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Record W4396939418 · doi:10.1016/j.isci.2024.109978

CHK1 inhibitor SRA737 is active in PARP inhibitor resistant and CCNE1 amplified ovarian cancer

2024· article· en· W4396939418 on OpenAlexafffund
Haineng Xu, Sarah B. Gitto, Gwo‐Yaw Ho, Sergey Medvedev, Kristy Shield‐Artin, Hyoung Kim, Sally Beard, Yasuto Kinose, Xiaolei Wang, Holly E. Barker, Gayanie Ratnayake, Wei‐Ting Hwang, Ryan J. Hansen, Bryan Strouse, Snezana Milutinovic, Christian A. Hassig, Matthew J. Wakefield, Cassandra J. Vandenberg, Clare L. Scott, Fiona Simpkins

Bibliographic record

VenueiScience · 2024
Typearticle
Languageen
FieldMedicine
TopicPARP inhibition in cancer therapy
Canadian institutionsSierra Wireless (Canada)
FundersCancer Council QueenslandCancer Council NSWNational Health and Medical Research CouncilCancer Council South AustraliaMedical Research CouncilCancer Council TasmaniaNational Institutes of HealthCooperative Research Centres, Australian Government Department of IndustryCancer Council VictoriaEisaiAustralian Centre for GeomechanicsSierra OncologyUniversity of MelbourneClovis OncologyBeiGeneAustralian GovernmentMedical Research and Materiel CommandVictorian Cancer AgencyUniversity of PennsylvaniaJohns Hopkins UniversityAstraZeneca
KeywordsOvarian cancerPARP inhibitorCancer researchChemistryMedicineCancerPoly ADP ribose polymeraseInternal medicineDNABiochemistryPolymerase

Abstract

fetched live from OpenAlex

High-grade serous ovarian cancers (HGSOCs) with homologous recombination deficiency (HRD) are initially responsive to poly (ADP-ribose) polymerase inhibitors (PARPi), but resistance ultimately emerges. HGSOC with CCNE1 amplification ( CCNE1 amp ) are associated with resistance to PARPi and platinum treatments. High replication stress in HRD and CCNE1 amp HGSOC leads to increased reliance on checkpoint kinase 1 (CHK1), a key regulator of cell cycle progression and the replication stress response. Here, we investigated the anti-tumor activity of the potent, highly selective, orally bioavailable CHK1 inhibitor (CHK1i), SRA737, in both acquired PARPi-resistant BRCA1/2 mutant and CCNE1 amp HGSOC models. We demonstrated that SRA737 increased replication stress and induced subsequent cell death in vitro . SRA737 monotherapy in vivo prolonged survival in CCNE1 amp models, suggesting a potential biomarker for CHK1i therapy. Combination SRA737 and PARPi therapy increased tumor regression in both PARPi-resistant and CCNE1 amp patient-derived xenograft models, warranting further study in these HGSOC subgroups.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not 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.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.237
Threshold uncertainty score0.688

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.001
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

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.

Opus teacher head0.033
GPT teacher head0.341
Teacher spread0.308 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

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".

Quick stats

Citations12
Published2024
Admission routes2
Has abstractyes

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