ArticleLeukemia2012
MRx102, a triptolide derivative, has potent antileukemic activity in vitro and in a murine model of AML.
Article in Leukemia, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
20 citing papers in PubMed, 42 citations in OpenAlex.
- Triptolide: A Narrative Review of Its Traditional Use, Derivatives, Pharmacology, Antitumor Effect, and Clinical Applications.Cancers · 2026Review
- From immunosuppression to immune reprogramming: is triptolide a potential "immune reset" agent in autoimmune diseases?Immunologic research · 2025Review
- Article
- Triptolide Modulates the Expression of Inflammation-Associated lncRNA-PACER and lincRNA-p21 inFrontiers in pharmacology · 2021Article
- Network pharmacology-based strategy for predicting therapy targets of Tripterygium wilfordii on acute myeloid leukemia.Medicine · 2020Article
- Cetuximab-Triptolide Conjugate Suppresses the Growth of EGFR-Overexpressing Lung Cancers through Targeting RNA Polymerase II.Molecular therapy oncolytics · 2020Article
- Effects of triptolide on bone marrow-derived mesenchymal stem cells from patients with multiple myeloma.Experimental and therapeutic medicine · 2019Article
- The Effect of Triptolide in Rheumatoid Arthritis: From Basic Research towards Clinical Translation.International journal of molecular sciences · 2018Review
- The analgesic effects of triptolide in the bone cancer pain rats via inhibiting the upregulation of HDACs in spinal glial cells.Journal of neuroinflammation · 2017Article
- The triptolide derivative MRx102 inhibits Wnt pathway activation and has potent anti-tumor effects in lung cancer.BMC cancer · 2016Article
- Broad targeting of resistance to apoptosis in cancer.Seminars in cancer biology · 2015Review
- Nobiletin suppresses the proliferation and induces apoptosis involving MAPKs and caspase-8/-9/-3 signals in human acute myeloid leukemia cells.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2014Article
- Preclinical antileukemic activity, toxicology, toxicokinetics and formulation development of triptolide derivative MRx102.Cancer chemotherapy and pharmacology · 2014Article
- Article
- Glabridin mediate caspases activation and induces apoptosis through JNK1/2 and p38 MAPK pathway in human promyelocytic leukemia cells.PloS one · 2014Article
- Triptolide-mediated inhibition of interferon signaling enhances vesicular stomatitis virus-based oncolysis.Molecular therapy : the journal of the American Society of Gene Therapy · 2013Article
- In vivo quantification of active decitabine-triphosphate metabolite: a novel pharmacoanalytical endpoint for optimization of hypomethylating therapy in acute myeloid leukemia.The AAPS journal · 2013Article
- Article
- Integrative oncology meets immunotherapy: new prospects for combination therapy grounded in Eastern medical knowledge.Chinese journal of integrative medicine · 2012Review
- Immunosuppressive, anti-inflammatory and anti-cancer properties of triptolide: A mini review.Avicenna journal of phytomedicineReview
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Triptolide, isolated from the herb Tripterygium wilfordii, has been shown to potently induce apoptosis in various malignant cells by inhibiting RNA synthesis and nuclear factor-κB activity. Previously, we showed that triptolide promotes apoptosis in acute myeloid leukemia (AML) cells via the mitochondria-mediated pathway, in part, by decreasing levels of the anti-apoptotic proteins XIAP and Mcl-1. MRx102 is a triptolide derivative, currently in preclinical development. Here we show that MRx102 potently promoted apoptosis in AML cell lines, with EC(50) values of 14.5±0.6 nM and 37.0±0.9 nM at 48 h for OCI-AML3 and MV4-11 cells, respectively. MRx102, at low nanomolar concentrations, also induced apoptosis in bulk, CD34(+) progenitor, and more importantly, CD34(+)CD38(-) stem/progenitor cells from AML patients, even when they were protected by coculture with bone marrow derived mesenchymal stromal cells. MRx102 decreased XIAP and Mcl-1 protein levels and inhibited RNA synthesis in OCI-AML3 cells. In vivo, MRx102 greatly decreased leukemia burden and increased survival time in non-obese diabetic/severe combined immunodeficiency mice harboring Ba/F3-ITD cells. Collectively, we demonstrated that MRx102 has potent antileukemic activity both in vitro and in vivo, has the potential to eliminate AML stem/progenitor cells and overcome microenvironmental protection of leukemic cells, and warrants clinical investigation.
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Registered trials
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.