ArticleJournal of medicinal chemistry2010
Exploring the structural requirements for inhibition of the ubiquitin E3 ligase breast cancer associated protein 2 (BCA2) as a treatment for breast cancer.
Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Who cites it
43 citing papers in PubMed, 152 citations in OpenAlex.
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- Disulfiram ameliorates STING/MITA-dependent inflammation and autoimmunity by targeting RNF115.Cellular & molecular immunology · 2024Article
- Structure-activity relationship of anticancer drug candidate quinones.Turkish journal of chemistry · 2024Article
- Cytotoxicity, acute and sub-chronic toxicities of the leaves of Bauhinia thonningii (Schumach.) Milne-Redh. (Caesalpiniaceae).BMC complementary medicine and therapies · 2023Article
- Cytotoxicity of the methanol extracts and compounds of Brucea antidysenterica (Simaroubaceae) towards multifactorial drug-resistant human cancer cell lines.BMC complementary medicine and therapies · 2023Article
- Disulfiram Oxy-Derivatives Suppress Protein Retrotranslocation across the ER Membrane to the Cytosol and Initiate Paraptosis-like Cell Death.Membranes · 2022Article
- Discovery of Triple Inhibitors of Both SARS-CoV-2 Proteases and Human Cathepsin L.Pharmaceuticals (Basel, Switzerland) · 2022Article
- RNF115 Inhibits the Post-ER Trafficking of TLRs and TLRs-Mediated Immune Responses by Catalyzing K11-Linked Ubiquitination of RAB1A and RAB13.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2022Article
- Multifaceted Roles of the E3 Ubiquitin Ligase RING Finger Protein 115 in Immunity and Diseases.Frontiers in immunology · 2022Review
- Article
- Phthalimide Analogs Enhance Genotoxicity of Cyclophosphamide and Inhibit Its Associated Hypoxia.Frontiers in chemistry · 2022Article
- E3 ubiquitin ligase RNF126 affects bladder cancer progression through regulation of PTEN stability.Cell death & disease · 2021Article
- Botanicals from the leaves ofHeliyon · 2020Article
- Cytotoxycity and antiplasmodial activity of phenolic derivatives from Albizia zygia (DC.) J.F. Macbr. (Mimosaceae).BMC complementary medicine and therapies · 2020Article
- Cytotoxic Constituents of the Bark ofEvidence-based complementary and alternative medicine : eCAM · 2020Article
- Ubiquitin-specific protease 7 downregulation suppresses breast cancer in vitro.Turkish journal of biology = Turk biyoloji dergisi · 2020Article
- Antimicrobial Peptide Reverses ABCB1-Mediated Chemotherapeutic Drug Resistance.Frontiers in pharmacology · 2020Article
- Deubiquitinase ubiquitin-specific protease 9X regulates the stability and function of E3 ubiquitin ligase ring finger protein 115 in breast cancer cells.Cancer science · 2019Article
- Cytotoxicity of Crude Extract and Isolated Constituents of theEvidence-based complementary and alternative medicine : eCAM · 2019Article
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
The zinc-ejecting aldehyde dehydrogenase (ALDH) inhibitory drug disulfiram (DSF) was found to be a breast cancer-associated protein 2 (BCA2) inhibitor with potent antitumor activity. We herein describe our work in the synthesis and evaluation of new series of zinc-affinic molecules to explore the structural requirements for selective BCA2-inhibitory antitumor activity. An N(C=S)S-S motif was found to be required, based on selective activity in BCA2-expressing breast cancer cell lines and against recombinant BCA2 protein. Notably, the DSF analogs (3a and 3c) and dithio(peroxo)thioate compounds (5d and 5f) were found to have potent activity (submicromolar IC(50)) in BCA2 positive MCF-7 and T47D cells but were inactive (IC(50) > 10 microM) in BCA2 negative MDA-MB-231 breast cancer cells and the normal breast epithelial cell line MCF10A. Testing in the isogenic BCA2 +ve MDA-MB-231/ER cell line restored antitumor activity for compounds that were inactive in the BCA2 -ve MDA-MB-231 cell line. In contrast, structurally related dithiocarbamates and benzisothiazolones (lacking the disulfide bond) were all inactive. Compounds 5d and 5f were additionally found to lack ALDH-inhibitory activity, suggestive of selective E3 ligase-inhibitory activity and worthy of further development.
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Registered trials
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