List of publications utilizing BI 2536 (Axon 1129) purchased from Axon Medchem
(Total 125 publication citations listed; updated up to January 2023)
Koike, A. (2023). Molekular und zellbiologischer Ansatz hin zu neuartigen Medikamenten gegen\(Echinococcus\)\(multilocularis\) (Doctoral dissertation, Universität Würzburg).
Juan, L.S., Freije, A., Sanz-Gómez, N. et al. DNA damage triggers squamous metaplasia in human lung and mammary cells via mitotic checkpoints. Cell Death Discov. 9, 21 (2023). https://doi.org/10.1038/s41420-023-01330-3
Lebrec, V., Poteau, M., Morretton, J. P., & Gavet, O. (2022). Chk1 dynamics in G2 phase upon replication stress predict daughter cell outcome. Developmental Cell, 57(5), 638-653.
Mehl, J. L., Earle, A., Lammerding, J., Mhlanga, M., Vogel, V., & Jain, N. (2022). Blockage of lamin-A/C loss diminishes the pro-inflammatory macrophage response. Iscience, 25(12), 105528.
ЧЕОНГ, Ш. И. А. ГИПЕРСТАБИЛИЗИРОВАННЫЕ ЛИПОСОМЫ, ПОВЫШАЮЩИЕ НАПРАВЛЕННОЕ ТАРГЕТИРОВАНИЕ МИТОТИЧЕСКИХ КЛЕТОК.
Le Roux-Bourdieu, M., Dwivedi, D., Harry, D., & Meraldi, P. (2022). PLK1 controls centriole distal appendage formation and centrobin removal via independent pathways. Journal of cell science, 135(8), jcs259120.
2021
Hino, M., Iemura, K., Ikeda, M., Itoh, G., & Tanaka, K. (2021). Chromosome alignment‐maintaining phosphoprotein CHAMP1 plays a role in cell survival through regulating Mcl‐1 expression. Cancer science, 112(9), 3711-3721.
Dantas, M., Oliveira, A., Aguiar, P., Maiato, H., & Ferreira, J. G. (2021). Mechanosensitive control of mitotic entry. bioRxiv, 2021-09.
Lim, Y., De Bellis, D., Sandow, J. J., Capalbo, L., D’Avino, P. P., Murphy, J. M., ... & Kumar, S. (2021). Phosphorylation by Aurora B kinase regulates caspase-2 activity and function. Cell Death & Differentiation, 28(1), 349-366.
Dehapiot, B., Clément, R., Bourdais, A., Carrière, V., Huet, S., & Halet, G. (2021). RhoA-and Cdc42-induced antagonistic forces underlie symmetry breaking and spindle rotation in mouse oocytes. PLoS Biology, 19(9), e3001376.
Herz, M. (2021). Genome wide expression profiling of Echinococcus multilocularis (Doctoral dissertation, Universität Würzburg).
Lee, H. S., Min, S., Jung, Y. E., Chae, S., Heo, J., Lee, J. H., ... & Cho, H. (2021). Spatiotemporal coordination of the RSF1-PLK1-Aurora B cascade establishes mitotic signaling platforms. Nature Communications, 12(1), 5931.
2020
O’Byrne, S. N., Scott, J. W., Pilotte, J. R., Santiago, A. D. S., Langendorf, C. G., Oakhill, J. S., ... & Drewry, D. H. (2020). In depth analysis of kinase cross screening data to identify CAMKK2 inhibitory scaffolds. Molecules, 25(2), 325.
Ng, C. Z., Matthews, A. A., Sum, R., Goh, S. M. P., Xu, A., Yap, L. W., & Cheong, I. (2020). Calibrated liposomal release of the anti-mitotic agent BI-2536 increases the targeting of mitotic tumor cells. European Journal of Pharmaceutics and Biopharmaceutics, 157, 183-190.
