The structure of nigericin

Steinrauf, L. K.; Pinkerton, Mary; Chamberlin, James W.

doi:10.1016/0006-291x(68)90249-0

Cited by 132 publications

(37 citation statements)

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“…Among the compounds that we identified for the first time as AR signaling inhibitors, we focused on nigericin (Steinrauf et al, 1968), an antibiotic derived from S. hygroscopicus, because it also inhibited the androgen-dependent growth of prostate cancer cells (see below). As shown in Fig.…”

Section: Resultsmentioning

confidence: 99%

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Pharmacological Targeting of Constitutively Active Truncated Androgen Receptor by Nigericin and Suppression of Hormone-Refractory Prostate Cancer Cell Growth

Mashima

Okabe²,

Seimiya³

2010

Mol Pharmacol

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In prostate cancer, blockade of androgen receptor (AR) signaling confers a therapeutic benefit. Nevertheless, this standard therapy allows relapse of hormone-refractory prostate cancer (HRPC) with a poor prognosis. HRPC cells often express variant ARs, such as point-mutated alleles and splicing isoforms, resulting in androgen-independent cell growth and resistance to antiandrogen (e.g., flutamide). However, a pharmacological strategy to block such aberrant ARs remains to be established. Here, we established a reporter system that monitors AR-mediated activation of a prostate-specific antigen (PSA) promoter. Our chemical library screening revealed that the antibiotic nigericin inhibits AR-mediated activation of the PSA promoter and PSA production in prostate cancer cells. Nigericin suppressed the androgen-dependent LNCaP cell growth even though the cells expressed a flutamide-resistant mutant AR. These effects were caused by AR suppression at the mRNA and post-translational levels. In HRPC 22Rv1 cells, which express the full-length AR and the constitutively active, truncated ARs lacking the carboxyl-terminal ligand-binding domain, small interfering RNA-mediated knockdown of both AR isoforms efficiently suppressed the androgen-independent cell growth, whereas knockdown of the full-length AR alone had no significant effect. It is noteworthy that nigericin was able to mimic the knockdown of both AR isoforms: it reduced the expression of the full-length and the truncated ARs, and it induced G 1 cellcycle arrest and apoptosis of 22Rv1 cells. These observations suggest that nigericin-like compounds that suppress AR expression at the mRNA level could be applied as new-type therapeutic agents that inhibit a broad spectrum of AR variants in HRPC.

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Section: Resultsmentioning

confidence: 99%

“…MO). Nigericin (Steinrauf et al, 1968) was purchased from LKT Lab., Inc. (St. Paul, MN). 17-Demethoxy-17-(2-propenylamino)geldanamycin (17-AAG) was purchased from InvivoGen (San Diego, CA).…”

Section: Methodsmentioning

confidence: 99%

Pharmacological Targeting of Constitutively Active Truncated Androgen Receptor by Nigericin and Suppression of Hormone-Refractory Prostate Cancer Cell Growth

Mashima

Okabe²,

Seimiya³

2010

Mol Pharmacol

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“…Valinomycingruppe -Valinomycin (l l, 13), Enniatin A, B und C (4,14), Makrotetrolide (15,16,17), Antamanid (18,19,20) und Beauvericin (11) -sind positiv geladen (11); monobasische Säuren der Nigericin-Gruppe -Nigericin (21,22), Monensin (21,23), Grisorixin (24,25), Dianemycin (21,26), X-206 (27), X-537A (28-31) -elektrisch neutral (l 1). Acyclische Antibiotika bauen bei der Komplexbüdung einen Pseudocyclus um das Kation (32).…”

Section: Metallkomplexe Makrocyclischer Neutraler Moleküle Derunclassified

Ammoniumselektive Disk-Elektrode mit dem Carrier-Antibiotikum Nonactin. Verfahren zur kontinuierlichen enzymatischen Elektroanalyse von Harnstoff, I. Mitteilung

Schindler¹,

Schindler²,

Aziz³

1978

Clinical Chemistry and Laboratory Medicine

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Zusammenfassung: Die Membran der beschriebenen ammoniumselektiven Disk-Elektrode besteht aus einer Polyvinylchlorid-Matrix mit der aktiven Phase Nonactin in Tris (2-ethylhexyl)-phosphat und Diphenylether als ioncnselektivem Kunststoff, der einerseits mit der Stirnfläche eines acrylglasummantelten Platin-Drahtes und andererseits mit der Meßflüssigkeit Kontakt hat, wobei sich an dieser Phasengrenze eine Potentialdifferenz ausbilden kann. Ammonium-selective disc-electrode with the carrier-antibiotic nonactin. A method for the continuous enzymatic, electrochemical determination of urea, LSummary: An ammonium-selective disc-electrode is described; the membrane consists of a polyvinylchloride-matrix with an active phase of nonactin in tris (2-ethylhexyl)phosphate and diphenyl ether as the ion-selective plastic. One side of the membrane is in contact with the solution to be measured and the other with the front surface of a platinum wire, which is enclosed in acrylic glass. This arrangement results in a very low drift potential. Einleitung

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“…The nigericic acids were isolated and their precise configuration was determined by using a chemical correlation. The opening of the terminal F ring observed for nigericic acids (2) and (3) induced the loss of the antibiotic and complexing properties. This confirms our previous results obtained with the same type of moleculeS) for (4) and (5).…”

Section: -Ch(oh)-cho)mentioning

confidence: 99%