Zobrazeno 1 - 10
of 287
pro vyhledávání: '"A H, Schinkel"'
Autor:
David Damoiseaux, Alfred H. Schinkel, Jos H. Beijnen, Alwin D. R. Huitema, Thomas P. C. Dorlo
Publikováno v:
Clinical and Translational Science, Vol 17, Iss 1, Pp n/a-n/a (2024)
Abstract First‐in‐human dose predictions are primarily based on no‐observed‐adverse‐effect levels in animal studies. Predictions from these animal models are only as effective as their ability to predict human results. To narrow the gap bet
Externí odkaz:
https://doaj.org/article/4492d5c59a174fd3b85d7757ccdc1918
Autor:
Changpei Gan, Jing Wang, Alejandra Martínez-Chávez, Michel Hillebrand, Niels de Vries, Joke Beukers, Els Wagenaar, Yaogeng Wang, Maria C. Lebre, Hilde Rosing, Sjoerd Klarenbeek, Rahmen Bin Ali, Colin Pritchard, Ivo Huijbers, Jos H. Beijnen, Alfred H. Schinkel
Publikováno v:
Acta Pharmaceutica Sinica B, Vol 13, Iss 2, Pp 618-631 (2023)
The mammalian carboxylesterase 1 (Ces1/CES1) family comprises several enzymes that hydrolyze many xenobiotic chemicals and endogenous lipids. To investigate the pharmacological and physiological roles of Ces1/CES1, we generated Ces1 cluster knockout
Externí odkaz:
https://doaj.org/article/87e193186c58427c9b561d417264b90f
Autor:
Wenlong Li, Dilek Iusuf, Rolf W. Sparidans, Els Wagenaar, Yaogeng Wang, Dirk R. de Waart, Margarida L.F. Martins, Stéphanie van Hoppe, Maria C. Lebre, Olaf van Tellingen, Jos H. Beijnen, Alfred H. Schinkel
Publikováno v:
Pharmacological Research, Vol 190, Iss , Pp 106724- (2023)
Organic anion transporting polypeptide 2B1 (OATP2B1/SLCO2B1) facilitates uptake transport of structurally diverse endogenous and exogenous compounds. To investigate the roles of OATP2B1 in physiology and pharmacology, we established and characterized
Externí odkaz:
https://doaj.org/article/f8d2c24093e5489fb6812b02a2a65cfa
Autor:
Joanne M. Donkers, Reinout L.P. Roscam Abbing, Michel van Weeghel, Johannes H.M. Levels, Anita Boelen, Alfred H. Schinkel, Ronald P.J. Oude Elferink, Stan F.J. van de Graaf
Publikováno v:
Cellular and Molecular Gastroenterology and Hepatology, Vol 10, Iss 3, Pp 451-466 (2020)
Background & Aims: Bile acids are important metabolic signaling molecules. Bile acid receptor activation promotes body weight loss and improves glycemic control. The incretin hormone GLP-1 and thyroid hormone activation of T4 to T3 have been suggeste
Externí odkaz:
https://doaj.org/article/947ce3d0a1cf41cdb360eb818de0b5b9
Autor:
Margarida L. F. Martins, Paniz Heydari, Wenlong Li, Alejandra Martínez-Chávez, Nikkie Venekamp, Maria C. Lebre, Luc Lucas, Jos H. Beijnen, Alfred H. Schinkel
Publikováno v:
Frontiers in Pharmacology, Vol 13 (2022)
The psychedelic alkaloid ibogaine is increasingly used as an oral treatment for substance use disorders, despite being unlicensed in most countries and having reported adverse events. Using wild-type and genetically modified mice, we investigated the
Externí odkaz:
https://doaj.org/article/42ec522121d9424fb99e7f0e402b71a9
Autor:
Jing Wang, M. Merve Susam, Changpei Gan, Rolf W. Sparidans, Maria C. Lebre, Jos H. Beijnen, Alfred H. Schinkel
Publikováno v:
Pharmaceuticals, Vol 15, Iss 9, p 1124 (2022)
EAI045 is a fourth-generation allosteric tyrosine kinase inhibitor (TKI) of the epidermal growth factor receptor (EGFR). It targets T790M and C797S EGFR mutants in the treatment of non-small cell lung cancer (NSCLC). EAI045 and cetuximab combined ind
Externí odkaz:
https://doaj.org/article/f35d28b40b0d4d2c8e00a50b67705a13
Autor:
David Damoiseaux, Wenlong Li, Alejandra Martínez-Chávez, Jos H. Beijnen, Alfred H. Schinkel, Alwin D. R. Huitema, Thomas P. C. Dorlo
Publikováno v:
Pharmaceuticals, Vol 15, Iss 7, p 860 (2022)
The extrapolation of drug exposure between species remains a challenging step in drug development, contributing to the low success rate of drug approval. As a consequence, extrapolation of toxicology from animal models to humans to evaluate safe, fir
Externí odkaz:
https://doaj.org/article/43a6e4f485c34a489be4e795886f503e
Autor:
Nancy H. C. Loos, Margarida L. F. Martins, Daniëlle de Jong, Maria C. Lebre, Matthijs Tibben, Jos H. Beijnen, Alfred H. Schinkel
Publikováno v:
Molecular Pharmaceutics. 20:2477-2489
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e89f95bc34496403afc2b407e4b0bae8
https://doi.org/10.1021/acs.molpharmaceut.2c01076
https://doi.org/10.1021/acs.molpharmaceut.2c01076
Autor:
Jeroen J. M. A. Hendrikx, Frederik E. Stuurman, Ji‐Ying Song, Vincent A. deWeger, Jurjen S. Lagas, Hilde Rosing, Jos H. Beijnen, Alfred H. Schinkel, Jan H. M. Schellens, Serena Marchetti
Publikováno v:
Pharmacology Research & Perspectives, Vol 8, Iss 4, Pp n/a-n/a (2020)
Abstract Oral administration of docetaxel in combination with the CYP3A4 inhibitor ritonavir is used in clinical trials to improve oral bioavailability of docetaxel. Diarrhea was the most commonly observed and dose‐limiting toxicity. This study com
Externí odkaz:
https://doaj.org/article/312864ef1c70464298e06dea8e715675
Autor:
Yaogeng Wang, Rolf W. Sparidans, Sander Potters, Rahime Şentürk, Maria C. Lebre, Jos H. Beijnen, Alfred H. Schinkel
Publikováno v:
Pharmaceuticals, Vol 14, Iss 11, p 1087 (2021)
Selpercatinib is a targeted, FDA-approved, oral, small-molecule inhibitor for the treatment of rearranged during transfection (RET) proto-oncogene mutation-positive cancer. Using genetically modified mouse models, we investigated the roles of the mul
Externí odkaz:
https://doaj.org/article/a3ac2265932f41afa84cd9b41d33fe43