ArticleFrontiers in oncology2011
An optically pure apogossypolone derivative as potent pan-active inhibitor of anti-apoptotic bcl-2 family proteins.
Article in Frontiers in oncology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed.
- Hypericin, a potential new BH3 mimetic.Frontiers in pharmacology · 2022Article
- Targeting the Intrinsic Apoptosis Pathway: A Window of Opportunity for Prostate Cancer.Cancers · 2021Review
- Design, Synthesis, and Structural Characterization of Lysine Covalent BH3 Peptides Targeting Mcl-1.Journal of medicinal chemistry · 2021Article
- Recombinant MDA-7/IL24 Suppresses Prostate Cancer Bone Metastasis through Downregulation of the Akt/Mcl-1 Pathway.Molecular cancer therapeutics · 2018Article
- Discovery of Mcl-1 inhibitors from integrated high throughput and virtual screening.Scientific reports · 2018Article
- Mcl-1 Degradation Is Required for Targeted Therapeutics to Eradicate Colon Cancer Cells.Cancer research · 2017Article
- DRP-1 is required for BH3 mimetic-mediated mitochondrial fragmentation and apoptosis.Cell death & disease · 2017Article
- Article
- Small-Molecule and Peptide Inhibitors of the Pro-Survival Protein Mcl-1.ChemMedChem · 2016Review
- Novel therapy of prostate cancer employing a combination of viral-based immunotherapy and a small molecule BH3 mimetic.Oncoimmunology · 2016Article
- Roe Protein Hydrolysates of Giant Grouper (Epinephelus lanceolatus) Inhibit Cell Proliferation of Oral Cancer Cells Involving Apoptosis and Oxidative Stress.BioMed research international · 2016Article
- Killing Two Cells with One Stone: Pharmacologic BCL-2 Family Targeting for Cancer Cell Death and Immune Modulation.Frontiers in pediatrics · 2016Review
- Article
- Emerging understanding of Bcl-2 biology: Implications for neoplastic progression and treatment.Biochimica et biophysica acta · 2015Review
- Pancreatic Cancer Combination Therapy Using a BH3 Mimetic and a Synthetic Tetracycline.Cancer research · 2015Article
- New dimension in therapeutic targeting of BCL-2 family proteins.Oncotarget · 2015Review
- Therapy of prostate cancer using a novel cancer terminator virus and a small molecule BH-3 mimetic.Oncotarget · 2015Article
- Targeting BCL2-Proteins for the Treatment of Solid Tumours.Advances in medicine · 2014Review
- Evaluation and critical assessment of putative MCL-1 inhibitors.Cell death and differentiation · 2013Article
- Sabutoclax (BI97C1) and BI112D1, putative inhibitors of MCL-1, induce mitochondrial fragmentation either upstream of or independent of apoptosis.Neoplasia (New York, N.Y.) · 2013Article
Corrections and comments
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Authors and funding
15 authors.
Funding
Abstract
Our focus in the past several years has been on the identification of novel and effective pan-Bcl-2 antagonists. We have recently reported a series of Apogossypolone (ApoG2) derivatives, resulting in the chiral compound (±) BI97D6. We report here the synthesis and evaluation on its optically pure (-) and (+) atropisomers. Compound (-) BI97D6 potently inhibits the binding of BH3 peptides to Bcl-X(L), Bcl-2, Mcl-1, and Bfl-1 with IC(50) values of 76 ± 5, 31 ± 2, 25 ± 8, and 122 ± 28 nM, respectively. In a cellular assay, compound (-) BI97D6 effectively inhibits cell growth in the PC-3 human prostate cancer and H23 human lung cancer cell lines with EC(50) values of 0.22 ± 0.08 and 0.14 ± 0.02 μM, respectively. Similarly, compound (-) BI97D6 effectively induces apoptosis in the BP3 human lymphoma cell line in a dose-dependent manner. The compound also shows little cytotoxicity against bax(-/-)/bak(-/-) cells, suggesting that it kills cancers cells predominantly via a Bcl-2 pathway. Moreover, compound (-) BI97D6 displays in vivo efficacy in both a Bcl-2-transgenic mouse model and in a prostate cancer xenograft model in mice. Therefore, compound (-) BI97D6 represents a promising drug lead for the development of novel apoptosis-based therapies for cancer.
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