Zobrazeno 1 - 10
of 435
pro vyhledávání: '"Adriaan P, IJzerman"'
Autor:
Daniela Digles, Alvaro Ingles-Prieto, Vojtech Dvorak, Tamara A. M. Mocking, Ulrich Goldmann, Andrea Garofoli, Evert J. Homan, Alberto Di Silvio, Lucia Azzollini, Francesca Sassone, Mario Fogazza, Felix Bärenz, Antje Pommereau, Yasmin Zuschlag, Jasper F. Ooms, Jeppe Tranberg-Jensen, Jesper S. Hansen, Josefina Stanka, Hubert J. Sijben, Helena Batoulis, Eckhard Bender, Riccardo Martini, Adriaan P. IJzerman, David B. Sauer, Laura H. Heitman, Vania Manolova, Juergen Reinhardt, Alexander Ehrmann, Philipp Leippe, Gerhard F. Ecker, Kilian V. M. Huber, Thomas Licher, Lia Scarabottolo, Tabea Wiedmer, Giulio Superti-Furga
Publikováno v:
Frontiers in Pharmacology, Vol 15 (2024)
With over 450 genes, solute carriers (SLCs) constitute the largest transporter superfamily responsible for the uptake and efflux of nutrients, metabolites, and xenobiotics in human cells. SLCs are associated with a wide variety of human diseases, inc
Externí odkaz:
https://doaj.org/article/d3ca8f18dbc2476ea3722a966b570ca6
Autor:
Tamara A. M. Mocking, Wieke M. van Oostveen, Jacobus P. D. van Veldhoven, Hugo Minnee, Cynthia M. Fehres, Charles E. Whitehurst, Adriaan P. IJzerman, Laura H. Heitman
Publikováno v:
Frontiers in Pharmacology, Vol 15 (2024)
The prostaglandin transporter (PGT, SLCO2A1) mediates transport of prostanoids (a.o. prostaglandin E2 (PGE2)) into cells and thereby promotes their degradation. Overexpression of PGT leads to low extracellular PGE2 levels and has been linked to impai
Externí odkaz:
https://doaj.org/article/e0cc08e3ad25430fb31c87cdf54e7ca2
Autor:
Marina Gorostiola González, Remco L. van den Broek, Thomas G. M. Braun, Magdalini Chatzopoulou, Willem Jespers, Adriaan P. IJzerman, Laura H. Heitman, Gerard J. P. van Westen
Publikováno v:
Journal of Cheminformatics, Vol 15, Iss 1, Pp 1-19 (2023)
Abstract Proteochemometric (PCM) modelling is a powerful computational drug discovery tool used in bioactivity prediction of potential drug candidates relying on both chemical and protein information. In PCM features are computed to describe small mo
Externí odkaz:
https://doaj.org/article/1a3bbdb4d14241b5a95862590f309cd3
Autor:
Marina Gorostiola González, Hubert J. Sijben, Laura Dall’ Acqua, Rongfang Liu, Adriaan P. IJzerman, Laura H. Heitman, Gerard J. P. van Westen
Publikováno v:
Frontiers in Molecular Biosciences, Vol 10 (2023)
Glutamate is an essential excitatory neurotransmitter and an intermediate for energy metabolism. Depending on the tumor site, cancer cells have increased or decreased expression of excitatory amino acid transporter 1 or 2 (EAAT1/2, SLC1A3/2) to regul
Externí odkaz:
https://doaj.org/article/db6bd9e55f7a43348580c6357b600742
Publikováno v:
Journal of Cheminformatics, Vol 15, Iss 1, Pp 1-14 (2023)
Abstract Rational drug design often starts from specific scaffolds to which side chains/substituents are added or modified due to the large drug-like chemical space available to search for novel drug-like molecules. With the rapid growth of deep lear
Externí odkaz:
https://doaj.org/article/12e2403ede4e4bc28f5d4d15dd0d5517
Autor:
Marina Gorostiola González, Pepijn R. J. Rakers, Willem Jespers, Adriaan P. IJzerman, Laura H. Heitman, Gerard J. P. van Westen
Publikováno v:
International Journal of Molecular Sciences, Vol 25, Iss 7, p 3698 (2024)
Cancer remains a leading cause of mortality worldwide and calls for novel therapeutic targets. Membrane proteins are key players in various cancer types but present unique challenges compared to soluble proteins. The advent of computational drug disc
Externí odkaz:
https://doaj.org/article/3fa34ac451034cf5b0ad007a8dfa1c00
Autor:
Xuhan Liu, Kai Ye, Herman W. T. van Vlijmen, Michael T. M. Emmerich, Adriaan P. IJzerman, Gerard J. P. van Westen
Publikováno v:
Journal of Cheminformatics, Vol 13, Iss 1, Pp 1-15 (2021)
Abstract In polypharmacology drugs are required to bind to multiple specific targets, for example to enhance efficacy or to reduce resistance formation. Although deep learning has achieved a breakthrough in de novo design in drug discovery, most of i
Externí odkaz:
https://doaj.org/article/0871ce20cd084c358f772f94aba024a5
Autor:
Xuesong Wang, Willem Jespers, Rubén Prieto-Díaz, Maria Majellaro, Adriaan P. IJzerman, Gerard J. P. van Westen, Eddy Sotelo, Laura H. Heitman, Hugo Gutiérrez-de-Terán
Publikováno v:
Scientific Reports, Vol 11, Iss 1, Pp 1-10 (2021)
Abstract The four adenosine receptors (ARs) A1AR, A2AAR, A2BAR, and A3AR are G protein-coupled receptors (GPCRs) for which an exceptional amount of experimental and structural data is available. Still, limited success has been achieved in getting new
Externí odkaz:
https://doaj.org/article/e3d7468f1f4048819ea81f585f212118
Autor:
Hubert J. Sijben, Wieke M. van Oostveen, Peter B. R. Hartog, Laura Stucchi, Andrea Rossignoli, Giovanna Maresca, Lia Scarabottolo, Adriaan P. IJzerman, Laura H. Heitman
Publikováno v:
Scientific Reports, Vol 11, Iss 1, Pp 1-14 (2021)
Abstract The human norepinephrine transporter (NET) is an established drug target for a wide range of psychiatric disorders. Conventional methods that are used to functionally characterize NET inhibitors are based on the use of radiolabeled or fluore
Externí odkaz:
https://doaj.org/article/f31bd47fc7a84a55966bc22ad396c6be
Autor:
Hubert J. Sijben, Laura Dall’ Acqua, Rongfang Liu, Abigail Jarret, Eirini Christodoulaki, Svenja Onstein, Gernot Wolf, Simone J. Verburgt, Sylvia E. Le Dévédec, Tabea Wiedmer, Giulio Superti-Furga, Adriaan P. IJzerman, Laura H. Heitman
Publikováno v:
Frontiers in Pharmacology, Vol 13 (2022)
Excitatory amino acid transporters (EAAT/SLC1) mediate Na+-dependent uptake of extracellular glutamate and are potential drug targets for neurological disorders. Conventional methods to assess glutamate transport in vitro are based on radiolabels, fl
Externí odkaz:
https://doaj.org/article/3013a65420c249ca84a2b5a7b907dc82