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Record W3042826057 · doi:10.1002/cmdc.202000430

Identification of a Suitable Peptidic Molecular Platform for the Development of NPY(Y<sub>1</sub>)R‐Specific Imaging Agents

2020· article· en· W3042826057 on OpenAlexaff
Korbinian Krieger, Björn Wängler, Ralf Schirrmacher, Carmen Wängler

Bibliographic record

VenueChemMedChem · 2020
Typearticle
Languageen
FieldNeuroscience
TopicNeuropeptides and Animal Physiology
Canadian institutionsUniversity of Alberta
FundersDeutsche Forschungsgemeinschaft
KeywordsNeuropeptide Y receptorReceptorMetabolic stabilityChemistryPositron emission tomographyPeptideLigand (biochemistry)EndogenyDOTABiochemistryNeuropeptideMolecular biologyBiologyIn vitroMedicineNuclear medicineChelation

Abstract

fetched live from OpenAlex

Abstract NPY(Y 1 )R (neuropeptide Y receptor subtype 1) is an important target structure for tumor‐specific imaging and therapy as this receptor subtype is overexpressed in very high density and incidence especially in human breast cancer. Targeting this receptor with radiolabeled truncated analogues of the endogenous ligand NPY (neuropeptide Y) has, however, not yet resulted in satisfactory imaging results when using positron emission tomography (PET). This can be attributed to the limited stability of these PET imaging agents caused by their fast proteolytic degradation. Although highly promising NPY analogues were developed, their stability has only been investigated in very few cases. In this systematical work, we comparatively determined the stability of the five most promising truncated analogues of NPY that were developed over the last years, showing the highest receptor affinities and subtype selectivities. The stability of the peptides was assessed in human serum as well as in a human liver microsomal stability assay; these gave complementary results, thus demonstrating the necessity to perform both assays and not just conventional serum stability testing. Of the tested peptides, only [Lys(lauroyl) 27 ,Pro 30 ,Lys(DOTA) 31 ,Bip 32 ,Leu 34 ]NPY 27‐36 showed high stability against peptidase degradation; thus this is the best‐suited truncated NPY analogue for the development of NPY(Y 1 )R‐specific imaging agents.

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 score0.005
Threshold uncertainty score0.435

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
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 head0.067
GPT teacher head0.269
Teacher spread0.202 · 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

Citations6
Published2020
Admission routes1
Has abstractyes

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