Sanz-Gómez, N., de Pedro, I., Ortigosa, B., Santamaría, D., Malumbres, M., de Cárcer, G., & Gandarillas, A. (2020). Squamous differentiation requires G2/mitosis slippage to avoid apoptosis. Cell Death & Differentiation, 27(8), 2451-2467.
2019
Cabral, G., Laos, T., Dumont, J., & Dammermann, A. (2019). Differential requirements for centrioles in mitotic centrosome growth and maintenance. Developmental cell, 50(3), 355-366.
https://www.sciencedirect.com/science/article/pii/S1534580719305222
Zhang, T., Xin, G., Jia, M., Zhuang, T., Zhu, S., Zhang, B., ... & Zhang, C. (2019). The Plk1 kinase negatively regulates the Hedgehog signaling pathway by phosphorylating Gli1. J Cell Sci, 132(2), jcs220384.
Wang, R., Wang, Y., Qu, L., Chen, B., Jiang, H., Song, N., & Xie, J. (2019). Iron-induced oxidative stress contributes to α-synuclein phosphorylation and up-regulation via polo-like kinase 2 and casein kinase 2. Neurochemistry international, 125, 127-135.
Moon, J., & Roh, S. (2018). Inhibition of Polo-like Kinase 1 Prevents the Male Pronuclear Formation Via Alpha-tubulin Recruiting in In vivo-fertilized Murine Embryos. 한국수정란이식학회지 (KJET), 33(4), 229-235.
Sanz‐Gómez, N., Freije, A., Ceballos, L., Obeso, S., Sanz, J. R., García‐Reija, F., ... & Gandarillas, A. (2018). Response of head and neck epithelial cells to a DNA damage‐differentiation checkpoint involving polyploidization. Head & neck, 40(11), 2487-2497.
Lee, J. K., Ha, G. H., Kim, H. S., & Lee, C. W. (2018). Oncogenic potential of BEX4 is conferred by Polo-like kinase 1-mediated phosphorylation. Experimental & molecular medicine, 50(10), 138.
Liu, T. T., Yang, K. X., Yu, J., Cao, Y. Y., Ren, J. S., Hao, J. J., ... & Wang, M. R. (2018). Co-targeting PLK1 and mTOR induces synergistic inhibitory effects against esophageal squamous cell carcinoma. Journal of Molecular Medicine, 96(8), 807-817.
M.C. Helms et al. Mitotic-dependent phosphorylation of leukemia-associated RhoGEF (LARG) by Cdk1.
Cell Signal. 2016 Jan;28(1):43-52.
2015
V. Zuco et al. PLK1 is a critical determinant of tumor cell sensitivity to CPT11 and its inhibition enhances the drug antitumor efficacy in squamous cell carcinoma models sensitive and resistant to camptothecins.
Oncotarget. 2015 Apr 20;6(11):8736-49.
V. Baran et al. PLK1 regulates spindle formation kinetics and APC/C activation in mouse zygote.
Zygote. 2015 Jul 15:1-8.
T.G. Tut et al. Upregulated Polo-Like Kinase 1 Expression Correlates with Inferior Survival Outcomes in Rectal Cancer.
PLoS One. 2015 Jun 5;10(6):e0129313.
I.Gasic et al. Centrosome age regulates kinetochore-microtubule stability and biases chromosome mis-segregation.
Elife. 2015 Aug 19;4.
Application of RNAi to Genomic Drug Target Validation in Schistosomes.
Guidi A, Mansour NR, Paveley RA, Carruthers IM, Besnard J, Hopkins AL, et al. (2015)
PLoS Negl Trop Dis 9(5): e0003801.
Suppression of Interferon β gene transcription by inhibitors of Bromodomain and Extra-Terminal (BET) family members.
N Malik, S Vollmer, SK Nanda, M Lopez-Pelaez, A Prescott, N Gray and P Cohen.
Biochem. J. (2015) April 20. [E-pub ahead of print]
JNK2 controls fragmentation of the Golgi complex and G2/M transition trough phosphorylation of GRASP65.
