In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonist degarelix on human prostate cell growth.

Sakai M, Martinez-Arguelles DB, Patterson NH, Chaurand P, Papadopoulos V

PloS one26 Mar 2015Cited by 18 (Europe PMC)

PMID25811175PMCIDPMC4374753DOI10.1371/journal.pone.0120670PepBankPUB-25811175

Summary

Degarelix is a gonadrotropin-releasing hormone (GnRH) receptor (GnRHR) antagonist used in patients with prostate cancer who need androgen deprivation therapy. GnRHRs have been found in extra-pituitary tissues, including prostate, which may be affected by the GnRH and GnRH analogues used in therapy. The direct effect of degarelix on human prostate cell growth was evaluated. Normal prostate myofibroblast WPMY-1 and epithelial WPE1-NA22 cells, benign prostatic hyperplasia (BPH)-1 cells, androgen-independent PC-3 and androgen-dependent LNCaP prostate cancer cells, as well as VCaP cells derived from a patient with castration-resistant prostate cancer were used. Discriminatory protein and lipid fingerprints of normal, hyperplastic, and cancer cells were generated by matrix-assisted laser desorption/ionization (MALDI) mass spectrometry (MS). The investigated cell lines express GNRHR1 and GNRHR2 and their endogenous ligands. Degarelix treatment reduced cell viability in all prostate cell lines tested, with the exception of the PC-3 cells; this can be attributed to increased apoptosis, as indicated by increased caspase 3/7, 8 and 9 levels. WPE1-NA22, BPH-1, LNCaP, and VCaP cell viability was not affected by treatment with the GnRH agonists leuprolide and goserelin. Using MALDI MS, we detected changes in m/z signals that were robust enough to create a complete discriminatory profile induced by degarelix. Transcriptomic analysis of BPH-1 cells provided a global map of genes affected by degarelix and indicated that the biological processes affected were related to cell growth, G-coupled receptors, the mitogen-activated protein kinase (MAPK) pathway, angiogenesis and cell adhesion. Taken together, these data demonstrate that (i) the GnRH antagonist degarelix exerts a direct effect on prostate cell growth through apoptosis; (ii) MALDI MS analysis provided a basis to fingerprint degarelix-treated prostate cells; and (iii) the clusters of genes affected by degarelix suggest that this compound, in addition to its known use in the treatment of prostate cancer, may be efficacious in BPH.

CC BYText from Europe PMC. Highlighted sentences are the source of results.

Results from this study9

9 results from studies that gave the peptide. No result from this study comes from people.

