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Items: 1 to 20 of 192


Elucidation of the pathogenic mechanism and potential treatment strategy for a female patient with spastic paraplegia derived from a single-nucleotide deletion in PLP1.

Yamamoto-Shimojima K, Imaizumi T, Aoki Y, Inoue K, Kaname T, Okuno Y, Muramatsu H, Kato K, Yamamoto T.

J Hum Genet. 2019 Apr 19. doi: 10.1038/s10038-019-0600-x. [Epub ahead of print]


Aurora kinase inhibitor VX‑680 suppresses the proliferation and migration of HUVECs and angiogenesis.

Sun X, Niu S, Zhang Z, Wang A, Yang C, Guo Z, Hao Y, Li X, Wang X.

Mol Med Rep. 2019 May;19(5):3841-3847. doi: 10.3892/mmr.2019.9996. Epub 2019 Feb 27.


What Makes a Kinase Promiscuous for Inhibitors?

Hanson SM, Georghiou G, Thakur MK, Miller WT, Rest JS, Chodera JD, Seeliger MA.

Cell Chem Biol. 2019 Mar 21;26(3):390-399.e5. doi: 10.1016/j.chembiol.2018.11.005. Epub 2019 Jan 3.


Synthesis and identification of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential Aurora A inhibitors.

Sang CY, Qin WW, Zhang XJ, Xu Y, Ma YZ, Wang XR, Hui L, Chen SW.

Bioorg Med Chem. 2019 Jan 1;27(1):65-78. doi: 10.1016/j.bmc.2018.11.006. Epub 2018 Nov 7.


Palmitoylation enables MAPK-dependent proteostasis of axon survival factors.

Summers DW, Milbrandt J, DiAntonio A.

Proc Natl Acad Sci U S A. 2018 Sep 11;115(37):E8746-E8754. doi: 10.1073/pnas.1806933115. Epub 2018 Aug 27.


Discovery and optimization of novel benzothiophene-3-carboxamides as highly potent inhibitors of Aurora kinases A and B.

Gyulavári P, Szokol B, Szabadkai I, Brauswetter D, Bánhegyi P, Varga A, Markó P, Boros S, Illyés E, Szántai-Kis C, Krekó M, Czudor Z, Őrfi L.

Bioorg Med Chem Lett. 2018 Oct 15;28(19):3265-3270. doi: 10.1016/j.bmcl.2018.05.064. Epub 2018 Jun 1.


VX-680 induces p53-mediated apoptosis in human cholangiocarcinoma cells.

Liu J, Qin CY.

Anticancer Drugs. 2018 Nov;29(10):1004-1010. doi: 10.1097/CAD.0000000000000682.


Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy.

Rossari F, Minutolo F, Orciuolo E.

J Hematol Oncol. 2018 Jun 20;11(1):84. doi: 10.1186/s13045-018-0624-2. Review.


An Investigation into the Prediction of the Plasma Concentration-Time Profile and Its Interindividual Variability for a Range of Flavin-Containing Monooxygenase Substrates Using a Physiologically Based Pharmacokinetic Modeling Approach.

Reddy VP, Jones BC, Colclough N, Srivastava A, Wilson J, Li D.

Drug Metab Dispos. 2018 Sep;46(9):1259-1267. doi: 10.1124/dmd.118.080648. Epub 2018 Jun 12.


From Cancer to Pain Target by Automated Selectivity Inversion of a Clinical Candidate.

Turk S, Merget B, Eid S, Fulle S.

J Med Chem. 2018 Jun 14;61(11):4851-4859. doi: 10.1021/acs.jmedchem.8b00140. Epub 2018 May 24. Review.


Synthesis and biological evaluation of 2,4-disubstituted phthalazinones as Aurora kinase inhibitors.

Wang W, Feng X, Liu HX, Chen SW, Hui L.

Bioorg Med Chem. 2018 Jul 23;26(12):3217-3226. doi: 10.1016/j.bmc.2018.04.048. Epub 2018 Apr 23.


