Search results for "STING"
showing 10 items of 3756 documents
Identification of a Terphenyl Derivative that Blocks the Cell Cycle in the G0−G1 Phase and Induces Differentiation in Leukemia Cells
2006
To further explore the SAR of resveratrol-related trans-stilbene derivatives, here we describe the synthesis of (a) a series of 3,5-dimethoxy analogues in which a variety of substituents were introduced at positions 2', 3', 4', and 5' of the stilbene scaffold and (b) a second group of derivatives (2-phenylnaphthalenes and terphenyls) that incorporate a phenyl ring as a bioisosteric replacement of the stilbene alkenyl bridge. We thoroughly characterized all of the new compounds with respect to their apoptosis-inducing activity and their effects on the cell cycle. One of the new derivatives, 13g, behaved differently from the others, as it was able to block the cell cycle in the G(0)-G(1) phas…
Identification of N- and C-terminal Amino Acids of Lhca1 and Lhca4 Required for Formation of the Heterodimeric Peripheral Photosystem I Antenna LHCI-…
2002
Apoproteins of higher plant light-harvesting complexes (LHC) share considerable amino acid sequence identity/similarity. Despite this fact, they occur in different oligomeric states (i.e., monomeric, dimeric, and trimeric). As a step toward understanding the underlying structure requirements for different oligomerization behavior, we analyzed whether amino acids at the N- and C-termini of Lhca1 and Lhca4 are involved in the formation of the heterodimeric LHCI-730. Using altered proteins produced by deletion or site-directed mutagenesis for reconstitution, we were able to identify amino acids required for the assembly of LHCI-730. At the N-terminus of Lhca1, W4 is involved in heterodimerizat…
Barriers to rotation in ortho-substituted tertiary aromatic amides: Effect of chloro-substitution on resonance and distortion
2018
Planarity of the amide bond represents one of the most widely recognized properties of amides. Herein, we report a combined structural and computational study on the effect of ortho-substitution on resonance and barriers to rotation in tertiary aromatic amides. We demonstrate that ortho-chloro substitution in a class of benzamides that are important from the reactivity and medicinal chemistry perspective results in increased barriers to rotation around both the N-C(O) and C-C(O) axes. The effect of steric hindrance on structures, resonance energies, barriers to rotation, and proton affinities is discussed. The present study strongly supports the use of ortho-substitution in common benzamide…
Synthesis and structural characterisation of bulky heptaaromatic (hetero)aryl o-substituted s-aryltetrazines
2020
An expedient two-step synthesis produces in good yield polyaromatic heptacyclic (hetero)arylated o-substituted s-aryltetrazines (s-Tz) directly from diphenyl s-tetrazine. This methodology overcomes the steric limitations of classical Pinner-like syntheses encountered for o-functionalized s-Tz. A single step palladium-catalyzed N-directed C–H bond tetrahalogenation is followed by a Pd-catalyzed Suzuki (hetero)arylation that is achieved simultaneously on four sites. The single crystal X-ray diffraction structure of the resulting typical polyaromatic heptacyclic aromatic compound 3,6-bis(2,6-diphenyl)-1,2,4,5-tetrazine (3) is analyzed, together with R-functionalized peripheral phenyl derivativ…
Benzoannulated quinone-type electron acceptors: evolution of the molecular and electronic structures upon reduction
1998
Abstract The molecular and electronic structures of DCNQI and its π-extended derivatives benzo-DCNQI and DCAQI have been investigated using ab initio 6-31G ∗ calculations. The steric hindrance introduced by lateral benzoannulation determines the loss of planarity of the DCNQI moiety for DCAQI. The most stable conformation of DCAQI corresponds to a butterfly-type structure, in which the DCNQI ring adopts a boat conformation and the lateral benzene rings remain planar. This structure lies 2.75 kcal mol −1 below the fully planar conformation. MP2/6-31G ∗ calculations including full geometry optimization confirm the greater stability of the butterfly structure. The geometries of the anions and …
Prediction of Airport Pavement Moduli by Machine Learning Methodology Using Non-destructive Field Testing Data Augmentation
2022
For the purpose of the Airport Pavement Management System (APMS), in order to optimize the maintenance strategies, it is fundamental monitoring the pavement conditions’ deterioration with time. In this way, the most damaged areas can be detected and intervention can be prioritized. The conventional approach consists in performing non-destructive tests by means of a Heavy Weight Deflectometer (HWD). This equipment allows the measurement of the pavement deflections induced by a defined impact load. This is a quite expensive and time-consuming procedure, therefore, the points to be investigated are usually limited to the center points of a very large mesh grid. Starting from the measured defle…
Kopējo augšstilba artēriju hemodinamisko parametru maiņas unilaterālas pēc-oklūzijas hiperēmijas laikā
2016
Pēc pēdējiem literatūras datiem ir zināms, ka pastāv būtiskas atšķirības augšējo un apakšējo ekstremitāšu artēriju reakcijās. Neskatoties uz to, joprojām ir maz pētījumu par hemodinamisko parametru maiņām kāju maģistrālajās artērijās. Īpaši aktuāls ir jautājums par asins plūsmas lineārā ātruma profila komponentiem un to maiņām dažādos apstākļos. Tāpat joprojām nav vienota priekšstata par plūsmas-izraisītās dilatācijas (FMD) reakcijām un to regulācijas mehānismiem kopējās augšstilba artērijās (CFA), kā arī par lokālā stinguma maiņām pēc-oklūzijas reaktīvās hiperēmijas laikā. Darba mērķis ir novērtēt kopējo augšstilba artēriju hemodinamisko parametru maiņas unilaterālas distālas oklūzijas un …
Adaptive sparse representation of continuous input for tsetlin machines based on stochastic searching on the line
2021
This paper introduces a novel approach to representing continuous inputs in Tsetlin Machines (TMs). Instead of using one Tsetlin Automaton (TA) for every unique threshold found when Booleanizing continuous input, we employ two Stochastic Searching on the Line (SSL) automata to learn discriminative lower and upper bounds. The two resulting Boolean features are adapted to the rest of the clause by equipping each clause with its own team of SSLs, which update the bounds during the learning process. Two standard TAs finally decide whether to include the resulting features as part of the clause. In this way, only four automata altogether represent one continuous feature (instead of potentially h…
Balanced difficulty task finder: an adaptive recommendation method for learning tasks based on the concept of state of flow
2020
An adaptive task difficulty assignment method which we reckon as balanced difficulty task finder (BDTF) is proposed in this paper. The aim is to recommend tasks to a learner using a trade-off between skills of the learner and difficulty of the tasks such that the learner experiences a state of flow during the learning. Flow is a mental state that psychologists refer to when someone is completely immersed in an activity. Flow state is a multidisciplinary field of research and has been studied not only in psychology, but also neuroscience, education, sport, and games. The idea behind this paper is to try to achieve a flow state in a similar way as Elo’s chess skill rating (Glickman in Am Ches…
Compared Activity-Based Costing Case Studies in the Information System Departments of two Groups in France:A Strategic Management Accounting Approach
2010
International audience; This paper analyses the strategic management accounting concept with an instrumental point of view. We try to show in what extend the ABC developments could be included in a strategic approach of the management accounting and to test if the ABC is a relevant tool to drive the strategy. The first part synthesizes the strategic management accounting developments, which try to improve the Activity-Based Costing method. In the first part, we describe them using the Strategic Management Accounting stream, with a link with cost management and ABC. The second part exposes a taxonomy of the reasons why using the ABC method. In a third part, we confront our developments to th…