Zobrazeno 1 - 10
of 252
pro vyhledávání: '"Alfred H, Schinkel"'
Autor:
Jamie Rijmers, Irene A. Retmana, Viët Bui, Davinia Arguedas, Maria C. Lebre, Rolf W. Sparidans, Jos H. Beijnen, Alfred H. Schinkel
Publikováno v:
Biomedicine & Pharmacotherapy, Vol 175, Iss , Pp 116720- (2024)
Opnurasib (JDQ443) is a newly developed oral KRASG12C inhibitor, with a binding mechanism distinct from the registered KRASG12C inhibitors sotorasib and adagrasib. Phase I and II clinical trials for opnurasib in NSCLC are ongoing. We evaluated the ph
Externí odkaz:
https://doaj.org/article/aee126997e694d2fb3116e085d0ab755
Autor:
Wenlong Li, Rolf W. Sparidans, Yaogeng Wang, Margarida L.F. Martins, Dirk R. de Waart, Olaf van Tellingen, Ji-Ying Song, Maria C. Lebre, Stéphanie van Hoppe, Els Wagenaar, Jos H. Beijnen, Alfred H. Schinkel
Publikováno v:
Biomedicine & Pharmacotherapy, Vol 175, Iss , Pp 116644- (2024)
Transmembrane drug transporters can be important determinants of the pharmacokinetics, efficacy, and safety profiles of drugs. To investigate the potential cooperative and/or counteracting interplay of OATP1A/1B/2B1 uptake transporters and ABCB1 and
Externí odkaz:
https://doaj.org/article/397facf01d244b2c89255b44205a2de9
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:
Nancy H.C. Loos, Irene A. Retmana, Jamie Rijmers, Yaogeng Wang, Changpei Gan, Maria C. Lebre, Rolf W. Sparidans, Jos H. Beijnen, Alfred H. Schinkel
Publikováno v:
Biomedicine & Pharmacotherapy, Vol 166, Iss , Pp 115304- (2023)
Adagrasib (Krazati™) is the second FDA-approved specific KRASG12C inhibitor for non-small cell lung cancer (NSCLC) patients harboring this mutation. The impact of the drug efflux transporters ABCB1 and ABCG2, and the drug-metabolizing enzymes CYP3A
Externí odkaz:
https://doaj.org/article/d1dc8905ed1b43a4a3acf85b155c81d5
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:
Changpei Gan, Jing Wang, Yaogeng Wang, Alejandra Martínez-Chávez, Michel Hillebrand, Niels de Vries, Joke Beukers, Maria C. Lebre, Els Wagenaar, Hilde Rosing, Sjoerd Klarenbeek, Onno B. Bleijerveld, Ji-Ying Song, Maarten Altelaar, Jos H. Beijnen, Alfred H. Schinkel
Publikováno v:
Biomedicine & Pharmacotherapy, Vol 164, Iss , Pp 114956- (2023)
Mammalian carboxylesterase 1 enzymes can hydrolyze many xenobiotic chemicals and endogenous lipids. We here identified and characterized a mouse strain (FVB/NKI) in which three of the eight Ces1 genes were spontaneously deleted, removing Ces1c and Ce
Externí odkaz:
https://doaj.org/article/6feb859d901d4d4c97531a2a7f1a6338
Publikováno v:
Biomedicine & Pharmacotherapy, Vol 162, Iss , Pp 114636- (2023)
Ritonavir, originally developed as HIV protease inhibitor, is widely used as a booster in several HIV pharmacotherapy regimens and more recently in Covid-19 treatment (e.g., Paxlovid). Its boosting capacity is due to the highly potent irreversible in
Externí odkaz:
https://doaj.org/article/03dab517f99548f4ada0fff17f17f4f8
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:
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:
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