epipolythiodioxopiperazine / epipolythiopiperazine-2,5-dione / SUV39H Cancer Research Results

HDN-1, epipolythiodioxopiperazine / epipolythiopiperazine-2,5-dione: Click to Expand ⟱
Features:

HDN-1 is a naturally occurring fungal epipolythiodioxopiperazine / epipolythiopiperazine-2,5-dione (ETP) isolated from the Antarctic fungus Oidiodendron truncatum GW3-13. HDN-1 has demonstrated preclinical anticancer activity and acts as a direct Hsp90 inhibitor, binding the C-terminal region of Hsp90α. Hsp90 inhibition by HDN-1 promotes degradation of multiple oncogenic client proteins, enhances downregulation of wild-type and mutant EGFR and suppresses tumour-cell proliferation. HDN-1 has also induced differentiation followed by apoptosis in selected promyelocytic leukemia cell lines. Its mechanism overlaps with that of the structurally related ETP chaetocin, which also inhibits Hsp90, but HDN-1 and chaetocin are chemically distinct compounds and should be maintained as separate products. HDN-1 should be classified as an experimental natural fungal metabolite / epipolythiodioxopiperazine / Hsp90 inhibitor, with current anticancer evidence predominantly preclinical.
HDN-1 is an analogue of chaetocin, which is a fungal mycotoxin with histone methyltransferase SUV39H1 inhibitory activity
SUV39H, suppressor of variegation 3-9 homolog: Click to Expand ⟱
Source:
Type:

SUV39H1/KMT1A (suppressor of variegation 3-9 homolog 1; H3K9 histone methyltransferase) is a SET-domain lysine methyltransferase that catalyzes methylation of histone H3 lysine 9, particularly formation of H3K9me3, a repressive chromatin mark associated with heterochromatin and transcriptional silencing. SUV39H1 regulates chromatin organization, genome stability, cellular differentiation, senescence and gene expression. In several cancers, increased SUV39H1 activity can promote epigenetic silencing of tumour-suppressive genes, stemness, proliferation and treatment resistance, although its role can vary by tumour context. In such settings, the cancer-associated direction is commonly up and the desired anticancer modulation is down or methyltransferase inhibition.



Scientific Papers found: Click to Expand⟱
7169- HDN-1,  CHA,    Identification of epipolythiodioxopiperazines HDN-1 and chaetocin as novel inhibitor of heat shock protein 90
- in-vitro, Lung, H1975 - in-vitro, Lung, HCC827 - in-vitro, Lung, A549
HSP90↓, TumCP↓, EGFR↓, STAT3↓, Akt↓, ERK↓, Raf↓, cycD1/CCND1↓, SUV39H↓,

Showing Research Papers: 1 to 1 of 1

* indicates research on normal cells as opposed to diseased cells
Total Research Paper Matches: 1

Pathway results for Effect on Cancer / Diseased Cells:


NA, unassigned(tgid=0) ⓘ

SUV39H↓, 1,  

Mitochondria & Bioenergetics(tgid=3) ⓘ

Raf↓, 1,  

Cell Death(tgid=5) ⓘ

Akt↓, 1,  

Protein Folding & ER Stress(tgid=8) ⓘ

HSP90↓, 1,  

Cell Cycle & Senescence(tgid=11) ⓘ

cycD1/CCND1↓, 1,  

Proliferation, Differentiation & Cell State(tgid=12) ⓘ

ERK↓, 1,   STAT3↓, 1,  

Migration(tgid=13) ⓘ

TumCP↓, 1,  

Angiogenesis & Vasculature(tgid=14) ⓘ

EGFR↓, 1,  

Clinical Biomarkers(tgid=22) ⓘ

EGFR↓, 1,  
Total Targets: 10

Pathway results for Effect on Normal Cells:


Total Targets: 0

Scientific Paper Hit Count for: SUV39H, suppressor of variegation 3-9 homolog
Query results interpretion may depend on "conditions" listed in the research papers.
Such Conditions may include : 
  -low or high Dose
  -format for product, such as nano of lipid formations
  -different cell line effects
  -synergies with other products 
  -if effect was for normal or cancerous cells

Filter Conditions: Pro/AntiFlg:%  IllCat:%  CanType:%  Cells:%  prod#:434  Target#:1592  State#:%  Dir#:%
  wNotes=0  sortOrder:rid,rpid

 

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