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排序方式: 共有4545条查询结果,搜索用时 18 毫秒
21.
C Martel L Provencher X Li A St Pierre G Leblanc S Gauthier Y Mérand F Labrie 《Canadian Metallurgical Quarterly》1998,64(3-4):199-205
Tamoxifen (TAM), the only antiestrogen currently available for the endocrine therapy of breast cancer behaves as a mixed agonist/antagonist of estrogen action, thus limiting its therapeutic potential. We report the binding characteristics of a novel series of nonsteroidal antiestrogens to the rat uterine estrogen receptor. As measured by competition studies, the affinity of EM-652, the active metabolite of the prodrug EM-800, for the estrogen receptor is 7-11 times higher than that of 17beta-estradiol (E2), ICI 182780, and hydroxy-tamoxifen (OH-TAM), the active metabolite of Tamoxifen. EM-652 is 20x more potent than ICI 164384 and Droloxifene while it is 400 times more potent than Toremifene in displacing [3H]E2 from the rat uterine estrogen receptor. On the other hand, the prodrug EM-800 and Tamoxifen have respectively 150-fold and 410-fold less affinity for the estrogen receptor than the pure antiestrogen EM-652. No significant binding of EM-652, EM-800, TAM or OH-TAM was observed to the rat uterine progesterone receptor at concentrations up to 10,000 nM except for TAM that caused a 50% displacement of labeled R5020 at 4000 nM. No significant binding of EM-652 or EM-800 was observed on the rat ventral prostate androgen receptor or the rat uterine progesterone receptor. The present data demonstrate the high affinity and specificity of the new antiestrogen, EM-652, for the rat uterine estrogen receptor. The antiestrogen EM-652 thus becomes the compound having the highest known affinity for the estrogen receptor. Due to its unique potency and its pure antiestrogenic activity already demonstrated in many systems, this antiestrogen could well offer an important advance for the endocrine therapy of breast cancer, uterine cancer, and other estrogen-sensitive diseases in women. 相似文献
22.
Lei Guo Lennart Ljung Pierre Priouret 《International Journal of Adaptive Control and Signal Processing》1993,7(6):525-537
An analysis is given of the performance of the standard forgetting factor recursive least squares (RLS) algorithm when used for tracking time-varying linear regression models. Three basic results are obtained: (1) the ‘P-matrix’ in the algorithm remains bounded if and only if the (time-varying) covariance matrix of the regressors is uniformly non-singular; (2) if so, the parameter tracking error covariance matrix is of the order O(μ + γ2/μ), where μ = 1 - λ, λ is the forgetting factor and γ is a quantity reflecting the speed of the parameter variations; (3) this covariance matrix can be arbitrarily well approximated (for small enough μ) by an expression that is easy to compute. 相似文献
23.
In this paper,an adaptive control scheme is introduced for permanent magnet synchronous machines (PMSMs)as an alternative to classical control techniques.The adaptive control strategy capitalizes on the machine’s inverse dynamics to achieve accurate tracking by using an observer to approximate disturbance in the form of friction and load torque.The controller’s output is then fed to a space vector pulse width modulation(SVPWM)algorithm to produce duty cycles for the inverter.The control scheme is validated through a set of simulations on an experimentally validated PMSM model.Results for different situations highlight its high speed tracking accuracy and high performance in compensating for friction and load disturbances of various magnitudes. 相似文献
24.
Computing scattering rates of electrons and phonons stands at the core of studies of electron transport properties. In the high field regime, the interactions between all electron bands with all phonon bands need to be considered. This full band interaction implies a huge computational burden in calculating scattering rates. In this study, a new accelerated algorithm is presented for this task, which speeds up the computation by two orders of magnitude (100 times) and dramatically simplifies the coding. At the same time, it visually demonstrates the physical process of scattering more clearly. 相似文献
25.
