Published in Eur J Med Chem on June 07, 2012
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models. J Med Chem (2013) 0.84
A Potent Chemotherapeutic Strategy with Eg5 Inhibitor against Gemcitabine Resistant Bladder Cancer. PLoS One (2015) 0.78
Clotrimazole as a Cancer Drug: A Short Review. Med Chem (Los Angeles) (2016) 0.76
Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors. ACS Med Chem Lett (2015) 0.76
Eg5 inhibitor YL001 induces mitotic arrest and inhibits tumor proliferation. Oncotarget (2017) 0.75
Identification of the protein binding region of S-trityl-L-cysteine, a new potent inhibitor of the mitotic kinesin Eg5. Biochemistry (2004) 2.95
S-trityl-L-cysteine is a reversible, tight binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression. J Biol Chem (2006) 2.09
In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities. Mol Cancer Ther (2004) 1.98
Kinesins and cancer. Nat Rev Cancer (2012) 1.84
Functional roles of multiple feedback loops in extracellular signal-regulated kinase and Wnt signaling pathways that regulate epithelial-mesenchymal transition. Cancer Res (2010) 1.74
Automated analysis of vapor diffusion crystallization drops with an X-ray beam. Structure (2004) 1.53
Interaction of the mitotic inhibitor monastrol with human kinesin Eg5. Biochemistry (2003) 1.51
Motor-dependent microtubule disassembly driven by tubulin tyrosination. J Cell Biol (2009) 1.49
Positive- and negative-feedback regulations coordinate the dynamic behavior of the Ras-Raf-MEK-ERK signal transduction pathway. J Cell Sci (2009) 1.41
Kinesin-12, a mitotic microtubule-associated motor protein, impacts axonal growth, navigation, and branching. J Neurosci (2010) 1.40
The structure of the kinesin-1 motor-tail complex reveals the mechanism of autoinhibition. Science (2011) 1.39
Raf kinase inhibitor protein RKIP enhances signaling by glycogen synthase kinase-3β. Cancer Res (2011) 1.17
New chemical tools for investigating human mitotic kinesin Eg5. Bioorg Med Chem (2007) 1.12
The lower-generation polypropylenimine dendrimers are effective gene-transfer agents. Pharm Res (2002) 1.05
Crystal structure of the motor domain of the human kinetochore protein CENP-E. J Mol Biol (2004) 1.04
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5. J Med Chem (2008) 1.04
An allosteric transition trapped in an intermediate state of a new kinesin-inhibitor complex. Biochem J (2009) 1.04
In silico modelling of drug-polymer interactions for pharmaceutical formulations. J R Soc Interface (2010) 0.98
Docetaxel-resistant prostate cancer cells remain sensitive to S-trityl-L-cysteine-mediated Eg5 inhibition. Mol Cancer Ther (2010) 0.97
RAF kinase inhibitory protein (RKIP) modulates cell cycle kinetics and motility. Mol Biosyst (2010) 0.96
Molecular dissection of the inhibitor binding pocket of mitotic kinesin Eg5 reveals mutants that confer resistance to antimitotic agents. J Mol Biol (2006) 0.96
Recognition of the DNA minor groove by thiazotropsin analogues. Chembiochem (2014) 0.94
Use of hydrogen/deuterium exchange mass spectrometry and mutagenesis as a tool to identify the binding region of inhibitors targeting the human mitotic kinesin Eg5. Rapid Commun Mass Spectrom (2006) 0.93
Therapeutic strategies in the treatment of diabetic nephropathy - a translational medicine approach. Curr Med Chem (2009) 0.92
Extracellular signal-regulated kinase regulates RhoA activation and tumor cell plasticity by inhibiting guanine exchange factor H1 activity. Mol Cell Biol (2013) 0.92
Regulation of human myoblast differentiation by PEBP4. EMBO Rep (2009) 0.91
Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol. J Med Chem (2010) 0.90
Isobaric peptide termini labeling for MS/MS-based quantitative proteomics. J Proteome Res (2009) 0.90
Symmetrical and unsymmetrical analogues of isoxyl; active agents against Mycobacterium tuberculosis. Bioorg Med Chem Lett (2006) 0.90
Investigating dynamics of inhibitory and feedback loops in ERK signalling using power-law models. Mol Biosyst (2010) 0.89
How do carbon nanotubes serve as carriers for gemcitabine transport in a drug delivery system? J Mol Graph Model (2010) 0.88
Antimicrobial lexitropsins containing amide, amidine, and alkene linking groups. J Med Chem (2007) 0.88
Structure of human Eg5 in complex with a new monastrol-based inhibitor bound in the R configuration. J Biol Chem (2007) 0.88
Structural insights into human Kif7, a kinesin involved in Hedgehog signalling. Acta Crystallogr D Biol Crystallogr (2012) 0.88
Relocation of Aurora B and survivin from centromeres to the central spindle impaired by a kinesin-specific MKLP-2 inhibitor. Angew Chem Int Ed Engl (2010) 0.87
Current strategies for drug discovery through natural products. Expert Opin Drug Discov (2010) 0.87
Dual aromatase-steroid sulfatase inhibitors. J Med Chem (2007) 0.87
A comparison of the chromatographic properties of silica gel and silicon hydride modified silica gels. J Chromatogr A (2012) 0.86
Structure-activity relationship for the first-in-class clinical steroid sulfatase inhibitor Irosustat (STX64, BN83495). ChemMedChem (2011) 0.86
