Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Mark-Jean Gnoth"'
Publikováno v:
Biochemical Journal. 477:4191-4206
The transport efficiency (TE) describes the performance of a transport protein for a specific substrate. To compare the TE of different transporters, the number of active transporters in the plasma membrane must be monitored, as it may vary for each
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47ca01afa12bd75e1fcd10357daa59c9
https://doi.org/10.1042/bcj20200666
https://doi.org/10.1042/bcj20200666
Autor:
Susanne Roehrig, Kersten Matthias Gericke, Simone Schulz, Roman C. Hillig, Mark Jean Gnoth, Philip Lienau, Martina Schaefer, Swen Allerheiligen, Alexander Hillisch, Adrian Tersteegen, Stefan Heitmeier, Vera Puetter
Publikováno v:
Journal of medicinal chemistry. 63(21)
Despite extensive research on small molecule thrombin inhibitors for oral application in the past decades, only a single double prodrug with very modest oral bioavailability has reached human therapy as a marketed drug. We have undertaken major effor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e2d18a51ea3eae07ccb9b49344caf4e
https://pubmed.ncbi.nlm.nih.gov/33108181
https://pubmed.ncbi.nlm.nih.gov/33108181
Publikováno v:
Bioanalysis. 7:2777-2787
Background: Nifurtimox is a 5-nitrofuran derived antiprotozoal drug used to treat diseases caused by trypanosomes including Chagas’ disease and sleeping sickness (African trypanosomiasis). Available methods for the determination of nifurtimox in pl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e76a55eb5acb531b2ed719e37e0eec88
https://doi.org/10.4155/bio.15.185
https://doi.org/10.4155/bio.15.185
Publikováno v:
Bioanalysis. 7:193-205
Background: Riociguat (BAY 63–2521) is an oral NO-independent as well as NO-synergistic stimulator of soluble guanylate cyclase (sGC) for the treatment of pulmonary hypertension. BAY 60–4552 (M-1) is its pharmacologically active major metabolite.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5661792d7a6670c1d941625b155c182
https://doi.org/10.4155/bio.14.257
https://doi.org/10.4155/bio.14.257
Autor:
Stefan Kiesgen, Thomas Schwarz, Manuela Braun, Oliver Czupalla, Armin Schröder, Mark Jean Gnoth, Joanna Grudzinska-Goebel
Publikováno v:
Bioanalysis. 8(24)
Determination of concentration–time profiles in cynomolgus monkeys of a therapeutic monoclonal antibody against a soluble target revealed a substantial discrepancy between a generic anti-human IgG capture/detection and target bridging assay with th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ace9751b893cdffe79dbf019f80b2069
https://pubmed.ncbi.nlm.nih.gov/27884079
https://pubmed.ncbi.nlm.nih.gov/27884079
Autor:
Andreas Ohm, Thomas Kuhlmann, Uwe Muenster, Christian Pelzetter, Thomas Backensfeld, Andreas H. Göller, Mark Jean Gnoth, Klemens Lustig, Susanne Greschat, Jörg Keldenich, Hartwig Mueller
Publikováno v:
European Journal of Pharmaceutics and Biopharmaceutics. 78:522-530
Low solubility of drug candidates generated in research contributes to their elimination during subsequent development due to insufficient oral bioavailability (BA) of crystalline compound. Therefore, the purpose of the study was to identify critical
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f2f0352fbbd8c0aaffb331814f6b38d
https://doi.org/10.1016/j.ejpb.2011.01.023
https://doi.org/10.1016/j.ejpb.2011.01.023
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 338:372-380
Rivaroxaban, an oral, direct factor Xa inhibitor, has a dual mode of elimination in humans, with two-thirds metabolized by the liver and one-third renally excreted unchanged. P-glycoprotein (P-gp) is known to be involved in the absorption, distributi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b95e4c7ab1606059e46af352f1025e2
https://doi.org/10.1124/jpet.111.180240
https://doi.org/10.1124/jpet.111.180240
Publikováno v:
Drug Metabolism and Disposition. 38:1341-1346
Sorafenib (Nexavar) is a novel oral Raf kinase and vascular endothelial growth factor receptor inhibitor. Most anticancer drugs are substrates for ATP-binding cassette efflux pumps especially for P-glycoprotein (P-gp). To evaluate the influence of P-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9807c041f795086bfd0713b3eb8e971b
https://doi.org/10.1124/dmd.110.032052
https://doi.org/10.1124/dmd.110.032052
Publikováno v:
Molecular Pharmaceutics. 6:326-336
We report here the generation and pharmacological characterization of a phosphodiesterase 2A (PDE2A) reporter cell line. Human PDE2A was stably transfected in a parental cell line expressing the atrial natriuretic peptide (ANP) receptor and the cycli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8eb9de7c87a249e4bead96f3a6cefe7f
https://doi.org/10.1021/mp800127n
https://doi.org/10.1021/mp800127n
Autor:
K Zimmermann, Heimo Ehmke, Heiner Apeler, Santiago Figueroa-Pérez, Mario Lobell, Mark-Jean Gnoth, Klaus Münter, J Lenz, Joachim Dr. Hütter, K H Augstein, Johannes-Peter Stasch, Hartmut Schirok, Andreas Knorr, J K Franz, Joachim Mittendorf, Raimund Kast
Publikováno v:
British Journal of Pharmacology. 152:1070-1080
Background and purpose: Rho-kinase (ROCK) has been implicated in the pathophysiology of altered vasoregulation leading to hypertension. Here we describe the pharmacological characterization of a potent, highly selective and orally active ROCK inhibit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b8f78bdb486662f3bfff261afb450ca8
https://doi.org/10.1038/sj.bjp.0707484
https://doi.org/10.1038/sj.bjp.0707484