Experiment 1031661
Compounds isolated
Details
| Property | Value |
|---|---|
| Pharmacology | |
| Organism | Empty organism |
| Citation | JAKEN,S: SHUPNIK,MA: BLUMBERG,PM: TASHJIAN JR,AH:. (1983). RELATIONSHIP BETWEEN MEZEREIN-MEDIATED BIOLOGICAL RESPONSES AND PHORRBOL ESTER RECEPTOR OCCUPANCY.. 43() |
| Amount utilized | |
| Compound isolated | |
| Disease | THE TITLE COMPOUND IS A WEAK COMPLETE AND STAGE 1 TUMOR PROMOTER: HOWEVER IT IS AS POTENT AS THE MOST ACTIVE PHORBOL ESTERS AS A SECOND STAGE PROMOTER AND INFLAMMATORY AGENT. THUS, MEZEREIN IS A USEFUL COMPOUND FOR STUDYING RESPONSES ASSOCIATED WITH STAGE 1 OR STAGE 2 TUMOR PROMOTION. MEZEREIN IS 25-FOLD MORE POTENT IN CAUSING A DECREASE IN BINDING OF EPIDERMAL GROWTH FACTOR TO ITS SPECIFIC CELLULAR RECEPTOR THAN IN INDUCING PROSTAGLANDIN E-2 PRODUCTION. THIS DIFFERENTIAL POTENCY FOR THESE TWO ACTIONS WAS NOT NOTED FOR OTHER PHORBOL ESTERS. MEZEREIN INTERACTS WITH THE MAJOR PHORBOL DIBUTYRATE RECEPTOR TO INCREASE PROSTAGLANDIN E-2 PRODUCTION AND ALSO EITHER WITH A DISTINCT CELLULAR TARGET WITH A HIGHER AFFINITY OR THE SAME TARGET WITH INCREASED EFFICACY TO CAUSE A DECREASE IN THE BINDING OF EPIDERMAL GROWTH FACTOR. |
| Dose amount | 12.8 NANOMOLS |
| Number | 1 |
| Qualitative result | ACTIVE |
| Animal | CELL CULTURE |
| Dose expression | ED50 |