Lecture 6: Membrane Transport Proteins Flashcards
Transport system
-moving molecules across cell membrane
-cells need to bring in materials and excrete waste
Protein transporter steps
- bind cargo molecule on one side of membrane
- change in protein structure
- Release on opposite side
Pharmacokinetics (PK)
safety and efficacy profiles of drug
Clinical PK studies on drug interactions
-indicate transporters work together with enzymes in drug absorption and elimination
-drug substrate and inhibitor
Drug substrate
translocated across a membrane
drug inhibitor
-impair uptake/efflux of another drug
-not necessarily a substrate
ATP-dependent Transporters
-ATP-binding cassette
-ABC
Important transporters in drug distribution
-ATP-dependent
-Solute carrier (SLC)
P-glycoprotein
-important ABC transporter
-exports many drugs
-responsible for multi-drug resistance
-aka multidrug resistance protein 1
Human Solute Carrier (SLC) gene superfamily
-encodes membrane-bound transporters
-many substrates
-many of membrane transporters belong here
SLC transport substrates
-amino acids, oligopeptides
-glucose and sugars
-cations and anions
-bile salts, carboxylate, organic anions
-acetyl CoA
-essential metals, neurotransmitters, amines, vitamins, fatty acids, lipids, nucleosides, ammonium, choline, thyroid hormone, urea
Classes of Transporters
1st Class: Electrochemical-potential-driven transporters
-direction determined by electrochemical potentials
-move down concentration gradient
-NO energy input needed
-ports
uniport
one molecule one way
antiport
2+ molecules, opposite directions