This last point is the reason for the interest of regulatory authorities around the world, several of which (most notably the U.S. FDA and the EMA) now require that all new molecular entities (NMEs) be evaluated as P-gp substrates and inhibitors. This chapter will cover model test systems...
P-glycoprotein (Pgp) is known to play an important role in the mechanisms of ADME of a number of clinically important drugs. At the blood-brain barrier, Pgp can limit the penetration of drugs into the brain. Co-administration of Pgp inhibitors may result in drug-drug interactions (DDI) cau...
PGP 9.5封闭肽(PGP 9.5 Blocking Peptide),Proteases, Inhibitors, & Enzymes该背景资料请查看产品说明书。 产品描述 A synthetic peptide for use as a blocking control in assays to test for specificity of PGP 9.5 antibody, catalog no. 20R-PG011 ...
Structure-Activity Relationships for the Design of Small-Molecule Inhibitors One of the most important stages of the drug discovery process is the generation of lead compounds. Structure-activity relationships (SAR) are well-integra... Adriano,D.,Andricopulo,... - 《Mini Reviews》 被引量: 27发...
Studies on quinazolinones as dual inhibitors of Pgp and MRP1 in multidrug resistance. Bioorg Med Chem Lett, 2002; 12 (4): p. 571-4.Wang S, Ryder H, Pretswell I, Depledge P, Milton J, Hancox TC, et al. Studies on quinazolinones as dual inhibitors of Pgp and MRP1 in multidrug ...
Inhibitors of the ATPase activity will likely not be substrates for efflux but will inhibit efflux of other compounds (1). In contrast, a marker substrate-based Pgp transport assay can detect inhibited transport of a marker substrate by a test compound but will not reveal the mechanism. Promega...
PINmediated transport was also seen to be sensitive to inhibitors of organic anion transporters (OATs) in mammals and yeast, suggesting activation of other transport processes, as is the case with other major facilitator proteins (Wang et al., 2005; Campbell et al., 2004; Figure S1b). ...
16种具有Pgp抑制作用的上市药物对吉非替尼口服生物利用度和脑通透性的影响
Expression of G1/S‐cyclins and cyclin‐dependent kinase inhibitors in actinic keratosis and squamous cell carcinoma ic N, Manojlovic- Gacic E (2015) Expression of G1/S-cyclins and cyclin-dependent kinase inhibitors in actinic keratosis and squamous cell carcinoma. ... D Brasanac,J Stojkovic-...
The functions and structure of ABC transporters: implications for the design of new inhibitors of Pgp and MRP1 to control multidrug resistance (MDR). 机译:ABC转运蛋白的功能和结构:对设计新型Pgp和MRP1抑制剂以控制多药耐药性(MDR)的意义。 获取...