ID: h-ecfaa2cbb2
Hypothesis

Parthenolide perturbs adenosine transport or metabolism upstream of ADORA2A

Covalent modulation of transporters or metabolic enzymes changes local receptor occupancy in a context-dependent manner.
🧬 ADORA2A🩺 neuropharmacology🎯 Composite 51%💱 $0.51▼4.4%proposed
EvidencePending (0%)📖 1 cit🗣 1 debates 5 support 1 oppose
✓ All Quality Gates Passed
Mechanistic 0.57 (15%) Evidence 0.46 (15%) Novelty 0.67 (12%) Feasibility 0.61 (12%) Impact 0.55 (12%) Druggability 0.43 (10%) Safety 0.42 (8%) Competition 0.59 (6%) Data Avail. 0.52 (5%) Reproducible 0.48 (5%) KG Connect 0.50 (8%) 0.506 composite

🧪 Overview

Covalent modulation of transporters or metabolic enzymes changes local receptor occupancy in a context-dependent manner.

🧬 Mechanism

🧬 Curated Mechanism Pathway

Curated pathway from expert analysis

flowchart TD
    A["Adenosine Accumulation<br/>Metabolic Stress or Hypoxia"]
    B["ADORA2A Engagement<br/>Gi-coupled Anti-inflammatory Receptor"]
    C["cAMP Suppression<br/>PKA Activity Reduction"]
    D["Microglial Activation Threshold Raised<br/>Pro-inflammatory Mediator Release Reduced"]
    E["Neuroprotection<br/>Reduced Glutamate Toxicity and Oxidative Stress"]
    F["ADORA2A Blockade<br/>Pro-inflammatory Activation Restored"]
    A --> B
    B --> C
    C --> D
    D --> E
    F -.->|"counteracts"| B
    style A fill:#1a237e,stroke:#4fc3f7,color:#4fc3f7
    style E fill:#1b5e20,stroke:#81c784,color:#81c784
    style F fill:#b71c1c,stroke:#ef9a9a,color:#ef9a9a

⚖️ Evidence

⚖️ Evidence Matrix5 supports1 contradicts
Supports
Parthenolide inhibits neuroinflammation via adenosine and A2A receptor signaling.
Phytomedicine2025PMID:41795299medium
Supports
Parthenolide ameliorates neurological deficits and neuroinflammation in mice with traumatic brain injury by suppressing STAT3/NF-κB and inflammasome activation.
Int Immunopharmacol2022PMID:35729839
Supports
Parthenolide, an NF-κB Inhibitor Ameliorates Diabetes-Induced Behavioural Deficit, Neurotransmitter Imbalance and Neuroinflammation in Type 2 Diabetes Rat Model.
Neuromolecular Med2017PMID:27553015
Supports
Arglabin regulates microglia polarization to relieve neuroinflammation in Alzheimer's disease.
J Biochem Mol Toxicol2022PMID:35289014
Supports
Parthenolide attenuates LPS-induced fever, circulating cytokines and markers of brain inflammation in rats.
Cytokine2011PMID:22004922
Contradicts
Parthenolide promiscuity may make the apparent specificity illusory.
📖 Linked Papers

No linked papers recorded for this hypothesis yet.

🏥 Translation

🧬 3D Protein Structure — ADORA2A

🧬 PDB 4EIY Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

🧠 GTEx v10 Brain ExpressionJSON

Median TPM across 13 brain regions for ADORA2A from GTEx v10.

Nucleus accumbens basal ganglia45.7 Putamen basal ganglia42.1 Caudate basal ganglia41.2 Cerebellum9.7 Cerebellar Hemisphere8.1 Cortex4.7 Frontal Cortex BA93.8 Substantia nigra3.4 Hippocampus3.3 Hypothalamus3.2 Anterior cingulate cortex BA243.0 Amygdala2.7 Spinal cord cervical c-12.5median TPM (GTEx v10)

💉 Clinical Trials

No clinical trials data linked to this hypothesis yet.

No curated ClinVar variants loaded for this hypothesis.

Run scripts/backfill_clinvar_variants.py to fetch P/LP/VUS variants.

🔍 Search ClinVar for ADORA2A →

No DepMap CRISPR Chronos data found for ADORA2A.

Run python3 scripts/backfill_hypothesis_depmap.py to populate.

💰 Estimated Development
Cost
$0
Timeline

🏆 Tournament

🏆 Arenas / Elo

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📊 Market Indicators

7d Trend
Stable
7d Momentum
▲ 0.0%
Volatility
Medium
0.0214
Events (7d)
1
Price History
▼4.4%

💾 Resource Usage

LLM Tokens
1,598
$0.0048
Total Cost
$0.0048

🔮 Predictions

🔎 Predictions vs Observations2 predictions · 0 with recorded observations
PredictionPredictedObservedStatusConf
IF human SH-SY5Y neuroblastoma cells are treated with parthenolide (10 μM, 2-hour incubation), THEN extracellular adenosine concentration will increase by >50% compared to vehicle-treated controls, asExtracellular adenosine will increase from baseline ~200 nM to >300 nM in parthenolide-treated cultures— no observation —pending0.65
IF rat primary cortical neurons are pretreated with NBTI (10 μM, equilibrated nucleoside transporter inhibitor) followed by parthenolide (10 μM, 2 hours), THEN the parthenolide-induced increase in extAdenosine concentration in parthenolide+NBTI condition will not differ significantly from NBTI-only control (within 20% of baseline)— no observation —pending0.55
🔮 Falsifiable Predictions (2)
pendingconf 65%
IF human SH-SY5Y neuroblastoma cells are treated with parthenolide (10 μM, 2-hour incubation), THEN extracellular adenosine concentration will increase by >50% compared to vehicle-treated controls, as measured by HPLC-MS quantification of cell culture supernatant.
Predicted outcome: Extracellular adenosine will increase from baseline ~200 nM to >300 nM in parthenolide-treated cultures
Falsification: Extracellular adenosine remains within 20% of vehicle control levels (<240 nM) despite parthenolide treatment
pendingconf 55%
IF rat primary cortical neurons are pretreated with NBTI (10 μM, equilibrated nucleoside transporter inhibitor) followed by parthenolide (10 μM, 2 hours), THEN the parthenolide-induced increase in extracellular adenosine will be abolished (>80% attenuation) compared to parthenolide alone, as measure
Predicted outcome: Adenosine concentration in parthenolide+NBTI condition will not differ significantly from NBTI-only control (within 20% of baseline)
Falsification: Parthenolide+NBTI condition shows adenosine levels comparable to parthenolide alone, indicating the effect is independent of equilibrative nucleoside transporters
Metadatasource: v1_phase_c_backfill · origin_type: debate_synthesizer
sourcev1_phase_c_backfill
origin_typedebate_synthesizer
_schema_version1
📊 Evidence Profile
Evidence Balance
+0%
Certainty
0%
Debates
0
Incoming
0
Outgoing
0
0 supporting 0 contradicting 0 neutral
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