01LabIn vitro (cells)Mechanism
In human prostate cells, degarelix reduced viability in WPMY-1, WPE1-NA22, BPH-1, LNCaP, and VCaP cells.
In plain wordsIn cells, degarelix reduced viability in all tested prostate cell lines except PC-3.
Peptide
Degarelix
Outcome
DecreaseCell viability
Study
humann: not reported in source
Human prostate cell lines
Outcome group
Receptor activity and mechanism · Cancer
Studied dose
Dose not stated
Source sentences
Summary
Degarelix treatment reduced cell viability in all prostate cell lines tested, with the exception of the PC-3 cells;
1 context sentence(design, population, supporting numbers)
Summary · context
Normal prostate myofibroblast WPMY-1 and epithelial WPE1-NA22 cells, benign prostatic hyperplasia (BPH)-1 cells, androgen-independent PC-3 and androgen-dependent LNCaP prostate cancer cells, as well as VCaP cells derived from a patient with castration-resistant prostate cancer were used.
Show in the study text Report a problemFND-2581117501
02LabIn vitro (cells)Mechanism
In PC-3 prostate cancer cells, degarelix did not reduce cell viability.
In plain wordsIn cells, degarelix did not reduce PC-3 prostate cancer cell viability.
Peptide
Degarelix
Outcome
No significant changePC-3 cell viability
Study
humann: not reported in source
PC-3 prostate cancer cells
Outcome group
Receptor activity and mechanism · Cancer
Studied dose
Dose not stated
Source sentences
Summary
Degarelix treatment reduced cell viability in all prostate cell lines tested, with the exception of the PC-3 cells;
1 context sentence(design, population, supporting numbers)
Summary · context
Normal prostate myofibroblast WPMY-1 and epithelial WPE1-NA22 cells, benign prostatic hyperplasia (BPH)-1 cells, androgen-independent PC-3 and androgen-dependent LNCaP prostate cancer cells, as well as VCaP cells derived from a patient with castration-resistant prostate cancer were used.
Show in the study text Report a problemFND-2581117502
03LabIn vitro (cells)Mechanism
In human prostate cell lines responsive to degarelix, reduced viability was attributed to increased apoptosis.
In plain wordsIn cells, reduced prostate cell viability with degarelix was attributed to increased apoptosis.
Peptide
Degarelix
Outcome
IncreaseApoptosis
Study
humann: not reported in source
Human prostate cell lines
Outcome group
Receptor activity and mechanism · Cancer
Studied dose
Dose not stated
Source sentences
Summary
Degarelix treatment reduced cell viability in all prostate cell lines tested, with the exception of the PC-3 cells; this can be attributed to increased apoptosis, as indicated by increased caspase 3/7, 8 and 9 levels.
1 context sentence(design, population, supporting numbers)
Summary · context
Normal prostate myofibroblast WPMY-1 and epithelial WPE1-NA22 cells, benign prostatic hyperplasia (BPH)-1 cells, androgen-independent PC-3 and androgen-dependent LNCaP prostate cancer cells, as well as VCaP cells derived from a patient with castration-resistant prostate cancer were used.
Show in the study text Report a problemFND-2581117503
04LabIn vitro (cells)Mechanism
In human prostate cells, degarelix increased caspase 3/7 levels as an indicator of apoptosis.
In plain wordsIn cells, degarelix increased caspase 3/7 levels.
Peptide
Degarelix
Outcome
IncreaseCaspase 3/7 levels
Study
humann: not reported in source
Human prostate cell lines
Outcome group
Receptor activity and mechanism · Cancer
Studied dose
Dose not stated
Source sentences
Summary
Degarelix treatment reduced cell viability in all prostate cell lines tested, with the exception of the PC-3 cells; this can be attributed to increased apoptosis, as indicated by increased caspase 3/7, 8 and 9 levels.
1 context sentence(design, population, supporting numbers)
Summary · context
Normal prostate myofibroblast WPMY-1 and epithelial WPE1-NA22 cells, benign prostatic hyperplasia (BPH)-1 cells, androgen-independent PC-3 and androgen-dependent LNCaP prostate cancer cells, as well as VCaP cells derived from a patient with castration-resistant prostate cancer were used.
Show in the study text Report a problemFND-2581117504
05LabIn vitro (cells)Mechanism
In human prostate cells, degarelix increased caspase 8 levels as an indicator of apoptosis.
In plain wordsIn cells, degarelix increased caspase 8 levels.
Peptide
Degarelix
Outcome
IncreaseCaspase 8 levels
Study
humann: not reported in source
Human prostate cell lines
Outcome group
Receptor activity and mechanism · Cancer
Studied dose
Dose not stated
Source sentences
Summary
Degarelix treatment reduced cell viability in all prostate cell lines tested, with the exception of the PC-3 cells; this can be attributed to increased apoptosis, as indicated by increased caspase 3/7, 8 and 9 levels.
1 context sentence(design, population, supporting numbers)
Summary · context
