ArticleRecent patents on anti-cancer drug discovery2026
B-9-8, a Novel Harman Dimer, Reverses ABCG2-mediated Chemotherapeutic Drug Resistance.
Article in Recent patents on anti-cancer drug discovery, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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Who cites it
2 citing papers in PubMed.
- Harmane induces apoptosis through RRM2B and suppresses colorectal cancer progression.mSystems · 2026Article
- Reversal of ABCG2-mediated MDR by VEGFR3 inhibitor (S)-SAR131675.Frontiers in pharmacology · 2026Article
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
backgroundMultidrug resistance (MDR) in cancer is a major obstacle to achieving success in clinical chemotherapy. It has been observed that overexpression of ATP-Binding Cassette (ABC) transporters plays a crucial role in MDR.
objectiveThis study aimed to find an effective resistance-reversed agent of ABC transporter. A series of new β-carboline derivatives have been synthesized and are being applied in various invention patents. One of these is B-9-8, a novel harman dimer, which was synthesized to conduct a series of experiments.
methodsIn this study, we investigated whether B-9-8 could reverse ABCG2-mediated drug resistance by using MTT assay, [
resultsThe results showed that B-9-8 could significantly increase the sensitivity to mitoxantrone, SN-38, and topotecan and effectively overcame drug resistance at non-toxic concentrations in ABCG2-overexpressing cells. Further studies showed that B-9-8 increased the intracellular accumulation of [ DISCUSSION: B-9-8, as a novel harman dimer, exhibits its reversal activity against ABCG2- mediated multidrug resistance without obvious cytotoxicity. Its actions of inhibiting ABCG2 efflux function and down-regulating the protein expression of ABCG2 are crucial for overcoming drug resistance. This makes B-9-8 a possible candidate drug for combined chemotherapy. Its inhibitory effect of ATPase activity and the strong affinity to ABCG2 further demonstrate the potential of B-9-8 as a targeted modulator for drug resistance.
conclusionOur findings indicated that B-9-8 could reverse ABCG2-mediated MDR as a potential and reversible modulator in combination with conventional chemotherapeutic drugs.
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