Development of Plate Reader and On-Line Microfluidic Screening to Identify Ligands of the 5-Hydroxytryptamine Binding Protein in Venoms

Autor: Reka A. Otvos, Janaki Krishnamoorthy Iyer, René van Elk, Chris Ulens, Wilfried M. A. Niessen, Govert W. Somsen, R. Manjunatha Kini, August B. Smit, Jeroen Kool

Publikováno v: Toxins, Vol 7, Iss 7, Pp 2336-2353 (2015)

The 5-HT3 receptor is a ligand-gated ion channel, which is expressed in the nervous system. Its antagonists are used clinically for treatment of postoperative- and radiotherapy-induced emesis and irritable bowel syndrome. In order to better understan

Externí odkaz: https://doaj.org/article/0bcd8222bddc492cb2f1aad3e6d57a63

Miniaturized bioaffinity assessment coupled to mass spectrometry for guided purification of bioactives from toad and cone snail

Autor: Sybren S. Wijmenga, Ruud L. E. G. Aspers, Jenny I. Halff, René van Elk, Reka A. Otvos, Andreas W. Ehlers, Richard J. Lewis, Ferry Heus, Wilfried M. A. Niessen, Sébastien Dutertre, Jeroen Kool, August B. Smit

Publikováno v: Biology
Biology, MDPI 2014, 3 (1), pp.139-156. ⟨10.3390/biology3010139⟩
Biology, 3, 1, pp. 139-156
Heus, F A H, Otvos, R A, Aspers, R L E G, van Elk, R, Halff, J I, Ehlers, A W, Duterte, S, Lewis, R J, Wijmenga, S, Smit, A B, Niessen, W M A & Kool, J 2014, ' Miniaturized bioactivity assessment coupled to mass spectrometry for guided purification of bioactives from toad and cone snail ', Biology, vol. 3, pp. 139-156 . https://doi.org/10.3390/biology3010139
Biology, 3, 139-156. Multidisciplinary Digital Publishing Institute (MDPI)
Biology; Volume 3; Issue 1; Pages: 139-156
Biology, 3, 139-156
Biology, Vol 3, Iss 1, Pp 139-156 (2014)

A nano-flow high-resolution screening platform, featuring a parallel chip-based microfluidic bioassay and mass spectrometry coupled to nano-liquid chromatography, was applied to screen animal venoms for nicotinic acetylcholine receptor like (nAChR) a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca403a753e3c96642a854645b6c89308
https://doi.org/10.3390/biology3010139

Structural Characterization of Binding Mode of Smoking Cessation Drugs to Nicotinic Acetylcholine Receptors through Study of Ligand Complexes with Acetylcholine-binding Protein*

Autor: August B. Smit, Prakash Rucktooa, Titia K. Sixma, Claire A. Haseler, René van Elk, Timothy Gallagher

Publikováno v: Journal of Biological Chemistry; Vol 287
Rucktooa, P, Haseler, C A, van Elk, R, Smit, A B, Gallagher, T & Sixma, T K 2012, ' Structural characterization of binding mode of smoking cessation drugs to nicotinic acetylcholine receptors through study of ligand complexes with acetylcholine-binding protein ', Journal of Biological Chemistry, vol. 287, no. 28, pp. 23283-23293 . https://doi.org/10.1074/jbc.M112.360347
The Journal of Biological Chemistry
Journal of Biological Chemistry, 287(28), 23283-23293. American Society for Biochemistry and Molecular Biology Inc.

Background: Cytisine and varenicline are smoking cessation drugs binding to nicotinic receptors (nAChRs). Results: We studied crystal structures of cytisine and varenicline with AChBP and analyzed binding of α4β2-like or α7-like AChBP mutants to c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f376ba82b7b29112a46d7838163f493

Crystal structures of a cysteine-modified mutant in loop D of acetylcholine-binding protein

Autor: Marijke Brams, Elaine A. Gay, José Colón Sáez, Albert Guskov, René van Elk, Roel C. van der Schors, Steve Peigneur, Jan Tytgat, Sergei V. Strelkov, August B. Smit, Jerrel L. Yakel, Chris Ulens

Publikováno v: Journal of Biological Chemistry; Vol 286
Journal of Biological Chemistry, 286(6), 4420-4428. American Society for Biochemistry and Molecular Biology Inc.
Brams, M, Gay, E A, Sáez, J C, Guskov, A, van Elk, R, van der Schors, R C, Peigneur, S, Tytgat, J, Strelkov, S V, Smit, A B, Yakel, J L & Ulens, C 2011, ' Crystal Structures of a Cysteine-modified Mutant in Loop D of Acetylcholine-binding Protein ', Journal of Biological Chemistry, vol. 286, no. 6, pp. 4420-4428 . https://doi.org/10.1074/jbc.M110.188730

Covalent modification of alpha 7 W55C nicotinic acetylcholine receptors (nAChR) with the cysteine-modifying reagent [2-(trimethylammonium) ethyl] methanethiosulfonate (MTSET+) produces receptors that are unresponsive to acetylcholine, whereas methyl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c76e953d44fa94263daa90ad32d0faed

Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. In silico docking, pharmacological screening, and X-ray analysis

Autor: August B. Smit, Aldo Jongejan, René van Elk, Daniel Bertrand, Anastassis Perrakis, Sonia Bertrand, C. Ulens, Titia K. Sixma, Atilla Akdemir, Iwan J. P. de Esch, Rob Leurs

Publikováno v: Journal of Medicinal Chemistry, 52, 2372-2383. American Chemical Society
Ulens, C, Akdemir, A, Jongejan, A, van Elk, R, Bertrand, S, Perrakis, A, Leurs, R, Smit, A B, Sixma, T K, Bertrand, D & de Esch, I J P 2009, ' Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. In silico docking, pharmacological screening, and X-ray analysis ', Journal of Medicinal Chemistry, vol. 52, pp. 2372-2383 . https://doi.org/10.1021/jm801400g

Acetylcholine binding protein (AChBP) is widely considered as a functional and structural homologue of the ligand binding domain of Cys-loop receptors. We report the use of AChBP as template to identify ligands for the nicotinic receptors (nAChRs). A

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aae79e03b7735382f17f387f26cb271f
https://doi.org/10.1021/jm801400g