Characterization of Src kinase kinetic and inhibition mechanisms
Bibliographic record
Abstract
Src Kinase catalyzes phosphoryl transfer from ATP to tyrosine residues on proteins. In this study, we have investigated the steady state kinetics of the Src kinase reaction in a microfluidic chip‐based mobility shift assay using the Caliper LabChip 3000 instrument. Saturation kinetics is observed with both ATP and a gastrin‐derived peptide substrate. The bireactant kinetics observed suggest a sequential kinetic mechanism. Comparison of the rates of catalysis in the presence of H 2 O and D 2 O yields a significant solvent kinetic isotope effect on Vmax with a value of 3.3 ± 0.2, but no effect on V/K for either ATP or the peptide substrate. This observation suggests that the isotope sensitive step occurs after the first irreversible step, the release of the first product in the reaction cycle. To further support drug discovery efforts, the mechanism of small molecule inhibitors of Src kinase was determined. Steady state kinetic analysis of the data suggests that all of the compounds are competitive against ATP. The binding of these inhibitors to the ATP site is further supported by double inhibition (Yonetani‐Theorell) analysis, using a known competitive inhibitor of Src kinase.
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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 | 0.001 | 0.001 |
| 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 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.001 |
| Insufficient payload (model declined to judge) | 0.001 | 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".