8,540 research outputs found
Bock, Nils (Universität Münster)
No full textName/Nom: Bock Vorname/Prénom: Nils Titel/Fonction: M.A. Universität/Université: Westfälische Wilhelms-Universität Münster Forschungseinrichtung/Institution de recherche: Historisches Seminar Mittelalterliche Geschichte Email/Couriel: [email protected] Adresse/Adresse: Historisches Seminar, Domplatz 20-22, D-48143 Münster Homepage/Site Internet: http://www.uni-muenster.de/Geschichte/histsem/MA-G/L1/Personen/Bock/ Gewünschte Kooperationen/Coopérations souhaitées: Tagungen; Gem..
Bock, Nils (Universität Münster)
No full textName/Nom: Bock Vorname/Prénom: Nils Titel/Fonction: M.A. Universität/Université: Westfälische Wilhelms-Universität Münster Forschungseinrichtung/Institution de recherche: Historisches Seminar Mittelalterliche Geschichte Email/Couriel: [email protected] Adresse/Adresse: Historisches Seminar, Domplatz 20-22, D-48143 Münster Homepage/Site Internet: http://www.uni-muenster.de/Geschichte/histsem/MA-G/L1/Personen/Bock/ Gewünschte Kooperationen/Coopérations souhaitées: Tagungen; Gem..
Die Entführung aus dem Serail
No full textIn Musik gesetzt von W.A. MozartKV 384Vorlageform der Veröffentlichungsangabe: Berlin, chez Ed. Bote & G. Bock. G. Bock, Editeur de musique de S. Maj. le Roi et de S.A.R. le Prince Albert de Prusse. ; Ladenpreis 4 Thlr. 13 Sgr. Subscr.-Pr. 1 Thlr. 20 Sgr.Bibliographischer Nachweis: nicht in RISM A/I ; Hofmeister XIXLithographie (Titelblatt), Plattendruck (Notenteil)Text deutsch und italienisc
G. Bock & P. Thane, eds., Maternity and Gender Policies. Women and the Rise of the European Welfare States, 1880s- 1950s
No full textBrenes Anayansi Correa, Brandao Puppin Andréa. G. Bock & P. Thane, eds., Maternity and Gender Policies. Women and the Rise of the European Welfare States, 1880s- 1950s. In: L'Homme, 1996, tome 36 n°140. pp. 122-123
Dynamic ligand binding of dualsteric (allosteric/orthosteric) molecular probes controls the graded activation of muscarinic acetylcholine receptors
No full textWe investigated a class of bitopic (dualsteric) ligands of the M2 acetylcholine muscarinic receptor (M2AChR), i.e. compounds whose pharmacophoric groups are able to target the orthosteric as well as the allosteric binding site of the receptor.1,2 These model derivatives are composed of an allosteric fragment, an intermediate linker and an orthosteric moiety. As an example, ligands 1 and 2 incorporate the molecular portion of the allosteric compound Naphmethonium and the potent muscarinic agonist Iperoxo, which are connected by a flexible or a rigidified spacer group, respectively (Figure 1). These bipharmacophoric molecular probes were found to switch between two different binding orientations, resulting in both active and inactive populations of receptors bound by a given ligand, a behavior that has been termed dynamic ligand binding.3
Figure 1
In this study, pharmacological data analysis and computational simulations based on active and inactive M2AChR crystal structures led to identify two distinct binding topographies in a group of dualsteric partial agonists. One binding mode, which resembled that of the co-crystallized orthosteric ligand Iperoxo, engendered an agonist response. Conversely, dualsteric ligands binding to the allosteric site only showed a receptor-complex comparable to that of allosteric modulators. Thus, the observed agonist efficacies depended on the fraction of dualsteric (i.e. active) vs. purely allosteric (i.e. inactive) binding modes.4
References
1. Antony, J.; Kellershon, K.; Mohr-Andrä, M.; Kebig, A.; Prilla, S.; Muth, M.; Heller, E.; Disingrini, T.; Dallanoce, C.; Bertoni, S.; Schrobang, J.; Tränkle, C.; Kostenis, E.; Christopoulos, A.; Höltje, H.-D.; Barocelli, E.; De Amici, M.; Holzgrabe, U.; Mohr, K. FASEB J. 2009, 23, 442-450.
