🧪
hypothesis

Membrane-Localized HSP90 Disruption

Hypothesis

Membrane-Localized HSP90 Disruption

Cell-penetrating peptides or lipid-conjugated inhibitors that specifically target HSP90 complexes at cellular membranes where tau aggregation initiates, concentrating HSP90 inhibition at sites of tau pathology while sparing cytoplasmic H.
🧬 HSP90AA1🩺 drug-discovery🎯 Composite 46%💱 $0.52▲5.2%active
drug discovery
EvidencePending (0%)📖 5 cit🗣 1 debates 5 support 2 oppose
✓ All Quality Gates Passed
Mechanistic 0.50 (15%) Evidence 0.50 (15%) Novelty 0.50 (12%) Feasibility 0.50 (12%) Impact 0.00 (12%) Druggability 0.50 (10%) Safety 0.50 (8%) Competition 0.50 (6%) Data Avail. 0.50 (5%) Reproducible 0.50 (5%) KG Connect 0.50 (8%) 0.455 composite
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arXiv PreprintNeurIPSNature MethodsPLOS ONE
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Composite46%

🧪 Overview

Cell-penetrating peptides or lipid-conjugated inhibitors that specifically target HSP90 complexes at cellular membranes where tau aggregation initiates, concentrating HSP90 inhibition at sites of tau pathology while sparing cytoplasmic HSP90 essential functions.

🧬 Mechanism

🔗 Mechanism from KG for HSP90AA1

Auto-built from this analysis's top knowledge-graph edges.

graph TD
    HSP90AA1["HSP90AA1"] -->|participates in| protein_folding["protein_folding"]
    FKBP5["FKBP5"] -->|protein interactio| HSP90AA1_1["HSP90AA1"]
    FKBP4["FKBP4"] -->|protein interactio| HSP90AA1_2["HSP90AA1"]
    MAPT["MAPT"] -->|regulates| HSP90AA1_3["HSP90AA1"]
    HSP90AA1_4["HSP90AA1"] -->|regulates| tau_protein["tau protein"]
    FKBP51["FKBP51"] -.->|inhibits| HSP90AA1_5["HSP90AA1"]
    Ganetespib["Ganetespib"] -.->|inhibits| HSP90AA1_6["HSP90AA1"]
    n17_AAG["17-AAG"] -.->|inhibits| HSP90AA1_7["HSP90AA1"]
    HSP90AA1_8["HSP90AA1"] -->|regulates| tau_HSP90_interactions["tau-HSP90 interactions"]
    Co_chaperones["Co-chaperones"] -->|modulates| HSP90AA1_function["HSP90AA1 function"]
    HSP90AA1_9["HSP90AA1"] -->|regulates| proteasomal_degradation_p["proteasomal degradation pathway"]
    HSP90AA1_C_terminal_domai["HSP90AA1 C-terminal domain"] -->|regulates| tau_HSP90_complex_formati["tau-HSP90 complex formation"]
    style HSP90AA1 fill:#ce93d8,stroke:#333,color:#000
    style protein_folding fill:#81c784,stroke:#333,color:#000
    style FKBP5 fill:#ce93d8,stroke:#333,color:#000
    style HSP90AA1_1 fill:#ce93d8,stroke:#333,color:#000
    style FKBP4 fill:#ce93d8,stroke:#333,color:#000
    style HSP90AA1_2 fill:#ce93d8,stroke:#333,color:#000
    style MAPT fill:#ce93d8,stroke:#333,color:#000
    style HSP90AA1_3 fill:#ce93d8,stroke:#333,color:#000
    style HSP90AA1_4 fill:#4fc3f7,stroke:#333,color:#000
    style tau_protein fill:#4fc3f7,stroke:#333,color:#000
    style FKBP51 fill:#4fc3f7,stroke:#333,color:#000
    style HSP90AA1_5 fill:#4fc3f7,stroke:#333,color:#000
    style Ganetespib fill:#4fc3f7,stroke:#333,color:#000
    style HSP90AA1_6 fill:#4fc3f7,stroke:#333,color:#000
    style n17_AAG fill:#4fc3f7,stroke:#333,color:#000
    style HSP90AA1_7 fill:#4fc3f7,stroke:#333,color:#000
    style HSP90AA1_8 fill:#4fc3f7,stroke:#333,color:#000
    style tau_HSP90_interactions fill:#4fc3f7,stroke:#333,color:#000
    style Co_chaperones fill:#4fc3f7,stroke:#333,color:#000
    style HSP90AA1_function fill:#4fc3f7,stroke:#333,color:#000
    style HSP90AA1_9 fill:#4fc3f7,stroke:#333,color:#000
    style proteasomal_degradation_p fill:#81c784,stroke:#333,color:#000
    style HSP90AA1_C_terminal_domai fill:#4fc3f7,stroke:#333,color:#000
    style tau_HSP90_complex_formati fill:#4fc3f7,stroke:#333,color:#000

