Cloning and functional complementation of ten Schistosoma mansoni phosphodiesterases expressed in the mammalian host stages.

Autor: Jane C Munday, Stefan Kunz, Titilola D Kalejaiye, Marco Siderius, Susanne Schroeder, Daniel Paape, Ali H Alghamdi, Zainab Abbasi, Sheng Xiang Huang, Anne-Marie Donachie, Samia William, Abdel Nasser Sabra, Geert Jan Sterk, Sanaa S Botros, David G Brown, Charles S Hoffman, Rob Leurs, Harry P de Koning

Publikováno v: PLoS Neglected Tropical Diseases, Vol 14, Iss 7, p e0008447 (2020)

Only a single drug against schistosomiasis is currently available and new drug development is urgently required but very few drug targets have been validated and characterised. However, regulatory systems including cyclic nucleotide metabolism are em

Externí odkaz: https://doaj.org/article/dec44c4ba15a44afbe2fcc56f7a87eca

CCP4 Cloud for structure determination and project management in macromolecular crystallography

Autor: Eugene Krissinel, Andrey A. Lebedev, Ville Uski, Charles B. Ballard, Ronan M. Keegan, Oleg Kovalevskiy, Robert A. Nicholls, Navraj S. Pannu, Pavol Skubák, John Berrisford, Maria Fando, Bernhard Lohkamp, Marcin Wojdyr, Adam J. Simpkin, Jens M. H. Thomas, Christopher Oliver, Clemens Vonrhein, Grzegorz Chojnowski, Arnaud Basle, Andrew Purkiss, Michail N. Isupov, Stuart McNicholas, Edward Lowe, Josep Triviño, Kevin Cowtan, Jon Agirre, Daniel J. Rigden, Isabel Uson, Victor Lamzin, Ivo Tews, Gerard Bricogne, Andrew G. W. Leslie, David G. Brown

Nowadays, progress in the determination of three-dimensional macromolecular structures from diffraction images is achieved partly at the cost of increasing data volumes. This is due to the deployment of modern high-speed, high-resolution detectors, t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70211be538eb43722afb9f6169aea790
https://eprints.soton.ac.uk/471374/

Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors

Autor: Erik de Heuvel, Abhimanyu K. Singh, Ewald Edink, Tiffany van der Meer, Melanie van der Woude, Payman Sadek, Mikkel P. Krell-Jørgensen, Toine van den Bergh, Johan Veerman, Guy Caljon, Titilola D. Kalejaiye, Maikel Wijtmans, Louis Maes, Harry P. de Koning, Geert Jan Sterk, Marco Siderius, Iwan J.P. de Esch, David G. Brown, Rob Leurs

Publikováno v: Bioorganic and Medicinal Chemistry, 27(18), 3998-4012. Elsevier Limited
de Heuvel, E, Singh, A K, Edink, E, van der Meer, T, van der Woude, M, Sadek, P, Krell-Jørgensen, M P, van den Bergh, T, Veerman, J, Caljon, G, Kalejaiye, T D, Wijtmans, M, Maes, L, de Koning, H P, Jan Sterk, G, Siderius, M, de Esch, I J P, Brown, D G & Leurs, R 2019, ' Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors ', Bioorganic and Medicinal Chemistry, vol. 27, no. 18, pp. 3998-4012 . https://doi.org/10.1016/j.bmc.2019.06.027

Several 3',5'-cyclic nucleotide phosphodiesterases (PDEs) have been validated as good drug targets for a large variety of diseases. Trypanosoma brucei PDEB1 (TbrPDEB1) has been designated as a promising drug target for the treatment of human African

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7977de212c1b702b8e7a0a91b90f42f3
https://doi.org/10.1016/j.bmc.2019.06.027

Phenyldihydropyrazolones as Novel Lead Compounds Against Trypanosoma cruzi

Autor: Julianna Siciliano de Araújo, Louis Maes, Maria de Nazaré Correia Soeiro, Ignacio Cotillo, Iwan J. P. de Esch, Payman Sadek, Geert Jan Sterk, Stefan Kunz, Julio Martin, An Matheeussen, David G. Brown, Kristina M. Orrling, Marco Siderius, Ewald Edink, Susanne Schroeder, Hans Custers, Rob Leurs, Tiffany van de Meer, Maarten Sijm

Publikováno v: ACS Omega, Vol 4, Iss 4, Pp 6585-6596 (2019)
Sijm, M, Siciliano De Araújo, J, Kunz, S, Schroeder, S, Edink, E, Orrling, K M, Matheeussen, A, Van De Meer, T, Sadek, P, Custers, H, Cotillo, I, Martin, J J, Siderius, M, Maes, L, Brown, D G, De Nazaré Correia Soeiro, M, Sterk, G J, De Esch, I J P & Leurs, R 2019, ' Phenyldihydropyrazolones as Novel Lead Compounds Against Trypanosoma cruzi ', ACS Omega, vol. 4, no. 4, pp. 6585-6596 . https://doi.org/10.1021/acsomega.8b02847
ACS Omega, 4(4), 6585-6596. American Chemical Society
ACS Omega

As over 6 million people are infected with Chagas disease and only limited therapeutic options are available, there is an urgent need for novel drugs. The involvement of cyclic nucleotide phosphodiesterases (PDE) in the lifecycle and biological fitne

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9b5cce81802b5be7a51d2cb1a2a422c
https://doaj.org/article/10294135fb574185889e0e6a6942218f

Talin Rod Domain Containing Protein 1 (TLNRD1) is a novel actin-bundling protein which promotes filopodia formation

Autor: York-Christoph Ammon, Alana R Cowell, Johanna Ivaska, David G. Brown, Anna Akhmanova, A.K. Singh, Guillaume Jacquemet, Benjamin T. Goult

Publikováno v: BioRxiv

Talin is a mechanosensitive adapter protein which couples integrins to the cytoskeleton and regulates integrin-mediated adhesion. Talin rod domain-containing protein-1 (TLNRD1) shares 22% homology with the R7R8 domains of talin, and is highly conserv

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9e5b477c6875e2daec5fa95c8eb8251
https://kar.kent.ac.uk/81343/1/2020_Cowell_BioRxiv.pdf