2. Bock, A.; Merten, N.; Schrage, R.; Dallanoce, C.; Bätz, J.; Klöckner, J.; Schmitz, J.; Matera, C.; Simon, K.; Kebig, A.; Peters, L.; Müller, A.; Schrobang-Ley, J.; Tränkle, C.; Hoffmann, C.; De Amici, M.; Holzgrabe, U.; Kostenis, E.; Mohr; K. Nat. Commun. 2012, 3:1044, doi: 10.1038/ncomms2028.
3. Bock, A.; Chirinda, B.; Krebs, F.; Messerer, R.; Bätz, J.; Muth, M.; Dallanoce, C.; Klingenthal, D.; Tränkle, C.; Hoffmann, C.; De Amici, M.; Holzgrabe, U.; Kostenis, E.; Mohr, K. Nat. Chem. Biol. 2014, 10, 18-20.
4. Bock, A.; Bermudez, M.; Krebs, F.; Matera, C.; Chirinda, B.; Sydow, D.; Dallanoce, C.; Holzgrabe, H.; De Amici, M.; Lohse, M.; Wolber, G.; Mohr, K. J. Biol. Chem., in press
Mass communication review year book 1980/ G. Cleveland Wilhait; Harold de Bock
No full text751 hal.; 24 c
Molecular rigidity in dualsteric agonists affects signaling bias of the muscarinic M2 acetylcholine receptor
No full textFor the human M2 muscarinic receptor the crystal structures in the active [1] and the inactive [2] conformation are available. Both structures suggest a low tolerance of the receptor protein towards spatial restriction between the allosteric and the orthosteric binding site.
Dualsteric compounds consist of covalently linked moieties that address the orthosteric and the allosteric binding site, respectively. Thus, it is possible to constrain receptor flexibility.
In a previous study, it was found that dualsteric compounds such as iper-6-naph, in which the orthosteric and allosteric moiety are linked via a hexamethylene chain, show biased signaling (i.e. a preference for Gi over Gs signaling) [3].
Here we present new dualsteric ligands, which due to their molecular properties should further restrict conformational transitions of the receptor. Surprisingly, signaling bias was abolished. These unexpected findings will be discussed in our poster.
[1] Haga K. et al.: Nature 2012
[2] Kruse A. et al.: Nature 2013
[3] Bock A. et al.: Nat Chem Biol. 201
Influence of methylphenidate on brain development--an update of recent animal experiments.
Get PDFGrund T, Lehmann K, Bock N, Rothenberger A, Teuchert-Noodt G. Influence of methylphenidate on brain development--an update of recent animal experiments. Behav Brain Funct. 2006;2(1): 2.Methylphenidate (MPH) is the most commonly used drug to treat attention deficit/hyperactivity disorder (ADHD) in children effectively and safely. In spite of its widespread application throughout one of the most plastic and sensitive phases of brain development, very little is known to date about its long-term effects on brain structure and function. Hence, this short review updates the influence of MPH on brain development, since recent human and animal studies suggest that MPH alters the dopaminergic system with long-term effects beyond the termination of treatment.Animal studies imply that the effects of MPH may depend on the neural responder system: Whereas structural and functional parameters are improved by MPH in animals with psychomotor impairments, they remain unaltered or get worse in healthy controls. While recent behavioural studies do not fully support such a differential effect of MPH in ADHD, the animal studies certainly prompt for further investigation of this issue. Furthermore, the abuse of MPH, when (rarely) intravenously applied, may even impair the maturation of dopaminergic fibres in subcortical brain areas. This argues for careful clinical assessment and diagnostics of ADHD symptomatology not only in conjunction with the prescription of MPH. Hence, one should be assured that MPH is only given to children with clear ADHD symptomatology leading to psychosocial impairment. The animal data suggest that under these conditions MPH is supportive for brain development and the related behaviour in children with ADHD
Illustrations de l'Opéra L'Africaine De G. Meyerbeer
Get PDFILLUSTRATIONS DE L'OPÉRA L'AFRICAINE DE G. MEYERBEER
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