Transporters in regulatory science: Notable contributions from Dr. Giacomini in the past two decades

L Zhang, Q Liu, SM Huang, R Lionberger - Drug Metabolism and …, 2022 - ASPET
Transporters govern the access of molecules to cells or their exit from cells, thereby
controlling the overall distribution of drugs to their intracellular site of action. Clinically …

Downregulation of renal MRPs transporters in acute lymphoblastic leukemia mediated by the IL-6/STAT3/PXR signaling pathway

Y Zhou, AQ Nie, S Chen, MM Wang, R Yin… - Journal of …, 2021 - Taylor & Francis
Purpose Considering prior investigations on reductions of renal multidrug resistance-
associated protein (MRP) 2 and 4 transporters in mice with acute lymphoblastic leukemia …

Differences in Multicomponent Pharmacokinetics, Tissue Distribution, and Excretion of Tripterygium Glycosides Tablets in Normal and Adriamycin–Induced Nephrotic …

W Wu, R Cheng, H Boucetta, L Xu, J Pan… - Frontiers in …, 2022 - frontiersin.org
Tripterygium glycosides tablets (TGT) are widely used for treating nephrotic syndrome (NS),
but hepatotoxicity is frequently reported. The presence of underlying disease (s) can alter …

Role of Physiologically Based Pharmacokinetic Modeling and Simulation in Enabling Model‐Informed Development of Drugs and Biotherapeutics.

V Arya, K Venkatakrishnan - Journal of Clinical …, 2020 - search.ebscohost.com
The article discusses model-informed drug development (MIDD) strategies and associated
quantitative approaches have enhanced the design, development, and benefit-risk …

Hepatic Bile Acid Transporters and Drug-induced Hepatotoxicity

C Saran, KLR Brouwer - Toxicologic Pathology, 2023 - journals.sagepub.com
Drug-induced liver injury (DILI) remains a major concern in drug development from a patient
safety perspective because it is the leading cause of acute liver failure. One mechanism of …

Pharmacokinetic Imaging Using 99mTc-Mebrofenin to Untangle the Pattern of Hepatocyte Transporter Disruptions Induced by Endotoxemia in Rats

S Marie, I Hernández-Lozano, M Le Vée, L Breuil… - Pharmaceuticals, 2022 - mdpi.com
Endotoxemia-induced inflammation may impact the activity of hepatocyte transporters, which
control the hepatobiliary elimination of drugs and bile acids. 99mTc-mebrofenin is a non …

Representative Rodent Models for Renal Transporter Alterations in Human Nonalcoholic Steatohepatitis

KL Frost, JL Jilek, EL Toth, MJ Goedken… - Drug Metabolism and …, 2023 - ASPET
Alterations in renal elimination processes of glomerular filtration and active tubular secretion
by renal transporters can result in adverse drug reactions. Nonalcoholic steatohepatitis …

Feature, Function, and Information of Drug Transporter–Related Databases

J Yin, F Li, Z Li, L Yu, F Zhu, S Zeng - Drug Metabolism and Disposition, 2022 - ASPET
With the rapid progress in pharmaceutical experiments and clinical investigations, extensive
knowledge of drug transporters (DTs) has accumulated, which is valuable data for the …

Validation of Pharmacological Protocols for Targeted Inhibition of Canalicular MRP2 Activity in Hepatocytes Using [99mTc]mebrofenin Imaging in Rats

S Marie, I Hernández-Lozano, L Breuil, W Saba… - Pharmaceutics, 2020 - mdpi.com
The multidrug resistance-associated protein 2 (MRP2) mediates the biliary excretion of
drugs and metabolites.[99mTc] mebrofenin may be employed as a probe for hepatic MRP2 …

Hydrogen-deuterium exchange coupled to mass spectrometry: A multifaceted tool to decipher the molecular mechanism of transporters

K Coppieters't Wallant, C Martens - Biochimie, 2023 - Elsevier
Transporters regulate trafficking through the biological membrane of living cells and
organelles. Therefore, these proteins play an important role in key cellular processes …