selective progesterone receptor modulators) of progesterone receptor ligands with mixed agonist/antagonist properties has been described. Such compounds are envisaged, for example, as treatment for endometriosis, uterine fibroids, and leiomyomas. Existing SPRMs include Asoprisnil 1 and Uliprisnil acetate 2. In our hands, however, these compounds proved to have a predominantly or exclusively antagonistic in vitro profile, which may make this type of compound less attractive, for example, as contraceptives. We therefore aimed at a class of mixed-profile compounds that would show a more evenly balanced agonist/antagonist profile. A novel class of 11beta-[4-(heteroaryl)phenyl]-substituted pregnanes was identified that displayed the desired balance. Contrary to known SPRMs, this novel class of MPP (mixed-profile progestagen) was found to have a truly mixed activity, including a sizeable agonist component. 相似文献
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Anne S Rasmussen Henrik Lauridsen Christoffer Laustsen Bjarke G Jensen Steen F Pedersen Lars Uhrenholt Lene WT Boel Niels Uldbjerg Tobias Wang Michael Pedersen 《BMC physiology》2010,10(1):3
Background
In biomedical sciences, ex vivo angiography is a practical mean to elucidate vascular structures three-dimensionally with simultaneous estimation of intravascular volume. The objectives of this study were to develop a magnetic resonance (MR) method for ex vivo angiography and to compare the findings with computed tomography (CT). To demonstrate the usefulness of this method, examples are provided from four different tissues and species: the human placenta, a rice field eel, a porcine heart and a turtle. 相似文献6.
Paralogous origin of the red- and green-sensitive visual pigment genes in vertebrates 总被引:1,自引:0,他引:1
The nucleotide sequence of the red-sensitive visual pigment gene, R007Af,
in the fish Astyanax fasciatus, from the initiation codon to the stop codon
of this gene, including introns, is 1,592 bp, making it the shortest visual
pigment gene known in vertebrates. Analysis of this and other homologous
sequence data suggests that vertebrates initially had two duplicate genes
and that each ancestor of Astyanax, human, and chicken independently
duplicated the gene in the process of developing their red-green color
vision. Furthermore, many extant red-green colorblind organisms may be
explained simply by the failure of achieving very specific nucleotide
substitutions at the three codon positions 180, 277, and 285, rather than
by the lack of duplicate loci.
相似文献
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Unusual molecular evolution of an Adh pseudogene in Drosophila 总被引:2,自引:0,他引:2
Sullivan DT; Starmer WT; Curtiss SW; Menotti-Raymond M; Yum J 《Molecular biology and evolution》1994,11(3):443-458
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Supramolecular structures of peptide assemblies in membranes by neutron off-plane scattering: method of analysis 总被引:2,自引:1,他引:1
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In a previous paper (Yang et al., Biophys. J. 75:641-645, 1998), we showed a simple, efficient method of recording the diffraction patterns of supramolecular peptide assemblies in membranes where the samples were prepared in the form of oriented multilayers. Here we develop a method of analysis based on the diffraction theory of two-dimensional liquids. Gramicidin was used as a prototype model because its pore structure in membrane in known. At full hydration, the diffraction patterns of alamethicin and magainin are similar to gramicidin except in the scale of q (the momentum transfer of scattering), clearly indicating that both alamethicin and magainin form pores in membranes but of different sizes. When the hydration of the multilayer samples was decreased while the bilayers were still fluid, the in-plane positions of the membrane pores became correlated from one bilayer to the next. We believe that this is a new manifestation of the hydration force. The effect is most prominent in magainin patterns, which are used to demonstrate the method of analysis. When magainin samples were further dehydrated or cooled, the liquid-like diffraction turned into crystal-like patterns. This discovery points to the possibility of investigating the supramolecular structures with high-order diffraction. 相似文献
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Background
POU5F1 expression is required to maintain stem cell pluripotency and for primordial germ cells to retain proliferative capability in embryonic development. Recent evidence suggests that POU5F1 may also be a testicular germ cell carcinoma (TGCC) oncogene, and POU5F1 variation may influence TGCC risk. As an important first step to a genetic association study, we sought to identify all common sequence variants in an 11.3 kb region containing POU5F1, and to describe the linkage disequilibrium patterns, using DNA from individuals of African-descent (AD) and European-descent (ED).Results
A higher number of polymorphisms was observed in the AD (n = 102) versus ED (n = 82) population. Among the 41 observed haplotypes, 21 (51%) and 12 (29%) were unique to the AD and ED populations, respectively, while 8 (20%) were observed in both. The number of tagging polymorphisms necessary to explain at least 80% of common variation (minor allele frequency ≥ 0.10) due to the remaining untyped polymorphisms was 17 for an AD and 10 for an ED population, providing a 4.0- and 7.0-fold gain in genotyping efficiency for characterizing nucleotide variation, respectively.Conclusion
POU5F1 is highly polymorphic, however a smaller subset of polymorphisms can tag the observed genetic variation with little loss of information. 相似文献10.