Antimalarial benzo[c]phenanthridines. Bioorg Med Chem Lett (2005) 0.86
Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism. J Med Chem (2013) 0.85
Analysis of the human cofilin 1 structure reveals conformational changes required for actin binding. Acta Crystallogr D Biol Crystallogr (2013) 0.85
Mutations in the human kinesin Eg5 that confer resistance to monastrol and S-trityl-L-cysteine in tumor derived cell lines. Biochem Pharmacol (2009) 0.85
Inhibition of hepatitis C virus NS5B polymerase by S-trityl-L-cysteine derivatives. Eur J Med Chem (2012) 0.85
Structural variations in protein superfamilies: actin and tubulin. Mol Biotechnol (2009) 0.85
Structural insights into a unique inhibitor binding pocket in kinesin spindle protein. J Am Chem Soc (2013) 0.85
Small-molecule inhibitors of IκB kinase (IKK) and IKK-related kinases. Pharm Pat Anal (2013) 0.84
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models. J Med Chem (2013) 0.84
Regulation of RKIP binding to the N-region of the Raf-1 kinase. FEBS Lett (2006) 0.84
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5. J Med Chem (2011) 0.84
Identification of 2-aminothiazole-4-carboxylate derivatives active against Mycobacterium tuberculosis H37Rv and the beta-ketoacyl-ACP synthase mtFabH. PLoS One (2009) 0.84
Elucidating the functionality of kinesins: an overview of small molecule inhibitors. Semin Cell Dev Biol (2011) 0.83
The Drug Discovery Portal: a resource to enhance drug discovery from academia. Drug Discov Today (2010) 0.83
The marine natural product adociasulfate-2 as a tool to identify the MT-binding region of kinesins. Biochemistry (2006) 0.83
Evaluation of anionic half generation 3.5-6.5 poly(amidoamine) dendrimers as delivery vehicles for the active component of the anticancer drug cisplatin. J Inorg Biochem (2011) 0.83
A new therapeutic strategy against hormone-dependent breast cancer: the preclinical development of a dual aromatase and sulfatase inhibitor. Clin Cancer Res (2008) 0.83
The structure of human neuronal Rab6B in the active and inactive form. Acta Crystallogr D Biol Crystallogr (2006) 0.83
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity. J Med Chem (2012) 0.82
DNA binding of a short lexitropsin. Bioorg Med Chem Lett (2004) 0.82
"Snapshots" of ispinesib-induced conformational changes in the mitotic kinesin Eg5. J Biol Chem (2013) 0.82
Solid state stabilisation of the orally delivered drugs atenolol, glibenclamide, memantine and paracetamol through their complexation with cucurbit[7]uril. Org Biomol Chem (2010) 0.81
Treatment of rhinophyma with the Versajet Hydrosurgery System. J Plast Reconstr Aesthet Surg (2007) 0.81
Combining aspects of the platinum anticancer drugs picoplatin and BBR3464 to synthesize a new family of sterically hindered dinuclear complexes; their synthesis, binding kinetics and cytotoxicity. Dalton Trans (2012) 0.81
First dual aromatase-steroid sulfatase inhibitors. J Med Chem (2003) 0.81
Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies. J Med Chem (2009) 0.80
Synthesis, full chemical characterisation and development of validated methods for the quantification of (±)-4'-methylmethcathinone (mephedrone): a new "legal high". J Pharm Biomed Anal (2011) 0.80
Elucidation of the Phase I and Phase II metabolic pathways of (±)-4'-methylmethcathinone (4-MMC) and (±)-4'-(trifluoromethyl)methcathinone (4-TFMMC) in rat liver hepatocytes using LC-MS and LC-MS². J Pharm Biomed Anal (2012) 0.80
A detailed binding free energy study of 2:1 ligand-DNA complex formation by experiment and simulation. Phys Chem Chem Phys (2009) 0.80
Design and synthesis of EGFR dimerization inhibitors and evaluation of their potential in the treatment of psoriasis. Bioorg Med Chem (2012) 0.79
Amide isosteres in structure-activity studies of antibacterial minor groove binders. Eur J Med Chem (2011) 0.79
3D-QSAR studies on chromone derivatives as HIV-1 protease inhibitors: application of molecular field analysis. Arch Pharm (Weinheim) (2008) 0.79
Identification of the benzodiazepines as a new class of antileishmanial agent. Bioorg Med Chem Lett (2006) 0.79
Structure-activity relationships and molecular modeling of sphingosine kinase inhibitors. J Med Chem (2013) 0.79
Synthesis, full chemical characterisation and development of validated methods for the quantification of the components found in the evolved "legal high" NRG-2. J Pharm Biomed Anal (2011) 0.78
Two very unusual macrocyclic flavonoids from the water lily Nymphaea lotus. Phytochemistry (2003) 0.78
A modelling study of a non-concerted hydrolytic cycloaddition reaction by the catalytic antibody H11. Bioorg Med Chem (2005) 0.78
Synthesis and antimicrobial activity of some netropsin analogues. Org Biomol Chem (2004) 0.78
Confined compression of collagen hydrogels. J Biomech (2012) 0.78
Forensic electrochemistry: the electroanalytical sensing of synthetic cathinone-derivatives and their accompanying adulterants in "legal high" products. Analyst (2014) 0.78
Resveratrol and its oligomers: modulation of sphingolipid metabolism and signaling in disease. Arch Toxicol (2014) 0.77