RI Cervigni, R Bonavita, ML Barretta, D Spano, I Ayala1, N Nakamura, D Corda and A Colanzi.
J. Cell Sci. 2015, doi: 10.1242/jcs.164871
Pharmacological inhibition of Polo-like kinase 1 (PLK1) by BI-2536 decreases the viability and survival of hamartin and tuberin deficient cells via induction of …
M Valianou, AM Cox, B Pichette, S Hartley…
Cell Cycle. 2015;14(3):399-407.
Modeling the mitotic regulatory network identifies highly efficient anti-cancer drug combinations
Y Wu, X Zhuo, Z Dai, X Guo, Y Wang, C Zhang…
Mol Biosyst. 2015 Feb;11(2):497-505.
BI 6727 and GSK461364 suppress growth and radiosensitize osteosarcoma cells, but show limited cytotoxic effects when combined with conventional treatments
RFE Bogado, JA Pezuk, HF de Oliveira…
Anticancer Drugs. 2015 Jan;26(1):56-63.
PLK1 Phosphorylates PAX3-FOXO1, the Inhibition of Which Triggers Regression of Alveolar Rhabdomyosarcoma
V Thalhammer, LA Lopez-Garcia, D Herrero-Martin…
Cancer Res. 2015 Jan 1;75(1):98-110.
Multiple requirements of PLK1 during mouse oocyte maturation
P Solc, TS Kitajima, S Yoshida, A Brzakova, M Kaido…
PLoS One. 2015 Feb 6;10(2):e0116783.
Cyclin F suppresses B-Myb activity to promote cell cycle checkpoint control
DK Klein, S Hoffmann, JK Ahlskog, K O'Hanlon…
Nat Commun. 2015 Jan 5;6:5800.
2014
Inhibition of endocytic vesicle fusion by Plk1-mediated phosphorylation of vimentin during mitosis
K Ikawa, A Satou, M Fukuhara, S Matsumura…
Cell Cycle. 2014;13(1):126-37.
OPTINEURIN-DERIVED POLYPEPTIDES, THEIR NUCLEIC ACIDS AND USES THEREOF.
US Patent Application 20140336126 (2014).
Phosphorylation-mediated stabilization of Bora in mitosis coordinates Plx1/Plk1 and Cdk1 oscillations.
Feine, O., Hukasova, E., Bruinsma, W., Freire, R., Fainsod, A., Gannon, J., ... & Brandeis, M.
Cell Cycle, 2014, 13(11), 1727-1736.
Differing requirements for Augmin in male meiotic and mitotic spindle formation in Drosophila.
MS Savoian and DM Glover. Open Biol. 2014 4 (5), 140047.
Targeting Echinococcus multilocularis Stem Cells by Inhibition of the Polo-Like Kinase EmPlk1
A. Schubert et al.PLOS 2014, online Jun 5, 2014.
(*BI 6727 (Volasertib) was procured from Axon Medchem as well)
BRCA2 Coordinates the Activities of Cell-Cycle Kinases to Promote Genome Stability
K. Yata et al. Cell Reports, 2014, Available online 15 May 2014
Multisite phosphorylation of C-Nap1 releases it from Cep135 to trigger centrosome disjunction.
T. Hardy et al. J. Cell Sci, 2014.02.24.
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
P. Ciceriet al. Nat. Chem. Biol. 2014, 10, 305-312.
(*BI 2536, TG 101348, BI-D1870, AZ 3146 etc were procured from Axon Medchem)
PLK1 expression and BI 2536 effects in childhood acute lymphoblastic leukemia.
J.C. Oliveira et al. Pediatric Blood & Cancer. 2014, 61, 1227-1231.
PLK1-inhibition can cause radiosensitization or radioresistance dependent on the treatment schedule.
C. Lund-Andersen et al. Radiotherapy and Oncology, 2014, 110, 355-361.
Polo-Like Kinase 2, a NovelADAM17 Signaling Component, Regulates TNFα Ectodomain Shedding.
