Drugs transporters Drug absorption OATP PGP → Drug Metabolite CYP3A4 Enterocyte OATP:organic anion transporting polypeptide:PGP:P-glycoprotein
OATP Drug absorption Drug PGP Drugs transporters OATP: organic anion transporting polypeptide；PGP: P-glycoprotein Enterocyte Drug Metabolite CYP3A4
P-glycoprotein(PGP) P-glycoprotein (PGP)known as multidrug resistance protein 1 (MDR1)or ATP-binding P-glycoprolein cassette sub-family B member 1(ABCB1). ◆An important protein of the cell membrane that pumps many foreign substances out of cells. An ATP-dependent efflux pump with broad substrate specificity
P-glycoprotein (PGP) known as multidrug resistance protein 1 (MDR1) or ATP-binding cassette sub-family B member 1 (ABCB1) . P-glycoprotein (PGP) An important protein of the cell membrane that pumps many foreign substances out of cells. An ATP-dependent efflux pump with broad substrate specificity.
PGP polymorphism ？ Cancer patients are insensitive to chemotherapy and prone to bone marrow toxicity Tumor cell Marrow cell PGP PGP Drug insensitivity Marrow toxicity
PGP polymorphism Cancer patients are insensitive to chemotherapy and prone to bone marrow toxicity Tumor cell Marrow cell PGP Drug insensitivity Marrow toxicity PGP
Drug targets---receptor Receptor genetic polymorphism refers to mutations in receptor structural or regulatory genes in a certain nu mber of individuals (>1%)in a population. Dose-effect relationship and specificity of drug efficacy are determined by receptors
Drug targets---receptor Receptor genetic polymorphism refers to mutations in receptor structural or regulatory genes in a certain nu mber of individuals individuals (>1%) in a population population. Dose-effect relationship and specificity of drug efficacy are determined by receptors
31 adrenergic receptor Ser49->Gly ◆Two mutations: Gy369-→Arg 器贸 B1 adrenergic receptor polymorphism is associated with antihypertensive efficacy 389(Arg)homozygote:remarkable antihypertensive effect. 389(Gly)homozygote and Gly389Arg heterozygote: antihypertensive effect was not significant
β1 adrenergic receptor Two mutations ： β1 adrenergic receptor polymorphism is associated with antihypertensive efficacy ： 389(Arg) homozygote: remarkable antihypertensive effect. 389(Gly) homozygote and Gly389Arg heterozygote: antihypertensive effect was not significant.