Group:SMART:P-glycoprotein: Why Cancer Drugs Fail: Difference between revisions
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In our model of P-glycoprotein, the hydrophilic regions are highlighted in <font color=magenta><b>magenta</b></font>, the hydrophobic regions are highlighted in <font color=lilac><b>violet</b></font>, the active site residues for the drug Verapamil* is highlighted in <font color=lime><b>green</b></font>, and the Nucleotide Binding Domains or NBDs are highlighted in <font color=gold><b>yellow</b></font>. Since P-glycoprotein is a dimer, a molecule consisting of two similar subunits, only half of the dimer (or one of two subunits) is shown in our model. | In our model of P-glycoprotein, the hydrophilic regions are highlighted in <font color=magenta><b>magenta</b></font>, the hydrophobic regions are highlighted in <font color=lilac><b>violet</b></font>, the active site residues for the drug Verapamil* is highlighted in <font color=lime><b>green</b></font>, and the Nucleotide Binding Domains or NBDs are highlighted in <font color=gold><b>yellow</b></font>. Since P-glycoprotein is a dimer, a molecule consisting of two similar subunits, only half of the dimer (or one of two subunits) is shown in our model. | ||
Because P-glycoprotein is embedded in the cell membrane, it contains both hydrophilic and hydrophobic regions. If you look closely at the protein model, you will notice a band of violet or a hydrophobic band. The hydrophobic band is the region of the protein that is embedded in the cell membrane (since the inside of the cell membrane is hydrophobic and the outside of the cell membrane is hydrophilic). Both the hydrophobic and hydrophilic regions are critical in P-glycoprotein’s function in transporting drugs out of the cell. The active site residues that are important for the transport of Verapamil are highlighted with the color <font color=lime><b>green</b></font>. These residues are H60, A63, L64, S218, I302, L335, A338, F724, I864, G868, F938, T941, L971, V978, G980, and A981. The Nucleotide Binding Domains (NBDs), which are highlighted in <font color=gold><b>yellow</b></font>, are important because after binding to ATP, the conformation of the protein changes. By changing the conformation of the protein, drugs are transported out of the cell. P-glycoprotein is also an active transporter because it requires energy of ATP in order to transports drugs out of cells. | Because P-glycoprotein is embedded in the cell membrane, it contains both hydrophilic and hydrophobic regions. If you look closely at the protein model, you will notice a band of violet or a hydrophobic band. The hydrophobic band is the region of the protein that is embedded in the cell membrane (since the inside of the cell membrane is hydrophobic and the outside of the cell membrane is hydrophilic). Both the hydrophobic and hydrophilic regions are critical in P-glycoprotein’s function in transporting drugs out of the cell. The active site residues that are important for the transport of Verapamil are highlighted with the color <font color=lime><b>green</b></font>. These residues are <i>H60, A63, L64, S218, I302, L335, A338, F724, I864, G868, F938, T941, L971, V978, G980,</i> and <i>A981</i>. The Nucleotide Binding Domains (NBDs), which are highlighted in <font color=gold><b>yellow</b></font>, are important because after binding to ATP, the conformation of the protein changes. By changing the conformation of the protein, drugs are transported out of the cell. P-glycoprotein is also an active transporter because it requires energy of ATP in order to transports drugs out of cells. | ||