The Aurora-Kinase A Phe31-Ile polymorphism as possible predictor of response to treatment in head and neck squamous cell carcinoma.

Baumann A, Buchberger AMS, Piontek G, Schüttler D, Rudelius M, Reiter R, Gebel L, Piendl G, Brockhoff G, Pickhard A.

Oncotarget. 2018 Jan 30;9(16):12769-12780. doi: 10.18632/oncotarget.24355. eCollection 2018 Feb 27.


Tozasertib Analogues as Inhibitors of Necroptotic Cell Death.

Hofmans S, Devisscher L, Martens S, Van Rompaey D, Goossens K, Divert T, Nerinckx W, Takahashi N, De Winter H, Van Der Veken P, Goossens V, Vandenabeele P, Augustyns K.

J Med Chem. 2018 Mar 8;61(5):1895-1920. doi: 10.1021/acs.jmedchem.7b01449. Epub 2018 Feb 20.


RIPK1-dependent cell death: a novel target of the Aurora kinase inhibitor Tozasertib (VX-680).

Martens S, Goossens V, Devisscher L, Hofmans S, Claeys P, Vuylsteke M, Takahashi N, Augustyns K, Vandenabeele P.

Cell Death Dis. 2018 Feb 12;9(2):211. doi: 10.1038/s41419-017-0245-7.


Identifying host regulators and inhibitors of liver stage malaria infection using kinase activity profiles.

Arang N, Kain HS, Glennon EK, Bello T, Dudgeon DR, Walter ENF, Gujral TS, Kaushansky A.

Nat Commun. 2017 Nov 1;8(1):1232. doi: 10.1038/s41467-017-01345-2.


Enhanced Functional Genomic Screening Identifies Novel Mediators of Dual Leucine Zipper Kinase-Dependent Injury Signaling in Neurons.

Welsbie DS, Mitchell KL, Jaskula-Ranga V, Sluch VM, Yang Z, Kim J, Buehler E, Patel A, Martin SE, Zhang PW, Ge Y, Duan Y, Fuller J, Kim BJ, Hamed E, Chamling X, Lei L, Fraser IDC, Ronai ZA, Berlinicke CA, Zack DJ.

Neuron. 2017 Jun 21;94(6):1142-1154.e6. doi: 10.1016/j.neuron.2017.06.008.


Inhibition of AURKA kinase activity suppresses collective invasion in a microfluidic cell culture platform.

Xia JL, Fan WJ, Zheng FM, Zhang WW, Xie JJ, Yang MY, Kamran M, Wang P, Teng HM, Wang CL, Liu Q.

Sci Rep. 2017 Jun 7;7(1):2973. doi: 10.1038/s41598-017-02623-1.


A high-throughput small molecule screen identifies synergism between DNA methylation and Aurora kinase pathways for X reactivation.

Lessing D, Dial TO, Wei C, Payer B, Carrette LL, Kesner B, Szanto A, Jadhav A, Maloney DJ, Simeonov A, Theriault J, Hasaka T, Bedalov A, Bartolomei MS, Lee JT.

Proc Natl Acad Sci U S A. 2016 Dec 13;113(50):14366-14371. doi: 10.1073/pnas.1617597113. Epub 2016 Nov 23.


Identification of human flavin-containing monooxygenase 3 substrates by a colorimetric screening assay.

Catucci G, Polignano I, Cusumano D, Medana C, Gilardi G, Sadeghi SJ.

Anal Biochem. 2017 Apr 1;522:46-52. doi: 10.1016/j.ab.2017.01.024. Epub 2017 Jan 27.


SMARCA4-inactivating mutations increase sensitivity to Aurora kinase A inhibitor VX-680 in non-small cell lung cancers.

Tagal V, Wei S, Zhang W, Brekken RA, Posner BA, Peyton M, Girard L, Hwang T, Wheeler DA, Minna JD, White MA, Gazdar AF, Roth MG.

Nat Commun. 2017 Jan 19;8:14098. doi: 10.1038/ncomms14098.

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