Isozyme-specific inhibition of GSTP1-1: a crucial element in cancer-targeting drugs
Why this work is in the frame
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Bibliographic record
Abstract
-transferase pi 1 (GSTP1), because it is one of the overexpressed antioxidant enzymes in cancer and has been targeted for the purpose of killing cancer cells. However, most available GSTP1 inhibitors do not show selectivity towards the isozyme. This can potentially lead to many side effects. Therefore, the search for optimal selective GSTP1 inhibitors is still underway. The novelty of this review stems from highlighting the significance of selectively targeting GSTP1. We also addressed the structural feature of the enzyme which challenges the design of novel selective GSTP1 inhibitors. We then provide guidelines to help resolve these challenges to help design future compounds. The first objective of this review is to present a brief literature review to highlight the importance of selectively targeting GSTP1. Briefly, the lack of selectivity towards GSTP1 has resulted in extensive side effects which limited reaching advanced clinical trials. We screened publications on many potential inhibitors, including some that reached phase I and II clinical trials, for their ability to bind with GSTP1, GSTM, and GSTA. All compounds appear to bind different GST isozymes (at least to some extent). The second objective is to present differences in the structures of GST isotypes (GSTP1, GSTM, GSTA) which could allow selectively targeting a certain isotype. Our modelling results highlight the importance of certain structural moieties for better selective binding to GSTP1.
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Full frame distilled prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.
Codex and Gemma teacher scores by category
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 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 | 0.001 | 0.000 |
| Insufficient payload (model declined to judge) | 0.000 | 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 it