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Literature summary for 3.4.21.77 extracted from

  • Oikonomopoulou, K.; Soosaipillai, A.; Diamandis, E.P.
    Evaluation of prostate-specific antigen as a novel biomarker of Hsp90 inhibition (2009), Clin. Biochem., 42, 1705-1712.
    View publication on PubMed
Search for more literature for 3.4.21.77

Activating Compound

Activating Compound Comment Organism Structure
17-allylamine-17-demethoxygeldanamycin
-
 Homo sapiens
AUY922 reduces PSA concentration in a dose-dependent manner (2fold more than insulin-like growth factor-binding protein 2) and is accompanied by androgen receptor decrease Homo sapiens
dihydrotestosterone hormonal treatment of BT-474 cells with dihydrotestosterone (an androgen) for 48 h triggers an increase of prostate-specific antigen concentration in the supernatant of these cells Homo sapiens
insulin-like growth factor-binding protein 2
-
 Homo sapiens
norgestrel hormonal treatment of BT-474 cells with norgestrel (an androgenic progestin) for 48 h triggers an increase of prostate-specific antigen concentration in the supernatant of these cells Homo sapiens

Application

Application Comment Organism
medicine PSA may serve as a sensitive biomarker of Hsp90 inhibition and may aid in selecting new chemotherapeutics Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
AUY922
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
BT-474 cell minute amounts Homo sapiens
-
LNCaP cell
-
 Homo sapiens
-
serum
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
KLK3
-
 Homo sapiens
prostate-specific antigen
-
 Homo sapiens
PSA
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000001
-
-
 Homo sapiens AUY922

Expression

Organism Comment Expression
Homo sapiens at a dose of 0.00001 mM 17-allylamine-17-demethoxygeldanamycin, PSA expression is reduced by 40%. 17-allylamine-17-demethoxygeldanamycin-treated LNCaP cells reveal about 25% inhibition of PSA secretion. Potency of AUY922 to reduce PSA expression at inhibitor concentrations lower than 0.000005 mM (non-toxic at these levels) is greater (8fold) than the potency of 17-allylamine-17-demethoxygeldanamycin. Hsp90 inhibitors target PSA secretion via the androgen receptor pathway down