J. Schwarz et al. J. Biol. Chem. 2014, 289, 3080-3093.
CUL3 and protein kinases: Insights from PLK1/KLHL22 interaction.
T Metzger et al. Cell Cycle, 2013, 12, 2291-2296.
In vitro targeting of Polo-like kinase 1 in bladder carcinoma. Comparative effects of four potent inhibitors.
M.S. Brassescoet al.Cancer Biology & Therapy, 2013, 14 (7), 1-10.
(*BI 2536, BI 6727, GW843682X and GSK461364 were procured from Axon Medchem (Axon 1129, 1473, 1688 and 1131).
Aurora B suppresses microtubule dynamics and limits central spindle size by locally activating KIF4A.
R.N. Bastos et al. J. Cell Biol. 2013, 202, 605-621.
Polo-like kinase 1 inhibition causes decreased proliferation by cell cycle arrest, leading to cell death in glioblastoma.
J.A. Pezuk et al. Cancer Gene Therapy, 2013, 20, 499-506.
(*BI 2536, BI 6727, GW843682X and GSK461364 were pprocured from Axon Medchem)
PDK1 Signaling Towards PLK1-Myc Activation Confers Oncogenic Transformation and Tumor Initiating Cell Activation and Resistance to mTOR-targeted Therapy.
J. Tan et al. Cancer Discovery, 2013, 3, 1156.
(*60 inhibitors including BI2536 were purchased from Axon Medchem)
Cyclin-dependent kinase 4 signaling acts as a molecular switch between syngenic differentiation and neural transdifferentiation in human mesenchymal stem cells.
J. Lee et al. Cell Cycle, 2013, 12, 0-1.
PLK1 Signaling in Breast Cancer Cells Cooperates with Estrogen Receptor-Dependent Gene Transcription.
M. Wierer et al. Cell Repots, 2013, 3 (6), 2021–2032.
Inhibition of Polo-Like Kinase 1 Induces Cell Cycle Arrest and Sensitizes Glioblastoma Cells to Ionizing Radiation.
J.A. Pezuk et al. Cancer Biother. Radiopharm. 2013, 28(7), 516-522.
Cell cycle-dependent localization ofCHK2 at centrosomes during mitosis.
G. Chouinard et al. Cell Div. 2013, 8, 7.
Polo-like kinase 1 is essential for the first mitotic division in the mouse embryo.
V. Baran et al. Mol. Reprod. Devel. 2013, 80 (7), 522-534.
Centrobin controls mother–daughter centriole asymmetry in Drosophila neuroblasts.
J. Januschke et al. Nature Cell Biol. 2013, 15, 241–248.
Ubiquitylation-dependent localization of PLK1 in mitosis.
J. Beck et al. Nature Cell Biol. 2013, 15, 430-439.
PCM1 Recruits Plk1 to the Pericentriolar Matrix to Promote Primary Cilia Disassembly before Mitotic Entry.
G. Wang et al. J. Cell Sci. 2013, 126, 1355-1365.
(45 publications from 2012 and previous summary)
Neighbor communities in drug combination networks characterize synergistic effect.
J. Zou et al. Mol. BioSyst. 2012, 8, 3185-3196.
Mammalian Neurogenesis Requires Treacle-Plk1 for Precise Control of Spindle Orientation, Mitotic Progression, and Maintenance of Neural Progenitor Cells.
D. Sakai et al. PLoS Genet 2012, 8, e1002566.
Cdk1 and Plk1 mediate a CLASP2 phospho-switch that stabilizes kinetochore–microtubule attachments.
A.R.R. Maia et al. J. Cell Biol. 2012, 199, 285-301.
Polo-like kinase 1 (PLK1) inhibition suppresses cell growth and enhances radiation sensitivity in medulloblastoma cells.
P.S. Harris et al. BMC Cancer 2012, 12, 80.
Regulation of inositol 1,4,5-trisphosphate receptor type 1 function during oocyte maturation by MPM-2 phosphorylation.