Murray S. Blum Ray F. Severson Richard F. Arrendale Douglas W. Whitman Pierre Escoubas Olushola Adeyeye Clive G. Jones 《Journal of chemical ecology》1990,16(1):223-244
Adults of a generalist herbivore, the lubber grasshopper,Romalea guttata, can be converted to functional specialists by feeding them exclusively on catnip,Nepeta cataria. No obvious adverse effects on adult development resulted from this enforced monophagy. Notwithstanding the fact thatR. guttata has had no coevolutionary relationship with this Eurasian mint, it readily sequesters compounds that are identical to or derived from the terpenoid lactones that are characteristic ofN. cataria. R. guttata appears to both biomagnify minor allelochemicals and to sequester metabolites of theNepeta terpenes in its paired defensive glands. The levels of autogenously produced phenolics are not affected by feeding onN. cataria and the defensive secretions of catnip-fed grasshoppers are more repellent to ants than those of wild-fed acridids. Metabolites of theN. cataria monoterpenes are sequestered in the defensive glands when catnip is added to the natural diet ofR. guttata. The ability of a generalist,R. guttata, to facilely bioaccumulate a potpourri of foreign allelochemicals when feeding in a specialist mode is analyzed in terms of its biochemical, physiological, and functional significance. Sequestration is examined as a response to the enteric effronteries represented by the phytochemicals that can be characteristic of the overload in a monophagous diet. 相似文献
26.
Corinne Leprince Eric Vivier Dominique Treton Pierre Galanaud Jacques Benveniste Yolande Richard Yolene Thomas 《Lipids》1991,26(12):1204-1208
The role of paf-acether (paf), a phospholipid cytokine, in the modulation of human B cell function was investigated. Paf,
from 1×10−5 M to 10−6 M, decreased B cell proliferation induced by both phorbol myristate acetate (PMA) and anti-IgM antibodies (anti-IgM Ab).
By contrast, 1×10−7 M to 1×10−9 M paf enhanced PMA triggered, but not anti-IgM triggered B cell proliferation. B cell proliferation was modulated between
24 and 72 hr of culture indicating that the effect of paf did not merely reflect a shift in proliferation kinetics. Interestingly,
paf also enhanced the spontaneous proliferation of a Burkitt lymphoma-derived B cell line, Raji, which suggests that paf can
directly act on B cells. The modulatory effect of paf on peripheral blood B cells was independent of PMA concentration, yet
the effect on Raji cells was dependent upon cell density. The data suggest that paf is a potent modulator of B cell function,
and may be involved in the control of humoral immune response.
Based on a paper presented at the Third International Conference on Platelet-Activating Factor and Structurally Related Alkyl
Ether Lipids, Tokyo, Japan, May 1989. 相似文献
27.
The paper gives a general survey of the factors contributing to the deactivation of metal catalysts employed in liquid phase reactions for the synthesis of fine or intermediate chemicals. The main causes of catalyst deactivation are particle sintering, metal and support leaching, deposition of inactive metal layers or polymeric species, and poisoning by strongly adsorbed species. Weakly adsorbed species, poisons at low surface coverage and solvents, may act as selectivity promoters or modifiers. Three examples of long term stability studies carried out in trickle-bed reactor (glucose to sorbitol hydrogenation on Ru/C catalysts, hydroxypropanal to 1,3-propanediol hydrogenation on Ru/TiO2 catalysts, and wet air oxidation of paper pulp effluents on Ru/TiO2) are discussed. 相似文献
28.
Racemic -methyl--n-propyl--propiolactone is readily polymerized with zinc and cadmium chiral glycolates leading to optically active polyesters. The stereoelectivities observed are lower than for oxiranes and thiiranes with the same initiator system. A value of rotatory power for pure enantiomer o, is deduced from NMR measurements in the presence of chiral solvent. The structure of polymers is discussed on the basis of NMR results. 相似文献
29.
30.
The problem of determining whether several finite automata accept a word in common is closely related to the well-studied membership problem in transformation monoids. We raise the issue of limiting the number of final states in the automata intersection problem. For automata with two final states, we show the problem to be \({\oplus}\)L-complete or NP-complete according to whether a nontrivial monoid other than a direct product of cyclic groups of order 2 is allowed in the automata. We further consider idempotent commutative automata and (Abelian, mainly) group automata with one, two, or three final states over a singleton or larger alphabet, elucidating (under the usual hypotheses on complexity classes) the complexity of the intersection nonemptiness and related problems in each case. 相似文献