Results 31 to 40 of about 425,696 (264)

The stability and robustness of metabolic states: identifying stabilizing sites in metabolic networks

Molecular Systems Biology, 2007
The dynamic behavior of metabolic networks is governed by numerous regulatory mechanisms, such as reversible phosphorylation, binding of allosteric effectors or temporal gene expression, by which the activity of the participating enzymes can be adjusted to the functional requirements of the cell.
Grimbs, S., Selbig, J., Bulik, S., Holzhuetter, H., Steuer, R.   +4 more
openaire   +4 more sources

MetStabOn—Online Platform for Metabolic Stability Predictions [PDF]

International Journal of Molecular Sciences, 2018
Metabolic stability is an important parameter to be optimized during the complex process of designing new active compounds. Tuning this parameter with the simultaneous maintenance of a desired compound’s activity is not an easy task due to the extreme complexity of metabolic pathways in living organisms.
Sabina Podlewska, Rafał Kafel
openaire   +2 more sources

Pharmacokinetic interaction of saxagliptin with andrographolide and their hypoglycemic effect in type 2 diabetes rats [PDF]

Acta Poloniae Pharmaceutica, 2023
Controlling blood glucose is the primary therapeutic strategy for T2DM. Both saxagliptin and andrographolide possess hypoglycemic effects, which makes the combination easy.
Suyan Wu, Haifei Pan, Yingying Huang
doaj   +1 more source

Quantitative Determination of 5-Aminoisoquinoline, a PARP-1 Inhibitor by UPLC-MS/MS: In Silico ADME Profile and In Vitro Metabolic Stability Study

Applied Sciences, 2022
5-Aminoisoquinoline (5-AIQ) is a water-soluble, potent and selective Poly (ADP-ribose) polymerase 1 (PARP-1) inhibitor, widely used as a biochemical and pharmacological tool to study the inhibitory effect of PARPs enzyme.
Muzaffar Iqbal, Essam A. Ali, Mohd Abul Kalam, Sheikh F. Ahmad, Rashad Al-Salahi   +4 more
doaj   +1 more source

Cold Acclimation Favors Metabolic Stability in Drosophila suzukii [PDF]

Frontiers in Physiology, 2018
The invasive fruit fly pest, Drosophila suzukii, is a chill susceptible species, yet it is capable of overwintering in rather cold climates, such as North America and North Europe, probably thanks to a high cold tolerance plasticity. Little is known about the mechanisms underlying cold tolerance acquisition in D. suzukii. In this study, we compared the
Thomas Enriquez, David Renault, David Renault, Maryvonne Charrier, Hervé Colinet   +4 more
openaire   +6 more sources

Novel 4-Acrylamido-Quinoline Derivatives as Potent PI3K/mTOR Dual Inhibitors: The Design, Synthesis, and in vitro and in vivo Biological Evaluation

Frontiers in Chemistry, 2019
A novel structural series of quinoline derivatives were designed, synthesized and biologically evaluated as PI3K/mTOR dual inhibitors upon incorporation of C-4 acrylamide fragment.
Xiaodong Ma, Xiaodong Ma, Li Shen, Jiankang Zhang, Guoqiang Liu, Shuyu Zhan, Baoyue Ding, Xiaoqing Lv   +7 more
doaj   +1 more source

An UPLC–ESI–MS/MS Bioanalytical Methodology for the Quantification of Gilteritinib in Human Liver Microsomes: Application to In Vitro and In Silico Metabolic Stability Estimation

Separations, 2023
Gilteritinib (Xospata®) is a tyrosine kinase inhibitor (TKI) that works by inhibiting numerous receptor tyrosine kinases, involving AXL and FMS-like tyrosine kinase 3 (FLT3).
Mohamed W. Attwa, Haitham AlRabiah, Aishah M. Alsibaee, Ali S. Abdelhameed, Adnan A. Kadi   +4 more
doaj   +1 more source

From 2-Alkylsulfanylimidazoles to 2-Alkylimidazoles: An Approach towards Metabolically More Stable p38α MAP Kinase Inhibitors

Molecules, 2017
In vitro and in vivo metabolism studies revealed that 2-alkylsulfanylimidazole ML3403 (4-(5-(4-fluorophenyl)-2-(methylthio)-1H-imidazol-4-yl)-N-(1-phenylethyl)pyridin-2-amine) undergoes rapid oxidation to the sulfoxide.
Fabian Heider, Urs Haun, Eva Döring, Mark Kudolo, Catharina Sessler, Wolfgang Albrecht, Stefan Laufer, Pierre Koch   +7 more
doaj   +1 more source

Development and Validation of a Rapid LC-MS/MS Method for Quantifying Alvocidib: In Silico and In Vitro Metabolic Stability Estimation in Human Liver Microsomes

Molecules, 2023
Alvocidib (AVC; flavopiridol) is a potent cyclin-dependent kinase inhibitor used in patients with acute myeloid leukemia (AML). The FDA has approved orphan drug designation to AVC for treating patients with AML.
Mohamed W. Attwa, Haitham AlRabiah, Adnan A. Kadi   +2 more
doaj   +1 more source

Metabolic Stability and Metabolite Characterization of Capilliposide B and Capilliposide C by LC–QTRAP–MS/MS

Pharmaceutics, 2018
Capilliposide B (LC-B) and Capilliposide C (LC-C), two new triterpenoid saponins extracted from Lysimachia capillipes Hemsl, exhibit potential anticancer activity both in vitro and in vivo. However, their metabolic process remains unclear. In this study,
Zhongzhe Cheng, Xing Zhou, Zhifeng Du, Wenyi Li, Bingying Hu, Jingkui Tian, Lin Zhang, Jiangeng Huang, Hongliang Jiang   +8 more
doaj   +1 more source