Normal prostate myofibroblast WPMY-1 and epithelial WPE1-NA22 cells, benign prostatic hyperplasia (BPH)-1 cells, androgen-independent PC-3 and androgen-dependent LNCaP prostate cancer cells, as well as VCaP cells derived from a patient with castration-resistant prostate cancer were used.
Show in the study text Report a problemFND-2581117505
06LabIn vitro (cells)Mechanism
In human prostate cells, degarelix increased caspase 9 levels as an indicator of apoptosis.
In plain wordsIn cells, degarelix increased caspase 9 levels.
Peptide
Degarelix
Outcome
IncreaseCaspase 9 levels
Study
humann: not reported in source
Human prostate cell lines
Outcome group
Receptor activity and mechanism · Cancer
Studied dose
Dose not stated
Source sentences
Summary
Degarelix treatment reduced cell viability in all prostate cell lines tested, with the exception of the PC-3 cells; this can be attributed to increased apoptosis, as indicated by increased caspase 3/7, 8 and 9 levels.
1 context sentence(design, population, supporting numbers)
Summary · context
Normal prostate myofibroblast WPMY-1 and epithelial WPE1-NA22 cells, benign prostatic hyperplasia (BPH)-1 cells, androgen-independent PC-3 and androgen-dependent LNCaP prostate cancer cells, as well as VCaP cells derived from a patient with castration-resistant prostate cancer were used.
Show in the study text Report a problemFND-2581117506
07LabIn vitro (cells)Mechanism
In WPE1-NA22, BPH-1, LNCaP, and VCaP cells, goserelin did not affect cell viability.
In plain wordsIn cells, goserelin did not affect viability of the named prostate cell lines.
Peptide
Goserelin
Outcome
No significant changeCell viability
Study
humann: not reported in source
WPE1-NA22, BPH-1, LNCaP, and VCaP cells
Outcome group
Receptor activity and mechanism · Cancer
Studied dose
Dose not stated
Source sentences
Summary
WPE1-NA22, BPH-1, LNCaP, and VCaP cell viability was not affected by treatment with the GnRH agonists leuprolide and goserelin.
1 context sentence(design, population, supporting numbers)
Summary · context
Normal prostate myofibroblast WPMY-1 and epithelial WPE1-NA22 cells, benign prostatic hyperplasia (BPH)-1 cells, androgen-independent PC-3 and androgen-dependent LNCaP prostate cancer cells, as well as VCaP cells derived from a patient with castration-resistant prostate cancer were used.
Show in the study text Report a problemFND-2581117507
08LabIn vitro (cells)Mechanism
In human prostate cells, degarelix induced m/z signal changes sufficient to produce a complete discriminatory profile.
In plain wordsIn cells, degarelix changed mass-spectrometry signals enough to distinguish treated prostate cells.
Peptide
Degarelix
Outcome
Direction not reportedMALDI mass-spectrometry profile
Study
humann: not reported in source
Human prostate cell lines
Outcome group
Receptor activity and mechanism · Cancer
Studied dose
Dose not stated
Source sentences
Summary
Using MALDI MS, we detected changes in m/z signals that were robust enough to create a complete discriminatory profile induced by degarelix.
1 context sentence(design, population, supporting numbers)
Summary · context
Normal prostate myofibroblast WPMY-1 and epithelial WPE1-NA22 cells, benign prostatic hyperplasia (BPH)-1 cells, androgen-independent PC-3 and androgen-dependent LNCaP prostate cancer cells, as well as VCaP cells derived from a patient with castration-resistant prostate cancer were used.
Show in the study text Report a problemFND-2581117508
09LabIn vitro (cells)Mechanism
In BPH-1 cells, degarelix affected genes related to growth, G-coupled receptors, MAPK signaling, angiogenesis, and cell adhesion.
In plain wordsIn cells, degarelix affected genes related to growth, receptor signaling, blood vessel formation, and cell adhesion.
Peptide
Degarelix
Outcome
Direction not reportedTranscriptomic biological processes
Study
humann: not reported in source
BPH-1 cells
Outcome group
Receptor activity and mechanism · Cancer
Studied dose
Dose not stated
Source sentences
Summary
Transcriptomic analysis of BPH-1 cells provided a global map of genes affected by degarelix and indicated that the biological processes affected were related to cell growth, G-coupled receptors, the mitogen-activated protein kinase (MAPK) pathway, angiogenesis and cell adhesion.
1 context sentence(design, population, supporting numbers)
Summary · context
Normal prostate myofibroblast WPMY-1 and epithelial WPE1-NA22 cells, benign prostatic hyperplasia (BPH)-1 cells, androgen-independent PC-3 and androgen-dependent LNCaP prostate cancer cells, as well as VCaP cells derived from a patient with castration-resistant prostate cancer were used.
Show in the study text Report a problemFND-2581117509

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.

Version 3Current
28 Oct 2026, 02:03 UTC
Study results updated
Version 2
27 Oct 2026, 16:35 UTC
Study data updated · source update from Europe PMC
Version 1
27 Oct 2026, 16:34 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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