ArticleMolecular pharmacology2019
Colchicine Binding Site Agent DJ95 Overcomes Drug Resistance and Exhibits Antitumor Efficacy.
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Article in Molecular pharmacology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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9citing papers in PubMed
2.0field-weighted citation impact, top 12% of its field
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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
9 citing papers in PubMed, 31 citations in OpenAlex.
- Therapeutic potential of colchicine-binding site inhibitors in breast cancer brain metastasis.Cancer letters · 2026Review
- PM534, a Novel Colchicine Site Tubulin Inhibitor with Broad-Spectrum and Resistance-Overcoming Antitumor Activity.Molecular cancer therapeutics · 2026Article
- Development of a potential nano-based delivery system combining Colchicine-loaded lipid nanocapsules and BIOT-NFL-peptide to target glioblastoma.International journal of pharmaceutics: X · 2025Article
- Recent Advancements in the Development of HDAC/Tubulin Dual-Targeting Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Novel Antimitotic Agent SP-1-39 Inhibits Head and Neck Squamous Cell Carcinoma.Journal of dental research · 2024Article
- Molecular interactions at the colchicine binding site in tubulin: An X-ray crystallography perspective.Drug discovery today · 2022Review
- Discovery of novel quinoline-based analogues of combretastatin A-4 as tubulin polymerisation inhibitors with apoptosis inducing activity and potent anticancer effect.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor.Journal of medicinal chemistry · 2021Article
- Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review.Pharmaceuticals (Basel, Switzerland) · 2020Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
14 authors at 1 institution in 2 countries.
Kinsie E ArnstDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).ORCID 0000-0002-4429-590X
Yuxi WangDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).
Zi-Ning LeiDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).ORCID 0000-0003-1696-8385
Dong-Jin HwangDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).ORCID 0000-0002-0055-1916
Gyanendra KumarDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).
Dejian MaDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).ORCID 0000-0003-1393-3953
Deanna N ParkeDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).
Qiang ChenDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).
Jinliang YangDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).
Stephen W WhiteDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).ORCID 0000-0001-8188-5944
Tiffany N SeagrovesDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).ORCID 0000-0002-6937-943X
Zhe-Sheng ChenDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.).ORCID 0000-0002-8289-097X
Duane D MillerDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.) dmiller@uthsc.edu.
Wei LiDepartment of Pharmaceutical Sciences, College of Pharmacy (K.E.A., D.-J.H., D.M., D.D.M., W.L.), and Department of Pathology (D.N.P., T.N.S.), the University of Tennessee Health Science Center, Memphis, Tennessee; State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy (Y.W., Q.C., J.Y.), and Department of Respiratory Medicine (Y.W.), West China Hospital, Sichuan University, Chengdu, China; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York (Z.-N.L., Z.-S.C.); and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee (G.K., S.W.W.) wli@uthsc.edu.ORCID 0000-0002-9522-4474
St. Jude Children's Research Hospital · US
Funding
Targeting the colchicine site in tubulin for advanced melanomaR01CA148706 · NCI · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI LI, WEI, MILLER, DUANE D · 2011 to 2025
$5.3MSelective Targeting Survivin for Cancer TherapyR01CA193609 · NCI · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI LI, WEI · 2016 to 2020
$1.9MThe Role of HIF-1alpha in Breast Cancer Stem Cell ActivityR01CA138488 · NCI · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI SEAGROVES, TIFFANY NICOLE · 2010 to 2014
$1.5MAcquisition of a Q-TOF Mass SpectrometerS10OD010678 · OD · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI LI, WEI · 2012 to 2012
$325kMass Spectrometer for Small Molecule Drug DevelopmentS10OD016226 · OD · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI MEIBOHM, BERND · 2014 to 2014
$316kAcquisition of a 400MHz Solution NMR System with an AutosamplerS10RR026377 · NCRR · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI LI, WEI · 2010 to 2010
$253kNCI NIH HHS R01 CA138488NCI NIH HHS R01 CA148706NCI NIH HHS R01 CA193609NCRR NIH HHS S10 RR026377NIH HHS S10 OD010678NIH HHS S10 OD016226
Abstract
Interfering with microtubule dynamics is a well-established strategy in cancer treatment; however, many microtubule-targeting agents are associated with drug resistance and adverse effects. Substantial evidence points to ATP-binding cassette (ABC) transporters as critical players in the development of resistance. Herein, we demonstrate the efficacy of DJ95 (2-(1
Indexed as
AnimalsATP-Binding Cassette TransportersCell Line, TumorCell MovementCell SurvivalColchicineCrystallography, X-RayDrug Resistance, NeoplasmFemaleHEK293 CellsHumansHuman Umbilical Vein Endothelial CellsImidazolesMaleMelanomaMiceATP-Binding Cassette TransportersColchicineImidazolesPyridinesSmall Molecule LibrariesTubulinTubulin Modulators
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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.