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Study · Not a test of the peptide alone · 2014

1 result

Triple negative breast cancers express receptors for LHRH and are potential therapeutic targets for cytotoxic LHRH-analogs, AEZS 108 and AEZS 125.

Seitz S, Buchholz S, Schally AV, Weber F, Klinkhammer-Schalke M, Inwald EC, Perez R, Rick FG, Szalontay L, Hohla F, Segerer S, Kwok CW, Ortmann O, Engel JB

BMC cancer19 Nov 2014Cited by 40 (Europe PMC)

PMID25410881 (opens in a new tab)PMCIDPMC4289186 (opens in a new tab)DOI10.1186/1471-2407-14-847 (opens in a new tab)PepBankPUB-25410881
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Summary

BackgroundTriple negative breast cancer (TNBC) is a distinct subtype of breast cancer burdened with a dismal prognosis due to the lack of effective therapeutic agents. Receptors for LHRH (luteinizing hormone-releasing hormone) can be successfully targeted with AEZS-108 [AN-152], an analog of LHRH conjugated to doxorubicin. Our study evaluates the presence of this target LHRH receptor in human specimens of TNBC and investigates the efficacy and toxicity of AEZS-108 in vivo. We also studied in vitro activity of AEZS-125, a new LHRH analog conjugated with the highly potent natural compound, Disorazol Z.Methods69 human surgical specimens of TNBC were investigated for LHRH-R expression by immunohistochemistry. Expression of LHRH-R in two TNBC cell lines was evaluated by real time RT-PCR. Cytotoxicity of AEZS-125 was evaluated by Cell Titer Blue cytoxicity assay. LHRH- receptor expression was silenced with an siRNA in both cell lines. For the in vivo experiments an athymic nude mice model xenotransplanted with the cell lines, MDA-MB-231 and HCC 1806, was used. The animals were randomised to three groups receiving solvent only (d 1, 7, 14, i.v.) for control, AEZS-108 (d 1, 7, 14, i.v.) or doxorubicin at an equimolar dose (d 1, 7, 14, i.v.).ResultsIn human clinical specimens of TNBC, expression of the LHRH-receptor was present in 49% (n = 69).HCC 1806 and MDA-MB-231 TNBC cells expressed mRNA for the LHRH-receptor. Silencing of the LHRH-receptor significantly decreased the cytotoxic effect of AEZS-108. MDA-MB-231 and HCC 1806 tumors xenografted into nude mice were significantly inhibited by treatment with AEZS-108; doxorubicin at equimolar doses was ineffective.As compared to AEZS 108, the Disorazol Z - LHRH conjugate, AEZS-125, demonstrated an increased cytotoxicity in vitro in HCC 1806 and MDA-MB-231 TNBC; this was diminished by receptor blockade with synthetic LHRH agonist (triptorelin) pretreatment.ConclusionThe current study confirms that LHRH-receptors are expressed by a significant proportion of TNBC and can be successfully used as homing sites for cytotoxic analogs of LHRH, such as AEZS-108 and AEZS-125.
CC BYText from Europe PMC. Highlighted sentences are the source of results.

Results from this study1

No result from this study comes from a test of the peptide.

Studies that did not test the peptide alone1

In this study, Triptorelin (Trelstar, Decapeptyl) was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Triptorelin (Trelstar, Decapeptyl).

  1. 01LabNot a test of Triptorelin (Trelstar, Decapeptyl) aloneIn vitro (cells)Mechanism

    In TNBC cells, triptorelin pretreatment diminished the cytotoxicity of AEZS-125 through LHRH receptor blockade.

    In plain wordsIn cells, triptorelin pretreatment reduced AEZS-125 cytotoxicity compared with treatment without triptorelin pretreatment.

    Peptide
    Triptorelin (Trelstar, Decapeptyl)
    Outcome
    DecreaseAEZS-125 cytotoxicity after receptor blockade
    Study

    humann: not reported in source

    HCC 1806 and MDA-MB-231 TNBC cells
    Comparator
    AEZS-125 without triptorelin pretreatment
    Outcome group
    Receptor activity and mechanism · Cancer

    Source sentences

    Summary
    As compared to AEZS 108, the Disorazol Z - LHRH conjugate, AEZS-125, demonstrated an increased cytotoxicity in vitro in HCC 1806 and MDA-MB-231 TNBC; this was diminished by receptor blockade with synthetic LHRH agonist (triptorelin) pretreatment.

    In this study, Triptorelin (Trelstar, Decapeptyl) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Triptorelin (Trelstar, Decapeptyl).

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

  1. Version 2Current

    22 Oct 2026, 02:26 UTC

    Study results updated

  2. Version 1

    21 Oct 2026, 18:59 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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