Pub. Date : 1997 Mar 1
PMID : 9119038
8 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | P-glycoprotein, a plasma membrane protein overexpressed in multidrug-resistant (MDR) cells, exhibits in vitro an ATPase activity and is responsible for the energy-dependent efflux of structurally unrelated cytotoxic drugs (like vinblastine) and various MDR-reversing agents (like verapamil and progesterone) from these MDR cells. | Progesterone | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 2 | The basal P-glycoprotein ATPase activity is increased by verapamil and progesterone, with respective half-maximal activating concentrations of approximately 1.5 microM and approximately 25 microM, and activation factors of approximately 1.7 and approximately 2.2. | Progesterone | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 3 | Vinblastine inhibits the activation of P-glycoprotein ATPase induced by verapamil or progesterone with an inhibition constant approximately 0.5 microM in both cases. | Progesterone | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 4 | In contrast, the combined modulation of P-glycoprotein ATPase by vinblastine and progesterone reveals a non-competitive relationship between these two drugs, and hence shows that they can independently and simultaneously bind P-glycoprotein on distinct sites. | Progesterone | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 5 | In contrast, the combined modulation of P-glycoprotein ATPase by vinblastine and progesterone reveals a non-competitive relationship between these two drugs, and hence shows that they can independently and simultaneously bind P-glycoprotein on distinct sites. | Progesterone | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 6 | Since verapamil and progesterone are mutual inhibitors of P-glycoprotein ATPase stimulation in a non-competitive manner, these two molecules can also bind independently P-glycoprotein on separated sites. | Progesterone | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 7 | Since verapamil and progesterone are mutual inhibitors of P-glycoprotein ATPase stimulation in a non-competitive manner, these two molecules can also bind independently P-glycoprotein on separated sites. | Progesterone | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 8 | This is confirmed here by the observation of a synergistic effect when mixtures of verapamil and progesterone are tested for the modulation of P-glycoprotein ATPase. | Progesterone | ATP binding cassette subfamily B member 1 | Homo sapiens |