ArticlePharmaceutical research2012
Combination therapy of antiandrogen and XIAP inhibitor for treating advanced prostate cancer.
Article in Pharmaceutical research, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 35 citations in OpenAlex.
- Article
- Anti-tumor Effects of IL-1β Induced TRAIL-Expressing hUCMSCs on Embelin Treated Breast Cancer Cell Lines.Asian Pacific journal of cancer prevention : APJCP · 2023Article
- Lentiviral Gene Transfer Corrects Immune Abnormalities in XIAP Deficiency.Journal of clinical immunology · 2023Article
- Embelin: A multifaceted anticancer agent with translational potential in targeting tumor progression and metastasis.EXCLI journal · 2023Review
- Embelin and Its Derivatives: Design, Synthesis, and Potential Delivery Systems for Cancer Therapy.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Article
- Second-Generation Antiandrogens: From Discovery to Standard of Care in Castration Resistant Prostate Cancer.Frontiers in oncology · 2019Review
- The Application of Embelin for Cancer Prevention and Therapy.Molecules (Basel, Switzerland) · 2018Review
- XIAP underlies apoptosis resistance of renal cell carcinoma cells.Molecular medicine reports · 2018Article
- Epigenetic modulators as therapeutic targets in prostate cancer.Clinical epigenetics · 2016Review
- Antiandrogens act as selective androgen receptor modulators at the proteome level in prostate cancer cells.Molecular & cellular proteomics : MCP · 2015Article
- GDC-0152 induces apoptosis through down-regulation of IAPs in human leukemia cells and inhibition of PI3K/Akt signaling pathway.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2015Article
- LHRH-conjugated micelles for targeted delivery of antiandrogen to treat advanced prostate cancer.Pharmaceutical research · 2014Article
- Embelin, a small molecule quinone with a co-clinical power for castrate-resistant prostate cancer.Frontiers in pharmacology · 2014Article
- Nanomicellar carriers for targeted delivery of anticancer agents.Therapeutic delivery · 2014Review
- Selectively targeting prostate cancer with antiandrogen equipped histone deacetylase inhibitors.ACS chemical biology · 2013Article
- A co-clinical approach identifies mechanisms and potential therapies for androgen deprivation resistance in prostate cancer.Nature genetics · 2013Article
- PEG-derivatized embelin as a nanomicellar carrier for delivery of paclitaxel to breast and prostate cancers.Biomaterials · 2013Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeOverexpression of the androgen receptor (AR) and anti-apoptotic genes including X-linked inhibitor of apoptosis protein (XIAP) provide tumors with a proliferative advantage. Therefore, our objective was to determine whether novel antiandrogen (CBDIV17) and XIAP inhibitor based combination therapy can treat advanced prostate cancer.
methodsCBDIV17 and embelin-6g were synthesized and their effect on cell proliferation, apoptosis, cell cycle and AR and XIAP gene silencing determined.
resultsCBDIV17 was more potent than bicalutamide and inhibited proliferation of C4-2 and LNCaP cells, IC(50) for CBDIV17 was ≈ 12 μM and ≈ 21 μM in LNCaP and C4-2 cells, respectively, whereas bicalutamide had IC(50) of ≈ 46 μM in LNCaP cells and minimal effect in C4-2 cells. CBDIV17 induced apoptosis more effectively compared to bicalutamide and significantly inhibited DNA replication. Combination of CBDIV17 and embelin resulted in supra-additive antiproliferative and apoptotic effects. Embelin downregulated AR expression and decreased androgen-mediated AR phosphorylation at Ser(81). These hydrophobic drugs were solubilized using micelles prepared with polyethylene glycol-b-poly (carbonate-co-lactide) (PEG-b-p(CB-co-LA)) copolymer. Combination therapy inhibited prostate tumor growth more effectively compared to control or monotherapy in vivo.
conclusionsOur results demonstrated that CBDIV17 in combination with embelin can potentially treat advanced prostate cancer.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.