Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Lars Fogh Iversen"'
Publikováno v:
PPAR Research, Vol 2008 (2008)
Despite clinical promise, dual-acting activators of PPARαandγ(here termed PPARα+γagonists) have experienced high attrition rates in preclinical and early clinical development, due to toxicity. In some cases, discontinuation was due to carcinogeni
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8cf7658545abe7d18a10b617b4628edb
https://doi.org/10.1155/2008/103167
https://doi.org/10.1155/2008/103167
Autor:
Torben S. Guldberg, Peter R. Brinck, Inger Thorup, Anne Charlotte Hegelund, Marianne B. Jensen, Ulla K. Thinggaard, Ingrid Sjögren, Henriette S. Nielsen, Lars Fogh Iversen, Martin B. Oleksiewicz, Hanne V. Andersen, Lis Jørgensen
Publikováno v:
Toxicologic Pathology. 33:552-560
Some developmental dual-acting PPARα/γ agonists, such as ragaglitazar, have shown carcinogenic effects in the rodent urinary bladder urothelium after months-years of dosing. We examined early (precancerous) changes in the bladder urothelium of rats
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7c61986d6c55074d8bf062939d91022
https://doi.org/10.1080/01926230500214657
https://doi.org/10.1080/01926230500214657
Autor:
Martin B. Oleksiewicz, Frederikke Lihme Egerod, Inger Thorup, T. Storgaard, Lars Fogh Iversen, Henriette S. Nielsen
Publikováno v:
Biomarkers. 10:295-309
Small-molecule agonists of the peroxisome proliferator-activated receptor (PPAR) alpha and gamma isoforms (dual-acting PPAR agonists) can cause urothelial cancers in rodents. Rats were dosed orally for 16 days with bladder carcinogenic (ragaglitazar)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d09768b3467ca0722b475c1db6a19b28
https://doi.org/10.1080/13547500500218682
https://doi.org/10.1080/13547500500218682
Autor:
Jette S. Kastrup, Lars Fogh Iversen, Karin Bach Møller, Günther H.J. Peters, Anja K. Pedersen
Publikováno v:
Acta Crystallographica Section D Biological Crystallography. 60:1527-1534
Protein tyrosine phosphatase 1B (PTP1B) plays a key role as a negative regulator of insulin and leptin signalling and is therefore considered to be an important molecular target for the treatment of type 2 diabetes and obesity. Detailed structural in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::923b859cecd36fbefd8063a37f93439b
https://doi.org/10.1107/s0907444904015094
https://doi.org/10.1107/s0907444904015094
Publikováno v:
Journal of Medicinal Chemistry. 47:3537-3545
Inhibition of glycogen phosphorylase (GP) has attracted considerable attention during the last five to 10 years as a means of treating the elevated hepatic glucose production seen in patients with type 2 diabetes. Several different GP inhibitors bind
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c681e2253b2d6b8dcf037c5b9e27a3c7
https://doi.org/10.1021/jm031121n
https://doi.org/10.1021/jm031121n
Autor:
Karin Bach Møller, Niels Møller, Lars Fogh Iversen, Frank U. Axe, Anja K. Pedersen, Ole Hvilsted Olsen, Ida Katrine Lund, Michael J. Newman, Yu Ge, Henrik Sune Andersen, Daniel D. Holsworth
Publikováno v:
Journal of Biological Chemistry. 279:24226-24235
Protein-tyrosine phosphatases (PTPs) are considered important therapeutic targets because of their pivotal role as regulators of signal transduction and thus their implication in several human diseases such as diabetes, cancer, and autoimmunity. In p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a32dc28ebde358d9c0d4f76afde8e960
https://doi.org/10.1074/jbc.m313027200
https://doi.org/10.1074/jbc.m313027200
Autor:
K.B. Moller, Ana K. Pedersen, H.S. Andersen, Lars Fogh Iversen, Niels Møller, Günther H.J. Peters, Xiao Ling Guo, S.B. Mortensen, Jette S. Kastrup, Zhong Yin Zhang
Publikováno v:
Biochemical Journal. 378:421-433
Previous enzyme kinetic and structural studies have revealed a critical role for Asp181 (PTP1B numbering) in PTP (protein-tyrosine phosphatase)-mediated catalysis. In the E-P (phosphoenzyme) formation step, Asp181 functions as a general acid, while i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b04569d3493b164e3d4566929e354be2
https://doi.org/10.1042/bj20030565
https://doi.org/10.1042/bj20030565
Autor:
Lars Fogh Iversen, Niels Møller, Kirsten M. Klausen, Karin Bach Møller, Sven Branner, Anja K. Pedersen, H.Sune Andersen, Steen B. Mortensen
Publikováno v:
Journal of Chromatography B. 799:1-8
Our structure-based drug discovery program within the field of protein-tyrosine phosphatases (PTPs) demands delivery of significant amounts of protein with extraordinary purity specifications over prolonged time periods. Hence, replacement of classic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b68ae3023a3edc5fb02b8b522a9ca76
https://doi.org/10.1016/j.jchromb.2003.09.040
https://doi.org/10.1016/j.jchromb.2003.09.040
Autor:
Günther H.J. Peters, Thomas M. Frimurer, Ole Hvilsted Olsen, Henrik Sune Andersen, Lars Fogh Iversen, Niels Møller
Publikováno v:
Biophysical Journal. 84(4):2273-2281
A computational docking strategy using multiple conformations of the target protein is discussed and evaluated. A series of low molecular weight, competitive, nonpeptide protein tyrosine phosphatase inhibitors are considered for which the x-ray cryst
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03c14a84f84a498b0c2129e5fb67569b
Autor:
Klaus A. Rytved, Lars Fogh Iversen, Steen H. Ingwersen, Michael P. Andersen, Yvonne Petersen, Benedicte Kiehr
Publikováno v:
European Journal of Drug Metabolism and Pharmacokinetics. 27:203-212
We investigated the use of non-linear mixed effects modeling in two preclinical studies of the glycogen phosphorylase inhibitor 1,4-dideoxy-1,4-imino-D-arabinitol (DAB). In a 28-day repeated-dose toxicity study rats were dosed once daily p.o. with 0,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e900acae623cec4f46e2daaf0b8510e0
https://doi.org/10.1007/bf03190459
https://doi.org/10.1007/bf03190459