V. Vanderheyden et al. Cell Calcium, 2009, 46, 56–64.
α-Synuclein Aggregation and Ser-129 Phosphorylation-dependent Cell Death in Oligodendroglial Cells.
C.L. Kragh et al. J. Biol. Chem. 2009, 284, 10211-10222.
PLK1 Down-Regulates Parainfluenza Virus 5 Gene Expression.
D. Sun et al. PLoS Pathog 2009, 5, e1000525.
ATRactivation and replication fork restart are defective in FANCM-deficient cells.
R.A. Schwab et al. EMBO J. 2010, 29, 806-818
The Plk1 Inhibitor BI 2536 Temporarily Arrests Primary Cardiac Fibroblasts in Mitosis and Generates Aneuploidy In Vitro.
B. Lu et al. PLoS ONE 2010, 5, 9
Translationally controlled tumor protein interacts with nucleophosmin during mitosis in ES cells.
H. Johansson et al. Cell Cycle 2010, 9, 2160-2169.
Activation of cyclin B1–Cdk1 synchronizes events in the nucleus and the cytoplasm at mitosis.
O. Gavet et al. J. Cell Biol. 2010, 189, 247.
Plk1 negatively regulates Cep55 recruitment to the midbody to ensure orderly abscission.
R.N. Bastos et al. J. Cell Biol. 2010, 191, 751-760.
Schistosoma mansoni Polo-like kinase 1: A mitotic kinase with key functions in parasite reproduction.
T. Long et al. Int. J. Parasitol. 2010, 40, 1075–1086.
Aurora-A expressing tumour cells are deficient for homology-directedDNAdouble strand-break repair and sensitive to PARP inhibition.
T. Sourisseau et al. EMBO Mol. Medicine, 2010, 2, 130-142.
Polo-like kinase 1 is involved in hepatitis C virus replication by hyperphosphorylating NS5A.
Y.C. Chen et al. J. Virol, 2010, 84 (16), 7983-7993.
A single starfishAurorakinase performs the combined functions of Aurora-A and Aurora-B in human cells.
Y. Abe et al. J. Cell Sci. 2010, 123, 3978-3988.
Polo-like Kinase 1 Activated by the Hepatitis B Virus X Protein Attenuates Both theDNADamage Checkpoint andDNARepair Resulting in Partial Polyploidy.
L. Studach et al. J. Biol. Chem. 2010, 285, 30282-30293.
SPAT-1/Bora acts with Polo-like kinase 1 to regulatePARpolarity and cell cycle progression.
A. Noatynska et al. Development 2010, 137, 3315-3325.
In Silico Analysis of Kinase Expression Identifies WEE1 as a Gatekeeper against Mitotic Catastrophe in Glioblastoma.
S.E. Mir et al. Cancer Cell, 2010, 18, 244–257.
The Transforming Parasite Theileria Co-opts Host Cell Mitotic and Central Spindles to Persist in Continuously Dividing Cells.
C. von Schubert et al. PLOS Biol. 2010, 8(9): e1000499.
Nek9 is a Plk1-activated kinase that controls early centrosome separation through Nek6/7 and Eg5.
M.T. Bertran et al. EMBO J. 2011, 30, 2634-2647.
Differential control of Eg5-dependent centrosome separation by Plk1 and Cdk1.
E. Smith et al. EMBO J. 2011, 30, 2233-2245.
Small Molecule Kinase Inhibitor Screen Identifies Polo-Like Kinase 1 as a Target for Neuroblastoma Tumor-Initiating Cells.
N. Grinshtein et al. Cancer Res. 2011, 71, 1385.
Characterization of kinases involved in the phosphorylation of aggregated α-synuclein.
E.A. Waxman et al. J. Neurosci. Res. 2011, 89 (2) 231–247.
Effect of Ser-129 Phosphorylation on Interaction of α-Synuclein with Synaptic and Cellular Membranes.
N.P. Visanji et al. J. Biol. Chem. 2011, 286, 35863-35873.