⚖️ Evidence

⚖️ Evidence Matrix5 supports2 contradicts
Supports
Folding or holding?-Hsp70 and Hsp90 chaperoning of misfolded proteins in neurodegenerative disease.
J Biol Chem2022PMID:35398094medium
Supports
Hsp90-interacting Co-chaperones and their Family Proteins in Tau Regulation: Introducing a Novel Role for Cdc37L1.
Neuroscience2021PMID:33246057medium
Supports
The Hsp90 cochaperone, FKBP51, increases Tau stability and polymerizes microtubules.
J Neurosci2010PMID:20071522medium
Supports
To fold or not to fold: modulation and consequences of Hsp90 inhibition.
Future Med Chem2009PMID:20161407medium
Supports
Hsp90 co-chaperones, FKBP52 and Aha1, promote tau pathogenesis in aged wild-type mice.
Acta Neuropathol Commun2021PMID:33832539medium
Contradicts
Pharmacological mechanism and therapeutic efficacy of Icariside II in the treatment of acute ischemic stroke: a systematic review and network pharmacological analysis.
BMC Complement Med Ther2022PMID:36180911medium
Contradicts
Mapping the pathogenic nexus: Gene overlap and protein interaction networks in Alzheimer's and breast cancer as a precursor to protein structure prediction and analysis.
Adv Protein Chem Struct Biol2025PMID:40973403medium
📖 Linked Papers

No linked papers recorded for this hypothesis yet.

🏥 Translation

🧬 3D Protein Structure — HSP90AA1

🧬 PDB 2CG9 Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

💉 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 HSP90AA1 →

No DepMap CRISPR Chronos data found for HSP90AA1.

Run python3 scripts/backfill_hypothesis_depmap.py to populate.

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📊 Market Indicators

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💾 Resource Usage

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🔮 Predictions

🔎 Predictions vs Observations2 predictions · 0 with recorded observations
PredictionPredictedObservedStatusConf
IF we administer TAT-conjugated HSP90 membrane-binding domain peptide (10 mg/kg, i.p., daily) to 8-month-old 3xTg-AD mice for 4 weeks compared to vehicle or non-targeting TAT-scramble peptide, THEN we≥30% reduction in Sarkhosal-insoluble tau by ELISA; ≥40% improvement in probe trial latency (mean 25-30 sec improvement from ~45 sec baseline)— no observation —pending0.55
IF we treat SH-SY5Y cells expressing P301L tau with lipid-conjugated HSP90 inhibitors (membrane-targeted) at 1 μM compared to equimolar 17-AAG (cytoplasmic HSP90 inhibitor), THEN membrane-targeted inh≥50% reduction in AT8 fluorescence intensity with membrane-targeted inhibitor; cytoplasmic HSP70 mRNA levels ≥80% of vehicle control— no observation —pending0.65
🔮 Falsifiable Predictions (2)
pendingconf 65%
IF we treat SH-SY5Y cells expressing P301L tau with lipid-conjugated HSP90 inhibitors (membrane-targeted) at 1 μM compared to equimolar 17-AAG (cytoplasmic HSP90 inhibitor), THEN membrane-targeted inhibitors will reduce phospho-tau (AT8) by ≥50% while cytoplasmic HSP70 induction (HSP90 activity read
Predicted outcome: ≥50% reduction in AT8 fluorescence intensity with membrane-targeted inhibitor; cytoplasmic HSP70 mRNA levels ≥80% of vehicle control
Falsification: Both inhibitors produce equivalent (<20% difference) reduction in AT8 signal AND equivalent (<20% difference) cytoplasmic HSP70 induction, disproving selectivity for membrane HSP90 as mechanism
pendingconf 55%
IF we administer TAT-conjugated HSP90 membrane-binding domain peptide (10 mg/kg, i.p., daily) to 8-month-old 3xTg-AD mice for 4 weeks compared to vehicle or non-targeting TAT-scramble peptide, THEN we will observe ≥30% reduction in Sarkhosal-insoluble tau aggregates in hippocampal synaptoneurosomes
Predicted outcome: ≥30% reduction in Sarkhosal-insoluble tau by ELISA; ≥40% improvement in probe trial latency (mean 25-30 sec improvement from ~45 sec baseline)
Falsification: No significant difference (p>0.05) in Sarkhosal-insoluble tau between treatment and vehicle groups, OR Morris water maze performance shows no improvement, disproving efficacy of membrane-targeted HSP9
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