Table 1.
Pharmacological modulation of HSF1.
| Drug | Mechanism of action | Cell type in which its effects have been described | Related pathology | References |
|---|---|---|---|---|
| Drugs that inhibit or negatively modulate HSF1 activity | ||||
| NXP800 | Inhibitor of the HSF1 pathway | Ovarian clear cell carcinoma | Cancer | [89] |
| DTHIB | Binds to the HSF1 DNA‐binding domain (DBD) | Human prostate cancer cell line (CRPC cell line C4‐2) | Cancer | [90] |
| KRIBB11 | Binds to HSF1 | Papillary Adenocarcinoma (NCI‐H820), Non‐small cell lung cancer (PC9‐ErlR), Glioblastoma (A172), Myeloma (KMS‐11), and Plasmacytoma (H929) cell lines | Cancer | [91, 92] |
| Triptolide | Inhibits the transactivation function of HSF1 | Immunoglobulin A Lambda Myeloma (MM.1S) and multiple myeloma (INA‐6) cell lines | Cancer | [94] |
| CCT251236 | Inhibits HSF1‐mediated HSP27 induction | Myeloma and plasmacytoma cell lines (KMS‐11 and H929, respectively) | Cancer | [93] |
| KNK437 | Blocks HSF1‐mediated transcription | Plasma cell leukemia (L363) cell line | Cancer (multiple myeloma) | [95] |
| Drugs that activate or positively modulate HSF1 activity | ||||
| HSF1A | Negatively modulates the activity of the TRiC/CCT complex | Fibroblast (MEF) cell line | Neurodegenerative diseases | [96] |
| 17‐AAG | Inhibits HSP90 by binding to its amino‐terminal | Lung carcinoma (A549) cells | Cancer | [100] |
| Riluzole | Unknown | Glioblastoma neuroprogenitor cells (NG108‐15) | Parkinson’s disease | [101, 102] |
| Geranylgeranylacetone | Induces the phosphorylation and nuclear translocation of heat shock factor 1 (HSF1) | Fibroblasts (CCD‐25SK) and OA cells, lung and cardiac tissue | Rheumatoid arthritis, lung injury/fibrosis, myocardial injury | [97, 98, 99] |
| Celastrol | Involved in PKC activation (translocation of PKCδ), which primes the phosphorylation of HSF1 | Fibroblast sarcoma cells (10T1/2) and primary fat SVF cells | Obesity, insulin resistance | [103] |