Frequently, a generalized one-size-fits-all approach, such as protein binding does matter/does not matter, may not be applicable. An appropriate analysis requires careful consideration of both pharmacokinetic and pharmacodynamic processes, as they both contribute to the safety and efficacy of drugs. ...
plasma‐protein binding in drug researchIn broad terms, blood binding can either limit or favor the distribution of drugs to tissues. Blood binding can also direct drugs to their targets (receptors) in the plasma, blood cells or vessels. These various possibilities are presented here....
Chitinase-3-like protein 1 (CHI3L1) is a secreted glycoprotein that mediates inflammation, macrophage polarization, apoptosis, and carcinogenesis. The expression of CHI3L1 is strongly upregulated by various inflammatory and immunological diseases, including several cancers, Alzheimer’s disease, and atherosc...
Much of the toxicity associated with drugs such as clonidine, guanfacine, and tetrahydrozoline are due to their binding to imidazoline receptors. Knowledge of the imidazoline receptors may lead to new therapeutic agents and inform management of patients with imidazoline overdose. 展开 ...
G protein-coupled receptors (GPCRs) are the largest family of membrane-bound receptors and also the targets of many drugs. Understanding of the functional significance of the wide structural diversity of GPCRs has been aided considerably in recent years by the sequencing of the human genome and ...
Nonsteroidal anti-inflammatory drugs (NSAIDs) are frequently prescribed, and are known to interact with many other drugs in common usage by effects on protein binding, hepatic metabolism and renal clearance. NSAIDs can be prescribed in combination with all disease-modifying drugs in current use, ...
which reduce immunosuppression and enhance the efficacy of other anticancer drugs. The TDO inhibitor 680C91 and the dual IDO/TDO inhibitor RY103 also lower kynurenine levels, mitigating its effects on AHR signaling. Additionally, combining oncolytic adenoviral treatments, such as Delta-24-RGD and Delt...
Transport of the glutathione conjugates (GS-E) of electrophilic compounds generated during biotransformation of drugs and environmental pollutants is central to the mechanisms of defense against oxidative/electrophilic stress. In recent years emphasis has been placed on ATP-binding cassette (ABC) transport...
The overactivation of ACSL4, LPCAT3, and LOXs produces a large amount of phospholipid peroxides, which trigger ferroptosis. Phosphatidylethanolamine-binding protein 1 (PEBP1) and arachidonate 15-lipoxygenase (ALOX15) can interfere with phospholipid alcohol synthesis and induce ferroptosis [5,52]. ALO...
Sections were then washed in PBS, and incubated for 5 minutes in 1% Bovine Serum Albumin (BSA) to reduce non specific binding. The monoclonal antibodies for EBV CS1-4 (Dakopatts, diluted at 1:50) that recognizes EBV-encoded LMP1 and mouse anti-human Topoisomerase II α protein (DAKO, ...