Fluorescence Studies of Drug Binding and Translocation by Membrane Transporters
Bibliographic record
Abstract
Resistance to multiple drugs is a serious limitation to chemotherapy treatment of human cancers. In addition, many clinically useful drugs show limited uptake in the intestine and cannot gain access to the brain. Three multidrug efflux pumps of the ABC superfamily (P-glycoprotein/ABCB1, MRP1/ABCC1, and BCRP/ABGG2) are responsible for most drug transport out of mammalian cells. P-glycoprotein is the best characterized of the ABC drug transporters. However, the lipophilic nature of its substrates has made it difficult to directly quantitate drug binding to the protein by classical biochemical methods, and the measurement of drug transport rates has also proved challenging. In recent years, fluorescence spectroscopic approaches have proved very useful in overcoming these problems. This chapter focuses on the use of fluorescence tools to quantitate the affinity of binding of various drugs to purified P-glycoprotein and to measure its drug transport activity in reconstituted proteoliposomes in real time. The ability of various drugs to inhibit P-glycoprotein mediated transport can also be assessed using this approach.
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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.001 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.001 | 0.001 |
| Insufficient payload (model declined to judge) | 0.002 | 0.000 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from itClassification
machine, unvalidatedMachine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.
How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".