Polo-like kinase 1 is required for localization of Posterior End Mark protein to the centrosome-attracting body and unequal cleavages in ascidian embryos.
T. Negishi et al. Development, Growth & Differentiation, 2011, 53 (1), 76–87.
A genetic screen identifies BRCA2 and PALB2 as key regulators of G2 checkpoint maintenance.
T. Menzel et al. EMBO reports 2011, 12, 705-712.
The polo-like kinase inhibitor BI2536 exhibits potent activity against malignant plasma cells and represents a novel therapy in multiple myeloma.
H.J. Stewart et al. Experimental Hematol. 2011, 39 (3), 330–338.
Bcl-xL phosphorylation at Ser49 by polo kinase 3 during cell cycle progression and checkpoints.
J. Wang et al Cellular Signal. 2011, 23 (12), 2030–2038.
Integrated computational model of cell cycle and checkpoint reveals different essential roles of Aurora-A and Plk1 in mitotic entry.
J. et al. Mol. BioSyst. 2011, 7, 169-179.
A Sensitized RNA Interference Screen Identifies a Novel Role for the PI3K p110γ Isoform in Medulloblastoma Cell Proliferation and Chemoresistance.
A.S. Guerreiro et al. Mol Cancer Res. 2011, 9, 925.
A critical balance between Cyclin B synthesis and Myt1 activity controls meiosis entry in Xenopus oocytes.
M. Gaffré et al. Development, 2011, 138, 3735-3744.
Aurora A and Aurora B jointly coordinate chromosome segregation and anaphase microtubule dynamics.
N. Hégarat et al. J. Cell Biol. 2011, 195 (7) 1103-1113.
A primary microcephaly protein complex forms a ring around parental centrioles.
J.H. Sir et al. Nature Genetics, 2011, 43, 1147–1153.
Plk1 and CK2 Act in Concert to Regulate Rad51 duringDNADoubleStrandBreak Repair.
K. Yata et al. Mol. Cell, 2012, 45 (3), 371–383.
Cyclin E drives human keratinocyte growth into differentiation.
A. Freije et al. Oncogene, 2012, 31, 5180-5192.
ProliferationStateand Polo-like Kinase1 Dependence of Tumorigenic Colon Cancer Cells.
F. Francescangeli et al. Stem Cells 2012, 30(9):1819-30,
Reciprocal Activation Between PLK1 and Stat3 Contributes to Survival and Proliferation of Esophageal Cancer Cells.
Y. Zhang et al. Gastroenterology, 2012, 142 (3), 521–530.e3.
Protein Kinases as Potential Targets for Novel Anti-Schistosomal Strategies.
S. Beckmann et al. Curr. Pharm. Design, 2012, 18 (24), 3579-3594.
Furry Promotes Aurora A-mediated Polo-like Kinase 1 Activation.
M. Ikeda et al. J. Biol. Chem. 2012, 287, 27670-27681.
A Cell Cycle Role for the Epigenetic Factor CTCF-L/BORIS.
M. Rosa-Garrido et al. PLoS ONE, 2012, 7(6), e39371
Tankyrase-1 function at telomeres and during mitosis is regulated by Polo-like kinase-1-mediated phosphorylation.
G.H. Ha et al. Cell Death Differ. 2012, 19, 321-332.
Reduced Efficacy of the Plk1 Inhibitor BI 2536 on the Progression of Hepatocellular Carcinoma due to Low Intratumoral Drug Levels.
J. Haupenthal. Neoplasia. 2012, 14(5), 410-419.
Human cells enter mitosis with damagedDNAafter treatment with pharmacological concentrations of genotoxic agents.
P.M. Kubara et al. Biochem. J. 2012, 446(3), 373-381
Misshapen-like kinase 1 (MINK1) Is a Novel Component of Striatin-interacting Phosphatase and Kinase (STRIPAK) and Is Required for the Completion of Cytokinesis.
T. Hyodo et al. J. Biol. Chem. 2012, 287, 25019-25029.
