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1.
Enantiomeric Cyclic Peptides with Different Caco‐2 Permeability Suggest Carrier‐Mediated Transport 下载免费PDF全文
B. Sc. Eduard Puig Prof. Dr. Beat Ernst Prof. Dr. Horst Kessler 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(22):8023-8027
Recently, oral absorption of cyclic hexapeptides was improved by N‐methylation of their backbone amides. However, the number and position of N‐methylations or of solvent exposed NHs did not correlate to intestinal permeability, measured in a Caco‐2 model. In this study, we investigate enantiomeric pairs of three polar and two lipophilic peptides to demonstrate the participation of carrier‐mediated transporters. As expected, all the enantiomeric peptides exhibited identical lipophilicity (logD7.4) and passive transcellular permeability determined by the parallel artificial membrane permeability assay (PAMPA). However, the enantiomeric polar peptides exhibited different Caco‐2 permeability (Papp) in both directions a–b and b–a. The same trend was observed for one of the lipophilic peptide, whereas the second lipophilic enantiomer pair showed identical Caco‐2 permeability (within the errors). These findings provide the first evidence for the involvement of carrier‐mediated transport for peptides, especially for those of polar nature. 相似文献
2.
Michel Weber 《Transactions of the American Mathematical Society》2006,358(2):911-936
We apply a majorizing measure theorem of Talagrand to obtain uniform bounds for sums of random variables satisfying increment conditions of the type considered in Gál-Koksma Theorems. We give some applications.
3.
O. Kortner M.P. Locher V.E. Markushin P. Weber O. Wigger 《The European Physical Journal C - Particles and Fields》2002,25(3):353-360
We study correlations in the exclusive reaction at rest with complete reconstruction of the kinematics for each event. The inclusive distribution is fairly flat at small
invariant mass of the pion pair while a small enhancement in the double differential distribution is observed for small invariant
masses of both pion pairs. Dynamical models with resonances in the final state are shown to be consistent with the data while
the stochastic HBT mechanism is not supported by the present findings.
Received: 26 February 2002 / Revised version: 22 July 2002 / Published online: 30 August 2002 相似文献
4.
Horst Guido Müller 《Colloid and polymer science》1941,96(1):11-19
Zusammenfassung Einige charakteristische ?nderungen physikalischer Werkstoffeigenschaften beim heterogenen Zerfall übers?ttigter Mischkristalle
werden am Beispiel der fl?chenzentrierten Eisen-Nickel-Kupfer-Legierungen beschrieben. Bei der Behandlung des Einflusses der
Ausscheidungsvorg?nge auf die Rekristallisationserscheinungen tritt die Bedeutung des übers?ttigungsgrades der zerfallenden
festen L?sung für den Ablauf dieser Zustands?nderungen besonders klar zutage. Kritische Stadien der Ausscheidung und der Koagulation
der heterogenen Phasen sind bei diesen Legierungen für die Erzeugung besonders hochwertiger magnetischer Eigenschaften verantwortlich.
Der vorliegende Bericht wurde von Herrn Prof., Dr. Wo. Ostwald angeregt. Für das diesem Arbeitsgebiet entgegengebrachte Interesse
m?chte ich Herrn Prof. Ostwald meinen besten Dank aussprechen. 相似文献
5.
Michel Weber 《Results in Mathematics》2005,47(3-4):340-354
Under a very moderate assumption on the Fourier coefficients of a periodic function, we show the convergence almost everywhere of the sequence of averages of its associated Riemann sums. The structure of the set of averages is analyzed by proving a spectral regularization type inequality, which allows to control the corresponding Littlewood-Paley square function. 相似文献
6.
Kerstin Paech Adrian Dumitru Jürgen Schaffner-Bielich Stefan Schramm Horst Stöcker Gebhard Zeeb Detlef Zschiesche 《Acta Physica Hungarica A》2004,21(2-4):151-156
The measured particle ratios in central heavy-ion collisions are investigated within a chemical and thermal equilibrium chiral SU(3) σ?ω approach. Contrary to the commonly adopted non-interacting gas calculations, the chiral SU(3) model predicts modified effective hadron masses and effective chemical potentials in the medium and a transition to a chirally restored phase at high temperatures or chemical potentials. the influence of three different types of phase transitions is investigated. We show that the deduced freeze-out values considerably depend on the underlying model while the quality of the fit is approximately the same. 相似文献
7.
Kenneth Weber Vilmar Trevisan Luiz Felipe Martins 《Journal of Algorithms in Cognition, Informatics and Logic》2005,54(2):152-167
This paper describes the first algorithm to compute the greatest common divisor (GCD) of two n-bit integers using a modular representation for intermediate values U, V and also for the result. It is based on a reduction step, similar to one used in the accelerated algorithm [T. Jebelean, A generalization of the binary GCD algorithm, in: ISSAC '93: International Symposium on Symbolic and Algebraic Computation, Kiev, Ukraine, 1993, pp. 111–116; K. Weber, The accelerated integer GCD algorithm, ACM Trans. Math. Softw. 21 (1995) 111–122] when U and V are close to the same size, that replaces U by (U−bV)/p, where p is one of the prime moduli and b is the unique integer in the interval (−p/2,p/2) such that . When the algorithm is executed on a bit common CRCW PRAM with O(nlognlogloglogn) processors, it takes O(n) time in the worst case. A heuristic model of the average case yields O(n/logn) time on the same number of processors. 相似文献
8.
The association of complex formation with static quenching in CT systems was investigated. Evaluation of the data made evident
that the inner filter effect must be allowed for. Time-resolved and temperature-dependent stationary measurements of fluorescence
led to the separation of dynamic and static quenching components. The static quenching constant is discussed with respect
to the equilibrium constant of complex formation determined by absorption spectroscopy. 相似文献
9.
10.
Horst Szambien 《Results in Mathematics》1992,22(1-2):619-621